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   2019| Oct-Dec  | Volume 15 | Issue 65  
    Online since September 19, 2019

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A green method for preparation of curcuminoid-rich Curcuma longa extract and evaluation of its anticancer activity
Likit Lateh, Supreeya Yuenyongsawad, Haixia Chen, Pharkphoom Panichayupakaranant
Oct-Dec 2019, 15(65):730-735
Background: Curcuminoids, i.e., curcumin, demethoxycurcumin, and bisdemethoxycurcumin are a major active constituent of Curcuma longa L., which possess antioxidant, anti-inflammatory, antitumor, anticancer, and various other biological activities. Objective: To establish a green method for preparation of curcuminoid-rich C. longa extracts (CRE) using microwave-assisted extraction (MAE) together with a simple one-step fractionation and to investigate the anticancer activity of CRE compared with the three marker curcuminoids. Materials and Methods: MAE was used as a green extraction method, and a macroporous resin (Diaion® HP-20) column was used for fractionation of C. longa extract to produce CRE. The sulforhodamine B assay was used to evaluate in vitro anticancer activity of the curcuminoids. Results: The optimal conditions of MAE for extraction of curcuminoids are employing ethanol as the solvent and using three irradiation cycles in a microwave powered at 900 W (one cycle is 3 min power-on and 30 s power-off). The curcuminoid extract was subsequently fractionated on a Diaion® HP-20 column eluted with 55% and 60% v/v ethanol, respectively, to obtain CRE that contained total curcuminoids of 88% w/w. CRE exhibited good anticancer activities against A549, MCF-7, HeLa, and HT-29 cells, with 50% inhibitory concentration values of 5.2, 4.5, 7.5, and 8.3 μg/mL, respectively, which almost equals those of the marker curcuminoids. Conclusion: This study indicated a potential use of CRE for anticancer purposes in food and nutraceutical applications. CRE has more advantages than pure curcuminoids for industrial applications in terms of using simple, low-cost, and environmentally friendly processes.
  2,945 354 -
Tannic acid-rich porcupine bezoars induce apoptosis and cell cycle arrest in human colon cancer cells
Peng-Nian Yew, Yau-Yan Lim, Wai-Leng Lee
Oct-Dec 2019, 15(65):523-531
Background: Porcupine bezoar, a phytobezoar used as traditional medicine, was recently claimed to effectively treat cancer. However, there is a lack of scientific evidence to prove the claim. Objectives: This study aimed to scientifically examine porcupine bezoars as a potential anticancer agent and to investigate their principal bioactive constituents. Materials and Methods: The porcupine bezoars were extracted using methanol and further Sephadex LH-20 column chromatography was used to enrich the tannins content. The inhibitory effects of the crude extracts on a panel of cancer cell lines were first determined using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Then, the anticancer activities of the enriched fractions in selected cell lines were analyzed, while the chemical composition of the active fraction was identified using liquid chromatography––electrospray ionization-tandem mass spectrometry. Results: Crude extracts of black date and powdery date effectively inhibited colon cancer cell lines HT-29 and HT-116, but not the normal colon cells, and their tannin-enriched fractions demonstrated higher inhibitory effects when compared to the extracts. Further, the fractions arrested cell cycle at S phase and induced apoptosis in treated colon cancer cells with a similar effect to that of commercial tannic acid. Lipoxygenase activity which plays a role in tumorigenesis of colon cancer was also inhibited by these fractions. Chemical analysis found that both the enriched fractions and commercial tannic acid share similar chemical constituents, including gallic acid and its derivatives (polygalloyl glucose). Conclusion: Together, the results suggest that tannic acid in porcupine bezoars may inhibit colon cancer cells by interfering cell proliferation and triggering program cell death in the cells.
  2,899 165 -
Varthemia iphionoides and Pelargonium graveolens Extracts as a Treatment of Breast Cancer Implanted in Diabetic Mice
Rana Y Halees, Wamidh H Talib, Reem A Issa
Oct-Dec 2019, 15(65):698-707
Background: The relationship between cancer and type 2 diabetes is well documented. However, studies are very limited to test new therapies for both diseases in the same biological system. This study was conducted to test the potential of two antidiabetic plants from Jordan (Varthemia iphionoides and Pelargonium graveolens) to treat breast cancer implanted in diabetic mice. Materials and Methods: Different solvent extracts of both plants were prepared, and the in vitro antiproliferative activity was tested against MCF-7, T47D, and EMT6/P breast cancer cell lines in addition to Vero normal cell lines. Normal as well as diabetic Balb/C mice were transplanted with EMT6/P cell line, and in vivo antitumor activity was assessed for the most potent plant extract according to the in vitro results. Histological examination of tumors was performed using standard hematoxylin and eosin staining protocol. Apoptosis was detected using TUNEL colorimetric assay. Vascular endothelial growth factor expression of cancer cells was detected using ELISA. Aspartate aminotransferase, alanine aminotransferase, and creatinine were measured as well as interferon-gamma, interleukin-2 (IL-2), IL-4, and IL-10. Results: V. Iphionoides dichloromethane (DCM) extract was the most potent extract and could inhibit cell growth of breast cancer cell lines (EMT6, MCF-7, and T47D). It showed high ability in targeting growth and progression of breast cancer inoculated in diabetic and non-diabetic mice. Conclusion: V. iphionoids DCM extract is a promising therapeutic option to treat breast cancer in diabetic cases. However, further studies are essential to characterize the active ingredients in this extract.
  2,142 140 -
Antioxidant flavonoids from Alhagi maurorum with hepatoprotective effect
Muneera S M. Al-Saleem, Lamya H Al-Wahaib, Wael M Abdel-Mageed, Yaser G Gouda, Hanaa M Sayed
Oct-Dec 2019, 15(65):592-599
Background: Alhagi maurorum, commonly used in folk medicine, has been reported to have several biological activities. Objective: We have studied the antioxidant chemical components from A. maurorum to determine their in vitro antiproliferative and hepatoprotective activities. Materials and Methods: The alcoholic extract of A. maurorum root was subjected to a successive solvent fractionation and various chromatographic techniques guided by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay to isolate their antioxidant active compounds. The structures of the isolated compounds were identified through the extensive use of nuclear magnetic resonance and mass spectroscopy coupled with correlation to known compounds. The antioxidant and cytotoxic activities of the isolated compounds were quantified using DPPH and 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assays, respectively. The hepatoprotective activity of each extract and the total flavonoid fraction were assessed quantitatively on carbon tetrachloride (CCl4)-induced hepatotoxicity in rats. Results: Fourteen flavonoids, including four aglycones (1–4) and ten glycosides (5–14), were isolated. The flavonoid glycosides (6–14) are being reported for the first time to our knowledge. The free aglycones, those of the flavonol type, exhibited strong antioxidant and antiproliferative activities. The flavonoid glycosides exhibited weak cytotoxic activity against the hepatocellular carcinoma cell line. The total flavonoid fraction showed the strongest hepatoprotective activity against CCl4-induced hepatotoxicity. Conclusion: A total of 14 flavonoids were identified from A. maurorum; nine of them were isolated for the first time. Flavonoids were the main chemical group identified from the A. maurorum root extracts, and they are responsible for the hepatoprotective activity. The findings set up a scientific explanation for the folkloric administration of A. maurorum in the treatment of hepatic disorders.
