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   2016| Oct-Dec  | Volume 12 | Issue 48  
    Online since October 13, 2016

 
 
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ORIGINAL ARTICLES
Alpha-glucosidase inhibitory and antioxidant potential of antidiabetic herb Alternanthera sessilis : Comparative analyses of leaf and callus solvent fractions
Tsun-Thai Chai, Chee-Siong Khoo, Chong-Siang Tee, Fai-Chu Wong
Oct-Dec 2016, 12(48):253-258
DOI:10.4103/0973-1296.192202  PMID:27867265
Background: Alternanthera sessilis is a medicinal herb which is consumed as vegetable and used as traditional remedies of various ailments in Asia and Africa. Objective: This study aimed to investigate the antiglucosidase and antioxidant activity of solvent fractions of A. sessilis leaf and callus. Materials and Methods: Leaf and callus methanol extracts were fractionated to produce hexane, chloroform, ethyl acetate, butanol, and water fractions. Antiglucosidase and 1,1-diphenyl-2-picrylhydrazyl scavenging activities as well as total phenolic (TP), total flavonoid (TF), and total coumarin (TC) contents were evaluated. Lineweaver–Burk plot analysis was performed on leaf and callus fractions with the strongest antiglucosidase activity. Results: Leaf ethyl acetate fraction (LEF) had the strongest antiglucosidase (EC50 0.55 mg/mL) and radical scavenging (EC50 10.81 μg/mL) activity among leaf fractions. Callus ethyl acetate fraction (CEF) and chloroform fraction had the highest antiglucosidase (EC50 0.25 mg/mL) and radical scavenging (EC50 34.12 μg/mL) activity, respectively, among callus fractions. LEF and CEF were identified as noncompetitive and competitive α-glucosidase inhibitors, respectively. LEF and CEF had greater antiglucosidase activity than acarbose. Leaf fractions had higher phytochemical contents than callus fractions. LEF had the highest TP, TF, and TC contents. Antiglucosidase and antioxidant activities of leaf fractions correlated with phytochemical contents. Conclusion: LEF had potent antiglucosidase activity and concurrent antioxidant activity. CEF had the highest antiglucosidase activity among all fractions. Callus culture is a promising tool for enhancing production of potent α-glucosidase inhibitors. Abbreviations used: LHF: Leaf hexane fraction, LCF: Leaf chloroform fraction, LEF: Leaf ethyl acetate fraction, LBF: Leaf butanol fraction, LWF: Leaf water fraction, CHF: Callus hexane fraction, CCF: Callus chloroform fraction, CEF: Callus ethyl acetate fraction, CBF: Callus butanol fraction, CWF: Callus water fraction, TP: Total phenolic, TF: Total flavonoid, TC: Total coumarin.
  2,288 150 -
Effect of methanolic leaf extract of Talinum triangulare (Jacq). willd. on biochemical parameters in diet induced dyslipidemia wistar rats
Olubukola Sinbad Olorunnisola, Adewale Adetutu, Anthony Jide Afolayan, Abiodun Olusoji Owoade
Oct-Dec 2016, 12(48):333-339
DOI:10.4103/0973-1296.192194  PMID:27867278
Objective: To investigate the effect of methanolic leaf extract of Talinum triangulare on hematological parameters, enzymatic and non-enzymatic antioxidant status,and serum lipid in Wistar rats fed standard laboratory, or 2% cholesterol-enrich diet. Material and Methods: Wistar rats (180-210g) divided into six groups of six animals (males) each were fed 2% cholesterol-enriched diet and orally treated with 0.9% saline or extract of Talinum triangulare (250, 500, and 1000 mg/kg per body weight) daily for eight weeks. Lipid profile, lipid peroxidation (MDA), hematological parameters, and their functional indices and serum antioxidant enzymes (catalase, glutathione -S-transferase, and superoxide dismutase) activities and glutathione status were assessed in normal and diet-induced hypercholesterolemic extract treated rats and compared with the rats treated with 100 mg/kg per bwt standard drug gemfibrozil. Results: A significant (P < 0.05) increase in lipid profile (total glyceride, total cholestrol, low-density lipoprotein, and very low-density lipoprotein), MDA and reduction (P < 0.05) in enzymatic and nonenzymatic antioxidant status coupled with alterations in hematological parameters was observed in the serum of hypercholesterolemic rats when compared with animals on a normal diet. Coadministration of methanolic leaf extracts of Talinum triangulare or gemfibrozil significantly (P < 0.05) restored the elevated serum lipid profile, MDA, and the deranged hematological parameters to near normal. The extract also protected against hypercholesterolemic-induced diminished enzymatic and nonenzymatic antioxidant status. The activities of the plant extract are dose (250, 500, and 1000 mg/kg) dependent and it compared favorably with the standard drug gemfibrozil. Conclusion: The present study suggested that the extract of Talinum triangulare might protect against hypercholesterolemic-induced altered lipid profiles, oxidative stress, and also improve the status of antioxidant defense system and hematopoiesis. Abbreviation used: Lipid peroxidation (MDA), (catalase (CAT), glutathione–S-transferase (GST), superoxide dismutase (SOD), glutathione (GSH), Thrombocytes indices (PLT), Red blood cell (RBC), Packed cell volume (PVC), Mean corpuscular hemoglobin(MCH