  2,031 209 -
Effect of Piper nigrum ethanolic extract on human breast cancer cell growth and cell migration
Benjaporn Buranrat, Supavadee Boontha
Oct-Dec 2019, 15(65):538-546
Background: Piper nigrum (PN) is widely used as a traditional medicine, which has anti-cancer activity among others. Objective: Our study purposes to illuminate the inhibition of PN effects on breast cancer cells growth and migration along with its mechanisms. Materials and Methods: The piperine in the young fruit of PN extract was determined by the high-performance liquid chromatography method. Growth inhibition with a mechanism of PN extract was studied in the MCF-7 cells using sulforhodamine B assay, cell cycle analysis, colony formation, caspase-3 activity, and reactive oxygen species formation. Furthermore, the anti-migratory effects of PN were investigated using wound healing, matrigel migration, and gelatin zymography assay. Finally, PN mechanism was determined by reverse transcription polymerase chain reaction and Western blotting for the gene and protein levels. Results: Piperine level was showed at a high concentration in the PN extract. Further, the PN extract suppressed Rac1 mRNA expression in the mevalonate (MVA) pathway as well as repressed Rac1 and RhoA protein expression. Interestingly, PN stimulated growth inhibition in dose- and time-dependent as well as being accompanied by increasing the G1 phase arrest and inhibiting cyclin D1 and NF-κB as well as inducing caspase-3 expression. The PN extract inhibited MCF-7 cell migration by reducing matrix metalloproteinases (MMP) 9 protein expression as well as MMP 2, MMP 9, VEGFA, and ICAMP1 gene expression. Conclusion: PN could be herbal medicine for anti-cancer and anti-migratory activities with a correlation to the MVA pathway; therefore, PN maybe deserving further to study as a new candidate for treating breast cancer.
  2,031 171 -
Optimization of ultrasonic-assisted extraction of flavonoids and anti-oxidant capacity from the whole plant of Andrographis echioides (L.) nees by response surface methodology and chemical composition analysis
Jayalakshmi Ramasamy, Ruckmani Kandasamy, Selvamani Palanisamy, Subramanian Nadesan
Oct-Dec 2019, 15(65):547-556
Background: Andrographis echioides (L.) Nees is an annual herb mainly distributed in India and Sri Lanka. In traditional medicine system, the plant is used for treating various ailments such as fevers, skin diseases, stomach ache, toothache, snake bite, and eczema. The whole plant of A. echioides was reported as the rich source of flavonoids. Ultrasound-assisted extraction (UAE) is an effective extraction method used for secondary metabolite extraction from various plant materials over conventional methods. Today, the response surface methodology (RSM) is a successful statistical tool used to optimize the various extraction conditions of the secondary metabolite from various sources. Objective: The objective of this study is to optimize the UAE conditions such as ethanol concentration (50%–100%), solvent-to-solid ratio (10–50 mL/g), and sonication time (20–60 min) for the extraction of flavonoids and anti-oxidant capacity (AOC) from A. echioides (L.) Nees whole plant (AEWP) using the RSM strategy with Box–Behnken design (BBD). Materials and Methods: UAE conditions, i.e. ethanol concentration, solvent-to-solid ratio, and sonication time, were optimized with the corresponding responses of flavonoid yield and %DPPHAOCand %ABTSAOCby RSM. The effect of ultrasound on plant material was analyzed using Scanning electron microscope (SEM). The efficiency of the optimized extract was analyzed using Fourier-transformed infrared spectroscopy (FTIR) and liquid chromatography-mass spectra (LC-MS). Results: The BBD provided adequate mathematical models that accurately describe the behavior of the technique and help to predict the flavonoid yield, %DPPHAOCand %ABTSAOCfrom AEWP. The optimized UAE conditions were 77% of ethanol concentration, 35 mL/g of solvent-to-solid ratio, and 41 min of sonication time. Under these extraction conditions, UAE would obtain a maximum of 10.91 ± 0.04 mg CE/g for flavonoid yield, 87.36 ± 0.06% for %DPPHAOC, and 85.14 ± 0.03% for %ABTSAOC.The obtained experimental results of all the responses are in good agreement with the predicted values. SEM analysis explores the effect of UAE compared with the conventional extraction. The FTIR and LC-MS analysis revealed that the optimized extract of AEWP is rich in flavonoids; apart from the known flavonoids, five new flavonoids were identified from this optimization study. Conclusion: The study confirmed that UAE was the effective extraction method for the extraction of flavonoids from AEWP with ethanol as a solvent of choice with a low solvent usage in a reasonable time.
  1,958 163 -
Effects of selected moraceae plants on tyrosinase enzyme and melanin content
Sukanya Dej-adisai, Kedsaraporn Parndaeng, Chatchai Wattanapiromsakul, Wanlapa Nuankaew, Tong Ho Kang
Oct-Dec 2019, 15(65):708-714
Background: Hyperpigmentation is the one cause of skin disorder. The dark-colored skin causes from the increasing of melanin pigment production. It is synthesized by melanogenesis catalyzed by tyrosinase enzyme. Tyrosinase is one of the main causes of melanogenesis; thus, inhibition of the activity of tyrosinase can decrease melanogenesis. Hence, the potential tyrosinase inhibitor could be discovered from natural products. Objective: Discovery of tyrosinase inhibitor from natural products by focusing on Moraceae plants. Materials and Methods: Forty-eight Moraceae plant extracts were screened for antityrosinase and antibacterial activities; Streblus taxoides and Artocarpus chama were selected to study in B16F1 melanoma cell; intracellular antityrosinase activity and melanin content. Moreover, pigmentation inhibitory effect on the zebrafish of these samples was studied. Results: The extracts of S. taxoides and A. chama showed the potential activity against tyrosinase enzyme on both intracellular and extracellular enzymatic assays. Moreover, they suppressed pigmentation in zebrafish. Only ethyl acetate extract of these plants could show anti-bacterial activity. Conclusion: S. taxoides and A. chama are potential plants for further study of chemical constituents and biological activities especially the anti-tyrosinase activity of the isolated compound to find out the lead compound for whitening agent from natural product.
  1,849 183 -
In vitro UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes Activities of Clinacanthus nutans Leaf Juice and Aqueous Extract
Gabriel Akyirem Akowuah, Jin Han Chin, Siew Wei Yeong, Suk Yen Quah, Mariam Ahmad
Oct-Dec 2019, 15(65):532-537
Aim: The objective of the present study was to evaluate the in vitro effect of aqueous extract of Clinacanthus nutans leaves and the juice on the activity of UDP-glucuronosyltransferase (UGT), cytochrome P (CYP) 3A4, and CYP2E1 in human liver microsomes (HLMs). Materials and Methods: The herb-drug interactions of the leaf extracts and juice were determined by a specific enzyme activity of CYP isoforms with specific probe substrate using spectrophotometry. CYP3A4 activity was measured for aminopyrine-specific metabolite (formaldehyde) at 415 nm. CYP2E1 activity was determined using p-nitrophenol-specific metabolite (p-nitrocatechol) at 535 nm. UGT activity was quantified through the consumption of p-nitrophenol by UGT at 405 nm. Results: Results obtained showed that the juice and aqueous extract of C. nutans leaves exhibited significant inhibition (P < 0.05) in CYP3A4 and CYP2E1 activity in HLMs. The aqueous extract of C. nutans showed statistically significant (P < 0.05) activation on UGT activity at the concentration of 1000 ng/mL as compared to the negative control. Conclusion: There is a possibility that herb-drug interaction could occur with C. nutans through inhibitory effects on CYP3A4 and CYP2E1. The leaf preparation also activated UGT catalyzed metabolism which may result in a reduction of the potency of the drug metabolized by UGT pathway.
  1,724 130 -
Cytotoxic activity of Rauvolfia tetraphylla L. on human cervical cancer (HeLa) cells
José Angel Santiago-Cruz, Jesús Arrieta, Jazmín García-Machorro, Daniel Arrieta-Baez, María Elena Sánchez-Mendoza
Oct-Dec 2019, 15(65):631-637
Background: Although the plant Rauvolfia tetraphylla is used for the treatment of cancer in the traditional medicine of some regions of Mexico, its cytotoxic activity has not been subjected to rigorous investigation. Objective: The aim of the present study was to carry out a bioassay-guided fractionation of Rauvolfia tetraphylla leaves to evaluate the activity on cervical cancer (HeLa) and normal cells. Materials and Methods: Of hexane, dichloromethane and methanol extracts, hexane extract showed the most cytotoxic activity. Its most active fraction was characterized by mass spectrometry and assessed for cytotoxicity (by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide assays and trypan blue staining) on cervical cancer (HeLa) cells, normal human (HaCat) cells, and other cancer cell lines: A549, Caco-2, MDA-MB-231, and MCF7. Cisplatin served as the reference drug. Apoptosis was explored as a possible mechanism of action by examining DNA fragmentation and phosphatidylserine translocation. Results: The active fraction, composed of at least 5 constituents, was cytotoxic to all cancer cell lines, especially HeLa cells (IC30= 20.10 ± 1.1 μg/mL). To a lesser extent, it was also cytotoxic to normal cells (HaCat; IC30= 40.04 ± 12.78 μg/mL), indicating certain selectivity. Its mechanism of action in HeLa cells involved apoptosis. Conclusion: The active fraction of the hexane extract of R. tetraphylla was cytotoxic to cancer cells and did not produce excessive damage to normal cells. Apoptosis was apparently part of the mechanism of cytotoxicity.
  1,618 160 -
Antioxidative and Photocytotoxic Effects of Standardized Clinacanthus nutans and Strobilanthes crispus Extracts toward HepG2 Liver Cells
Sheri-Ann Tan, Shi Yun Lim, Chieu Shie Law, Chen Son Yue, Tze Ven Poh, Wan Zuhainis Saad, Saila Ismail, Khatijah Mohamad Yusoff, Chui Fung Loke
Oct-Dec 2019, 15(65):613-620
Introduction: The methanolic extracts of Clinacanthus nutans (CME) and Strobilanthes crispus (SME) are used in Malaysia as a complementary and alternative medicine for cancer. Objective: The present study aimed to determine the antioxidative and photocytotoxic effects of CME and SME toward liver cancer cells. Materials and Methods: Cell-based (2′,7′-dichlorodihydrofluorescein diacetate) and chemical-based (2,2-diphenyl-1-picrylhydrazyl [DPPH]) experiments were utilized to determine the antioxidative properties of both herbal extracts. CME and SME were also tested for their photocytotoxic potentials after photodynamic therapy (PDT). Phytochemical analysis was performed to identify the phytocompounds present in the extracts. Results: Both the extracts demonstrated dose-dependent DPPH radical scavenging activities, while SME was found to be a stronger reactive oxygen species scavenger than CME at all concentrations tested on liver cells. Interestingly, on PDT, HepG2 cells treated with SME and CME at non-toxic doses showed a decrease in cellular viability charting half-maximal inhibitory concentration of 13.45 μg/mL and 81.03 μg/mL, respectively. Total phenolic content of SME (36.27 ± 1.31 mg GAE/g extract) was slightly higher than CME (31.76 ± 0.10 mg GAE/g extract). On the contrary, the total flavonoid content of CME (11.32 ± 0.28 mg QE/g extract) was approximately seven times more than SME (1.69 ± 0.03 mg QE/g extract). Phenolic acids, flavonoids, and pheophorbide-a were identified in both extracts. In view of this, these phytocompounds present in CME and SME could lead to the observed beneficial effects. Conclusion: CME and SME, especially the latter, are strong antioxidants with photosensitizing potentials that should be further investigated.
  1,479 173 -
Study on pharmacokinetics and tissues distribution of neomangiferin, mangiferin, timosaponin BII, Timosaponin BIII, and timosaponin AIII after oral administration of Anemarrhenae rhizoma extract in rats
De Ji, Jin-Chun Qiu, Xiao-Nan Su, Yu-Wen Qin, Min Hao, Lin Li, Tu-Lin Lu, Xiao-Kun Li, Cheng-Xi Jiang
Oct-Dec 2019, 15(65):557-567
Background: Anemarrhenae rhizoma (AR) is widely used for the treatment of febrile diseases, cough, and diabetes in traditional Chinese medicines. AR mainly contains flavonoids and steroidal saponins, such as neomangiferin, mangiferin, timosaponin BII, timosaponin BIII, and timosaponin AIII, which showed various biological activities. Objective: The main objective of the study is to establish an ultra-high-performance liquid chromatography-tandem mass spectrometry (MS/MS) method to determine the concentrations of five bioactive constituents in rats' plasma and various tissues. Materials and Methods: The analytes were separated on a C18reversed-phase column. A triple-quadrupole MS/MS equipped with an electrospray ionization source was used as a detector. The main pharmacokinetic parameters were estimated with Drug and Statistics 2.0 Software Package. Results: Neomangiferin and mangiferin exhibit poor oral absorption and slow clearance from the body. Timosaponin BII and timosaponin BIII could be quickly absorbed into the blood circulation and showed double plasma concentration peaks. Timosaponin AIII exhibited a single peak in the plasma concentration-time plot and pharmacokinetic parameters of timosaponin AIII indicated slower absorption, longer body residence time, and slower elimination than timosaponin BII and timosaponin BIII. The five analytes were widely distributed to most of the tissues. Neomangiferin and mangiferin exhibited the maximum concentration in the lung at 6 h after oral administration, the highest levels of timosaponin BII and timosaponin BIII were also observed in the lung at 1 h after oral administration, and the maximum concentration of timosaponin AIII was observed in the liver. Conclusion: The findings of the present study might be helpful to better understand the pharmacokinetics and distribution of AR bioactive constituents in vivo, which would facilitate the clinical application of AR.
  1,380 198 -
Preventive effect of crude polysaccharide extract from chinese wolfberry against hyperglycemia-induced oxidative stress and inflammation in streptozotocin-induced diabetic rats
Junjie Li, Yong Zhang, Linshan Jiao, Opeyemi Joshua Olatunji, Bing He
Oct-Dec 2019, 15(65):638-644
Background: The protective effects of the crude polysaccharide extract Polysaccharide Lycium chinense (PLC) from the leaves of Lycium chinense (Chinese wolfberry) were evaluated in streptozotocin (STZ)-induced diabetic rats. Materials and Methods: Diabetes was induced in rats by administering STZ (60 mg/kg, i.p), and diabetic rats were orally treated with 100 or 400 mg/kg of PLC extract for 4 weeks. Results: Diabetic rats showed high fasting blood glucose levels, altered serum lipid profile; triglycerides, total cholesterol, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and liver function enzymes; and alanine aminotransferase, aspartate aminotransferase, and alkaline phosphatase. In addition, oxidative stress and pro-inflammatory cytokines were elevated in the kidney and liver tissues of diabetic rats. After treatment with PLC, it was observed that hyperglycemia, hyperlipidemia, and liver and kidney functions were restored to almost normal while enzymatic antioxidant levels of glutathione peroxidase, superoxide dismutase, and catalase were significantly increased, in addition to remarkable reduction in malondialdehyde and pro-inflammatory cytokines. Conclusion: These results demonstrated the protective effect of PLC may be mediated by its antioxidant and anti-inflammatory effects and may be employed as a therapy for preventing diabetes and its complications.
  1,369 161 -
FDY003 inhibits colon cancer in a Colo205 xenograft mouse model by decreasing oxidative stress
In-Hee Lee, Dae-Yeon Lee
Oct-Dec 2019, 15(65):675-681
Background: FDY003 is a traditional Korean medicine that has been developed as a complementary therapy for cancer. FDY003 contains various herbs such as Lonicera japonica, Artemisia capillaris Thunb., and Cordyceps militaris known to exhibit antioxidant and anticancer activities. Objective: The objective of this is to determine whether FDY003 represents a complementary therapy for colon cancer when it is injected using a syringe. Materials and Methods: High-performance liquid chromatography (HPLC) analysis was performed to determine the active ingredients of FDY003. The effect of FDY003 on the proliferation of Colo205 cells was investigated using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) assay. The antioxidant effects of FDY003 on Colo205 cells were ascertained using oxidative markers such as lipid peroxidation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Markers of apoptosis in Colo205 cells after treatment with FDY003 were also measured. Based on the in vitro results, in vivo experiments were performed using Colo205 cell-induced xenograft mouse cancer model treated with FDY003. Results: HPLC analysis revealed that FDY003 contained various active ingredients known to possess antioxidant activities. The viability of Colo205 cells was decreased by FDY003 in a concentration-dependent manner. Cancer size and weight were significantly decreased in the group treated with FDY003, similar to those in the group treated with anticancer drug irinotecan. The expression of Bcl-2-associated X protein and caspase-3 was increased in cancer tissues derived from the FDY003-treated group. Serum levels of lipid peroxidation and DPPH were also significantly increased in the FDY003-treated group. Conclusion: FDY003 represents a potential complementary therapy for cancer due to its antioxidative effects and anticancer activity.
  1,284 106 -
Bioactivity-guided isolation of cytotoxic and antioxidant phytochemicals from four Cousinia species from stenocephala bunge section
Leyla Pasayeva, Osman Üstün, Eren Demirpolat, Gökçe S Karatoprak, Osman Tugay, Müberra Kosar
Oct-Dec 2019, 15(65):682-692
Background: Asteraceae family contains several cytotoxic compounds bearing genus. Cousinia genus is included in the Asteraceae; it has not been studied phytochemically in detail. Objective: In this study, chemical compositions of four Cousinia species (Cousinia davisiana [CD], Cousinia foliosa, Cousinia ramosissima, and Cousinia stenocephala [CS]) were evaluated according to their cytotoxic and antioxidant effects using bioactivity-guided isolation. Materials and Methods: The cytotoxic effect was investigated with Sulphorhodamine B method against Colo205 (human colon carcinoma), A549 (human non-small cell lung cancer) cell lines, and antioxidant activity tested with 1,1-diphenyl-2-picrylhydrazyl, 2,2'-azino-bis 3-ethylbenzothiazoline-6-sulphonic acid scavenging tests, and β-carotene/linoleic acid co-oxidation test. Purified compounds were elucidated by one-dimensional and two-dimensional nuclear magnetic resonance and mass spectroscopic techniques. The quantitative and qualitative determination of unpurified compounds within the extracts was carried out by liquid chromatography-mass spectrometry/mass spectrometry. Results: CS methanol extract, dichloromethane subextract, and FR-3 showed more cytotoxicity; isolated compound (ψ-taraxasterol) showed no cytotoxic activity. CD methanol extract and n-butanol subextract showed significant antioxidant activity. Conclusion: This is the first report that these phytochemical compounds were identified in Cousinia genus, and it is thought that these compounds could contribute to the chemotaxonomy of the genus.
  1,211 132 -
Rosmarinic acid inhibits stem-like breast cancer through hedgehog and Bcl-2/Bax signaling pathways
Hong Li, Yuefeng Zhang, Hsiao-Huei Chen, En Huang, Hailin Zhuang, Dan Li, Feng Ni
Oct-Dec 2019, 15(65):600-606
Background: Rosmarinic acid (RA) is a natural phenolic acid present in various Lamiaceae herbs. RA shows anti-tumor effects on many tumors but has yet to be tested on triple negative breast cancer and its derived breast cancer stem-like cells (BCSCs). Objective: This study aimed to detect whether RA could inhibit the proliferation and migration of BCSCs through hedgehog (Hh) signaling while promoting apoptosis via Bcl-2/Bax. Materials and Methods: BCSCs from the human breast cancer cell line MD-MB-231 were isolated by fluorescence-activated cell sorting with the surface markers of CD44*/CD24-/low. The viability, migration, and apoptosis of BCSCs were assessed by the CCK-8 assay, cell wound healing test, and flow cytometry for positive staining for Annexin V-FITC and propidium iodine (PI), respectively. mRNA and protein levels of Hh and Bcl-2/Bax signaling pathways were obtained by real-time reverse transcriptase polymerase chain reaction and immunoblots. Results: RA inhibited the viability and migration of BCSCs and increased the numbers of late apoptotic cells. Consistent with the increased apoptosis, RA treatment downregulated Bcl-2 while upregulating Bax expression. In line with its effect to limit migration, RA treatment inhibited the expression of Hh-related genes smoothened and glioma-associated oncogene homolog 1. Conclusion: The present study suggests that RA exerts anti-cancer effects on BCSCs by inhibiting Bcl-2 and Hh signaling pathways.
  1,184 136 -
Anti-eczematic and molecular modeling of anthraquinones isolated from the seeds of Asphodelus microcarpus salzm. viv. growing in Egypt
Abd El-Salam I.Mohammed, Arafa Musa, Marwa S Abu-Bakr, Hatem S Abbass
Oct-Dec 2019, 15(65):586-591
Background: Eczema or atopic dermatitis is a widely spread skin disorder; the topical application of corticosteroids is the first choice for treatment. Natural products have a great contribution in the treatment of this disease; Asphodelus microcarpus seeds are rich in anthraquinones and known to possess both anti-inflammatory and antidermatitis effects. Objective: The objective of the study is to investigate the anti-eczematic activity, acute toxicity, and molecular modeling of A. microcarpus seeds. Materials and Methods: Nuclear magnetic resonance, ultraviolet, and mass spectroscopy were applied for characterization of isolated metabolites; induction of eczema was conducted by 2% and 0.2% w/v dinitrochlorobenzene in acetone; eczema was treated with topical application of the different seed extracts in the form of ointments (1% w/w); Swiss albino mice (25–30 g) were used for the determination of LD50and anti-eczematic effect. Docking studies were performed by Molecular Operating Environment software. Results: A. microcarpus seed extract exhibited promising ant-eczematic activity, six anthraquinones were isolated from chloroform portion and characterized as 10,7'-bichrysophanol (1), asphodelin (2), chrysophanol-8-O-methyl ether (3), chrysophanol (4), physcion (5), and emodin (6). Compounds 1, 3, and 5 exerted significant anti-eczematic effect. Conclusion: Six known anthraquinone derivatives were isolated and characterized for the first time from the seeds of A. microcarpus. Chloroform fraction (1% w/w) showed significant anti-eczematic effect compared to standard mometasone furoate (0.1 w/w). The docking study proved the anti-eczematic activity of anthraquinone content by their affinity to the target human histamine H1receptor.
  1,192 111 -
In vitro antitoxoplasmal activity of some medicinal plants
Ibrahim S Al Nasr, Waleed S Koko, Tariq A Khan, Gamal E Elghazali
Oct-Dec 2019, 15(65):568-572
Background: Toxoplasmosis is a serious zoonotic protozoal disease that is distributed worldwide and can infect almost all warm-blooded animals, including humans. In most cases, it is asymptomatic, but in immunocompromised individuals, it is associated with severe neurological and gastrointestinal disorders. A previous serological prevalence investigation in Saudi Arabia indicated that the disease prevalence ranged between 25% and 51% in various areas. Recommended commercial drugs cannot achieve 100% clearance due to side effects. Hence, the development of new safe and affordable drugs is an important goal. Aim: In the present study, extracts from the leaves and fruit of Azadirachta indica A. Juss. collected from different areas, along with two other medicinal plants (Argemone mexicana L. and Xanthium brasilicum Vell.) with established antiprotozoal activity, will be evaluated for antitoxoplasmal activity using an in vitro technique. Materials and Methods: All plants were extracted with 100% methanol and examined for activity against the Toxoplasma gondii RH strain via an intracellularly invaded Vero cell line with calculated inhibition percentages. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide colorimetric assay against the Vero cell line was used for cytotoxic evaluation, followed by selectivity index (SI) calculation. Results: X. brasilicum exhibited the best antitoxoplasmal activity with an IC50of 7.19 μg/ml, followed by the A. indica fruits collected from Qassim, Kingdom of Saudi Arabia, and leaves collected from Central Sudan with an IC50of 17.26 and 18.43 μg/ml, respectively. The best SI was obtained from the leaves of A. indica (6.28) collected from Sudan. Conclusion: Although X. brasilicum proved to have very potent antitoxoplasmal activity, the cytotoxicity was also very high, so the isolation of active compounds is highly recommended.
  1,138 127 -
Effects of Atractylodes macrocephala rhizoma on isoproterenol-induced myocardial hypertrophy in mice
Ke-Zhao Wei, Xiao-Hua Cui, Jia-Hua Feng, Ping-An Yao, Jian-Ping Gao
Oct-Dec 2019, 15(65):579-585
Background: The studies about the protective effect on the heart of single Atractylodes macrocephala rhizoma (AMR) herb and mechanisms have not been reported. Objective: The purpose of this study was to assess the effects of AMR on attenuating myocardial hypertrophy induced by isoproterenol (ISO) in mice. Materials and Methods: Mice were randomly divided into normal control group, ISO control group, ISO plus metoprolol (60 mg/kg) group, ISO plus AMR (2, 4, and 8 g/kg) groups, and AMR (4 g/kg) control group. The mice with myocardial hypertrophy were established by subcutaneous (s.c.) injection with ISO (2 mg/kg/d) and administered intragastrically with the corresponding drugs in the volume of 0.2 mL/10 g/d for 7 days. In the normal and AMR control groups, mice were injected (s.c.) with physiological saline (the solvent for ISO) and administered intragastrically with drinking water for 7 days. Results: Compared with the ISO-induced group, AMR significantly decreased heart weight index, left ventricular weight index, and average transverse area of cardiomyocytes, significantly increased the activity of total superoxide dismutase in serum and the level of the angiotensin II receptor type (AT) gene expression in myocardium and significantly decreased the contents of malondialdehyde, cyclic adenosine monophosphate , and aldosterone in serum and angiotensin II (Ang II) in myocardium. Conclusion: The ability of AMR to mitigate myocardial hypertrophy is partly associated with its anti-oxidative effect, restraining excessive secretion or activation of neuroendocrine factors, and the stronger upward effect on AT2gene expression than AT1.
  1,098 99 -
Chemical composition from the leaves of Lindera fragrans Oliv.
He-Zhong Jiang, Tian Gan, Ya-Nan Li, Chun-Yan Du, Jun-Long Li, Jun-Ting Fan, Rui Tan
Oct-Dec 2019, 15(65):736-739
Background: One hundred known species belong to the genus Lindera (Lauraceae) and rich in chemical structure types. The branch leaves of Lindera fragrans Oliv. show the special curative effect of treating gastroenteritis and gastric ulcer. There are not comparatively detailed reports carried on studying the chemical composition and bioactivity of L.fragrans. Objective: This paper reports the chemical investigation and biological evaluation of the L.fragrans. Materials and Methods: The petroleum ether and ethyl acetate soluble part of L.fragrans was isolated using chromatographic methods, and the structures of these compounds were identified by comparison of their spectroscopic data with those reported in the literature. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide method was used to determine the antitumor activity of the isolated compounds. Results: Twelve compounds were isolated from the leaves of L.fragrans and classified as six alkaloids (1–6), three flavonoids (7–9), two aromatics (10 and 11), and one anthraquinone (12). The study of antitumor activity showed that compounds 3–5 had weak antitumor activities with the half maximal inhibitory values ranging from 71.97 to 94.69 μM. Conclusion: All of these compounds were isolated from this plant for the first time and compounds 3–6, 8, and 9 were first reported from the genus Lindera. Compounds 3–5 exhibited weak antitumor activities. The chemical investigation of the leaves of Lindera fragrans resulted in the isolation of 12 compounds including six alkaloids (1–6), three flavonoids (7–9), two aromatics (10 and 11), one anthraquinone (12). The isolated compounds 3–9 were evaluated for their cytotoxicity against melanoma, glioma, and hepatoma cells by MTT method.
  1,089 103 -
Alisma orientalis (Sam.) juzep polysaccharide-regulated glucose-lipid metabolism in experimental rats and cell model of diabetes mellitus with regulation of miR-126
Zeng-Kun Qian, Fan Cui, Yun-Xi Ling, Wen-Juan Zhu, Xiao-Qin Li, Zheng Mao, Min-Ting Li
Oct-Dec 2019, 15(65):652-658
Background: Alismatis rhizome (AR) is a popular traditional Chinese medicine, used for hyperlipidemia and diabetes in China for centuries; Alisma polysaccharides (AP) are the bioactive components in AR. This study investigates if glucose–lipid metabolism can be regulated by AP via miR-126 in vivo and in vitro. Materials and Methods: The diabetes group (diabetes mellitus) was injected intraperitoneally with streptozotocin (35 mg/kg) for 7 days. Diabetic mice treated with AP at an oral dose of either 400 mg/kg (high), 200 mg/kg (middle), or 100 mg/kg (low); and mice treated with pioglitazone (15 mg/kg) each day. The hypoglycemic and hypolipidemic effects of AP were demonstrated by measuring fasting blood glucose (FBG) levels, fasting insulin level, total cholesterol, triglyceride, low-density lipoprotein and high-density lipoprotein, observing insulin-sensitizing effects, and testing oral glucose tolerance. In addition, the expression of both miR-126 and related glucose–lipid genes in the primary hepatocytes was examined in diabetic mice. Results: The FBG, long-term blood glucose, and the ability to resolve blood glucose by insulin in AP groups were significantly better than that in model group. AP could reverse the expression level of miR-126 and genes. The addition of AP could reduce the effect of miR-126, reversing the expression of glucose–lipid genes in HepG2 cell. Conclusion: The results demonstrate that the expression of miR-126 can be directly decreased by AP in diabetic mice, especially in HepG2 cell, and AP also can ameliorate the glucose–lipid metabolism.
  1,054 122 -
Metabolic profiling of Solanum villosum Mill subsp. miniatum (bernh. ex willd.): Hepatoprotective and antifibrotic activity in a rat model of liver fibrosis
Alaa El-Din E. Abdel-Hamid, Riham Salah El Dine, Jandirk Sendker, Soheir M El Zalabani, Meselhy R Meselhy, Elena Jimenez-Negro, Ashraf B Abdel-Naim
Oct-Dec 2019, 15(65):659-670
Aim/Background: To assess the liver antifibrotic action of ethanolic extract of aerial parts of Solanum villosum Mill subsp. miniatum (Bernh. ex Willd.) (SVE) and correlate this activity with its high performance liquid chromatography-quadrupole time of flight (HPLC-qTOF) Electrospray Ionisation Mass Spectrometry (ESIMS) phytochemical profile. Materials and Methods: The median lethal dose of SVE was determined, and a rat model of carbon tetrachloride (CCl4)-induced liver fibrosis was used to evaluate its antifibrotic activity. Markers for hepatotoxicity, fibrosis, and oxidative stress were assessed, and histopathological features of liver tissues were examined. Metabolite profiling of SVE was achieved via HPLC-qTOF-ESIMS coupled with Photodiode array (PDA). Liver fibrosis was induced in rats by oral administration of CCl4for 6 weeks. Silymarin (positive control) and SVE (100 and 250 mg/kg) were orally administered daily for 6 weeks. Results: Compared to CCl4-intoxicated group, administration of SVE obviously ameliorated fibrosis of the hepatic capsule associated with aggregation of multiple focal fat cells formation. Both silymarin and SVE ameliorated the rise in serum markers of hepatotoxicity (alanine transaminase, aspartate transaminase, and alkaline phosphatase), markedly attenuated CCl4-induced oxidative stress. The antifibrotic activity of SVE was evidenced by inhibiting the rise in hepatic hydroxyproline content and accumulation of collagen. This was confirmed by the ability of SVE to inhibit alterations in expression of the fibrosis-related genes Collagen Iα, matrixmetalloproteinase-2 (MMP-2), tissue inhibitor matrix metalloproteinase-2, and transforming growth factor beta 1. HPLC-qTOF-ESIMS analysis of SVE revealed the presence of 47 metabolites, among which 33 were tentatively identified. Conclusion: SVE exhibited hepatoprotective and antifibrotic activities in rats by enhancing the antioxidant capacity and regulating expression of fibrogenic mediators.
  1,043 129 -
Antitumor effects and mechanism of protein from Panax ginseng C. A. Meyer on human breast cancer cell line MCF-7
Xilin Wan, Xin Jin, Yuhe Ren, Yang Xiu, Yu Li, Changbao Chen, Shuying Liu
Oct-Dec 2019, 15(65):715-721
Context: Panax ginseng is well known for its various bioactivities, but specific knowledge on ginseng proteins (GPs) is limited. Aims: Protein components were extracted from ginseng and antitumor activity in human breast cancer cell line MCF-7 was investigated. Settings and Design: Five methods were applied to extract GP and the antitumor effects and mechanism of GP on MCF-7 were explored, including proliferation, cell cycle, apoptosis, and migration. Subjects and Methods: Five extraction methods were employed. MCF-7 cell proliferation was measured using a cell counting kit-8 with different GP concentrations (0, 0.25, 0.5, 1, 2, and 4 mg/mL) and half inhibitory concentration values were calculated. Cell cycle, morphology, and apoptosis were investigated using immunofluorescence staining and flow cytometry. Migration was probed by scratch wound healing and transwell assays. Quantitative-polymerase chain reaction and western blotting were performed to analyze apoptosis-associated gene/protein expression. Statistical Analysis: Experimental data were analyzed by Microsoft Excel and SPSS software. Results: Acetone extraction achieved the highest GP purity and yield. GP inhibited proliferation of MCF-7 in a time-dependent manner and induced cell cycle arrest at G1/S and apoptosis. Scratch wound healing and transwell assays showed that cell migration was also inhibited by GP and expression levels of Bcl-2 and Bax were affected. Conclusion: GP elicits antitumor activity by inhibiting cell proliferation and migration and inducing cell cycle arrest and apoptosis in MCF-7 cells and may act via the Bcl-2 and Bax apoptotic pathway.
  1,052 119 -
Systematic estimation of potential risk caused by the replacement of aconite's cultivar
Yan Shen, Sun Xu, Wang Mengyan, Tang Yongbin, Chi Xu, Honeycutt Hailey, Tong Kai, Mou Lan, Chen Ji, Zhong Weiping, Liu Chen, Mengliang Tian
Oct-Dec 2019, 15(65):722-729
Background: Aconite is a famous toxic medicinal plant in the world. But in China, the aconite cultivar, Qingchuan cultivar, which has been stably used for 2000 years, are being rapidly replaced by the Liangshan cultivar, a new cultivar with better agronomic traits. However, the risk of the replacement is still unknown. Materials and Methods: We combine field research and cultivation experiments to clarify differences in provenance and differences in agronomic traits. We used high-performance liquid chromatography (HPLC) to analyze the content of key ingredients in commercially available medicines and semi-finished drugs. We then performed a transcriptome analysis of the two resources to study the key differential pathways of the two species and conducted a systematic discussion. Statistical Analysis Used: Statistical differences were assessed by analysis of variance or least significant difference. P < 0.05 was considered statistically significant. Results: The survey and cultivation experiments showed that the overwhelming superiority of agronomic traits had already made Liangshan cultivar occupy the vast majority of areas. HPLC showed that the content of diester alkaloids in the Liangshan cultivar was slightly higher and that of higenamine was significantly lower. Analysis of the patented drug and fuzi flake demonstrated a strong correlation between higenamine and cardiac activity. Transcriptome analysis revealed that the upregulation of multiple genes in the isoquinoline pathway in Qingchuan cultivar resulted in the large difference of higenamine.
  999 157 -
Influence of Flavonoids from Galium verum L. on the activities of cytochrome P450 isozymes and pharmacokinetic and pharmacodynamic of warfarin in rats
Mingyu Cui, Conghui Li, Xiaoyue Kong, Kai Zhang, Yuanyuan Liu, Qimeng Hu, Yingli Ma, Yanfeng Li, Tingting Chen
Oct-Dec 2019, 15(65):645-651
Background: Galium verum L., a traditional Chinese medicine, has been widely used in the folk in China. Preparations of G. verum L. were used to treat thromboembolic disease in clinic for many years and often combined with anticoagulants. Flavonoids from G. verum L. (FGVL) are the main active component. Materials and Methods: We assessed the potential influence of FGVL on the activities of five cytochrome P450 (CYP) enzymes and on the pharmacokinetic of warfarin in rats. The pharmacokinetics of five probe drugs and of warfarin was compared between control and FGVL-pretreated groups, which could estimate the effect on the activities of the five isozymes and warfarin metabolism. Moreover, the potential influence of FGVL on the pharmacodynamic of warfarin was investigated. Results: There was no significant difference in the pharmacokinetic parameters of chlorzoxazone and midazolam between control and FGVL-pretreated groups. However, the pharmacokinetic parameters of caffeine in every dose, metoprolol in middle dose, and tolbutamide in high dose were affected significantly (P < 0.05). It indicated that the metabolism of caffeine was markedly faster in FGVL-pretreated group but metoprolol in the middle dose and tolbutamide in the high-dose FGVL-pretreated group were markedly slower. The anticoagulation of combination group is better than warfarin group or FGVL group. This suggested that FGVL showed no effect on the enzyme activities of CYP2E1 and CYP3A2, induced the enzyme activities of CYP1A2, but inhibited the enzyme activities of CYP2D4 in the middle dose and CYP2C11 in high dose. Conclusion: This indicates that FGVL may increase the anticoagulation of warfarin in clinic dose. The dose of warfarin should be adjusted when combined with FGVL or preparations of G. verum L.
  1,033 115 -
Estrogenic activity of glycosides from Cistanche deserticola as an estrogen receptors adjuvant in vitro
Hui Song, Wen-Lan Li, Xiang-Ming Sun, Yang Hu, Jing-Xin Ding, Yu-Bin Ji, Jing-Ya Wang
Oct-Dec 2019, 15(65):693-697
Background: Cistanche deserticola, a traditional Chinese herb medicine, has been widely used for thousands of years with the activities of hormone regulation, immunomodulatory, antioxidative, neuroprotective, anti-inflammatory, and estrogen. Glycosides of Cistanches (GCs) were the main bioactivity components of the herb. Objective: The objective of the study is to study estrogenic activity and the mechanism about estrogen receptors (ERs) of GCs. Materials and Methods: Cell proliferation was measured using the 3-[4,5-dimethyl-2-thiazolyl]-2,5-diphenyltetrazolium bromide assay for MCF-7 cells. The cell cycle was detected using flow cytometry, and proliferation index was calculated. The mRNA and protein expressions of ERα and ERβ were detected by reverse transcription-polymerase chain reaction (RT-PCR) and western blot analysis as the reported method with minor modifications. Results: GCs group at the concentrations of 1.75, 17.5, and 175 μg/mg could enhance proliferation of the MCF-7 cell lines with a time and dosage-dependent manner. Combined medication group (fulvestrant with estradiol [E2] or GCs) could lead to the incline of proliferation rate compared with the individual medication group (P < 0.01). Flow cytometry analysis indicated that GCs could advance MCF-7 cell lines from G0/G1 phase cells to S and G2/M phase, which could promote cell DNA synthesis. The mechanism of GCs on MCF-7 was similar to that of E2. RT-PCR and western blot analysis indicated that after treatment with GCs for 48 h, contents of ERα and ERβ mRNA and proteins in MCF-7 increased as a dosage-dependent manner with that of GCs. GCs can play a role of estrogenic activity according upregulated mRNA and proteins of ERα and ERβ. Conclusion: This study indicated the estrogenic activity of GCs, and also, ER is the target of GCs. GCs can play a role of estrogenic activity according upregulated mRNA and proteins of ERα and ERβ.
  1,028 112 -
Juglone Induces Michigan Cancer Foundation-7 Human Breast Cancer Cells Apoptosis through Bcl-2-Associated X protein/B-cell lymphoma/leukemia-2 Signal Way
Qing Luo, Kang Hu, Fang Chen, Feng-Jiao Gan, Yuan-Xiu Leng, Xu-Mei Chen, Su-Hong Sun
Oct-Dec 2019, 15(65):573-578
Background: Juglone is a natural pigment, which has a cytotoxic effect against tumor cells. However, its cytotoxicity to human breast cancer cells (Michigan Cancer Foundation-7 [MCF7]) has not been demonstrated. Objective: The objective was to observe the effect of Juglone on the protein expression of caspase-3, 9 in the apoptosis of Human Breast Cancer Cells (MCF7) and apoptosis-related protein, Bcl-2-associated X protein (Bax), and B-cell lymphoma-2 (Bcl-2) and investigate in the inhibitory effect of MCF7. Materials and Methods: Methyl thiazolyl tetrazolium experiment was performed for the detection of the cell growth inhibition effect of MCF7. The apoptosis rate was detected by flow cytometry. Western Blot was used to detect the protein expression of Bax, Bcl-2, and caspase. The messenger RNA (mRNA) was tested using quantitative real-time polymerase chain reaction. Results: Juglone inhibited the growth of MCF7 cells in a concentration- and time-dependent manner and promotes the apoptosis of MCF7 cells in a concentration-dependent manner. Compared with control group, the Juglone group raised the expression of Bax protein (*P < 0.05), and the protein expression of Bcl-2 was decreased (*P < 0.05). The expression of caspase-3 protein was not changed, and the caspase-9 was significantly elevated in the high concentration of Juglone. Cleaved caspase-3, -9 protein was significantly raised (*P < 0.05). The mRNA levels of Bax, caspase-3, and caspase-9 in MCF7 cells of Juglone group were significantly increased compared with control, while the expression of Bcl-2 was suppressed obviously. Conclusion: Juglone inhibited the growth of MCF7 cells and promotes the apoptosis of MCF7 cells. Its mechanism in promoting MCF7 cell apoptosis may be related to the decrease of the expression of the mitochondrial pathway-associated apoptosis factor Bcl-2, increase of the protein expression of Bax, and mitochondrial pathway downstream caspase-3, 9.
  1,047 92 -
Undulaterpene A: A new triterpene fatty acid ester from pulicaria undulata
Hossam Mohamed Abdallah, Gamal A Mohamed, Sabrin R M. Ibrahim, Hani Z Asfour, Maan T Khayat
Oct-Dec 2019, 15(65):671-674
Background: Natural products display a remarkable role not only in the synthesis, design, and discovery of new drugs but also as the most prominent source of innovative drugs and bioactive substances. Genus Pulicaria (Asteraceae) includes about 100 species that are widely distributed in Europe, Asia, and Africa. Objective: In this work, the chemical investigation of Pulicaria undulata aerial parts was performed. In addition, the cytotoxic activity of the isolated metabolites was estimated toward various cell lines. Materials and Methods: Plant extract was subjected to fractionation and different column chromatography to isolate the biometabolites. Their structures were verified using nuclear magnetic resonance, infrared, ultraviolet, and high-resolution mass spectrometry, as well as compared with the literature. The cytotoxic effect was evaluated in vitro toward various cell lines: HCT-116 (colorectal adenocarcinoma), MCF-7 (human breast adenocarcinoma), and A549 (lung carcinoma). Results: A new triterpene fatty acid ester, undulaterpene A (1) (3β,16β-dihydroxylup-20 (29)-ene 3-decanoate) and four known metabolites: 3-O-acetyl-pseudotaraxasterol (2), pseudotaraxasterol (3), stigmasterol (4), and tomentosin (5) were separated. Compound 1 displayed cytotoxic potential toward hormone-dependent breast carcinoma cell line (MCF7), colon carcinoma cell line (HCT116), and lung carcinoma cell line (A549) cell lines with half maximal inhibitory concentrations (IC50s) 8.2, 6.9, and 12.4 μM, respectively in comparison to doxorubicin (IC50s 0.14, 0.39, and 1.15 μM, respectively). However, 2, 3, and 4 displayed activity toward HCT-116 with IC50s 13.2, 23.1, and 16.4 μM, respectively. Conclusion: This work led to the identification of a new triterpene fatty acid ester (1) and four known metabolites (2–5) from P. undulata growing in Saudi Arabia. The new compound showed moderate cytotoxic potential against hormone-dependent breast carcinoma cell line (MCF7), colon carcinoma cell line (HCT116), and lung carcinoma cell line (A549) cancer cell lines.
  1,005 126 -
Structural characterization and immune regulation of a new heteropolysaccharide from Catathelasma imperiale(Fr.) sing
Lu Liu, Xiang Ding, Yiling Hou
Oct-Dec 2019, 15(65):621-630
Background: Polysaccharide has played the part of great role in pharmacology and physiology. Materials and Methods: In this study, the polysaccharides (CIS-A) from Catathelasma imperiale (Fr.) Sing, were isolated and purified by hot water extraction technology and column chromatography, respectively. Chemical methods, infrared spectrum, high-performance gel-permeation chromatography, high-performance liquid chromatography, gas chromatography–mass spectrometry,1H nuclear magnetic resonance spectroscopy (NMR),13C NMR, and two-dimensional NMR were used to characterize the polysaccharides of CIS-A. The anticancer and immunomodulatory ability of the polysaccharides (CIS-A) from the fruiting body of C. imperiale (Fr.) Sing was also investigated. Results: The structural feature analysis showed the polysaccharide (CIS-A) which had a molecular weight of 50486 Da was mainly composed of α-D-glucose pyranose (α-D-Glcp) and β-L-fucose pyranose (β-L-Fucp). It had a backbone of three 1, 3-linked α-D-Glcp. There is a branch at the C2 of the polysaccharide backbone. The branches were mainly composed of two 2, 3-linked β-L-Fucp residue. Antitumor activity results showed that CIS-A could inhibit the growth of S180 tumor and promote the apoptosis of L929 cells. Immunoregulatory activity results showed that CIS-A could promote the proliferation of T-cells and promote B-cells by affecting G0/G1 phase, S phase, and G2/M phase. It also could promote the proliferation and phagocytosis of macrophages and induce cytokine release. Conclusion: Polysaccharide CIS-A can be used as a candidate drug for antitumor and immunomodulator.
  930 120 -
Development of a species-specific polymerase chain reaction-based technology for authentication of asini corii colla and taurus corii colla
Liqun Chen, Zhaoqun Jiao, Yufei Chen, Pingtian Yu, Yang Zheng, Yaya Yang, Yuping Shen, Huan Yang
Oct-Dec 2019, 15(65):607-612
Background: Asini Corii Colla (ACC; donkey-hide glue) and Taurus Corii Colla (TCC; bovine-hide glue) are popular healthcare food supplements as well as well-recognized medicine in Traditional Chinese medicine clinics. Due to large demand of them and limited resources of their animal origins, the skin of other animals are often used to make their fake or adulterated products. Objective: In this study, we aimed to develop a species-specific polymerase chain reaction (PCR) approach to detect deoxyribonucleic acid (DNA) fragments of ACC and TCC for rapid authentication purpose. Materials and Methods: Four sets of novel species-specific primer were designed, and PCR conditions were optimized for the PCR assay, which was further validated for specificity and sensitivity. Then, deliberate mixture was analyzed to further verify the capability of adulteration detection by the developed PCR method. Finally, it was used to assess the authenticity of commercial products. Results: Four primers' sets were specific for amplification of extracted mitochondrial DNA of donkey, bovine, swine, and horse when the annealing temperature was 59°C, 59°C, 63°C, and 65°C, and 40 thermal cycles was performed. Under this optimized PCR conditions, 1 ng/μL of horse DNA template has been detected in the sensitivity test, with 0.1 ng/μL for donkey, bovine, and swine. The assay was capable of detecting spiked species at 10% level in premixed ACC or TCC samples. Conclusion: The newly developed PCR-based technology was specific and sensitive, and it was a convenient approach for the authentication of commercial ACC and TCC products.
  905 113 -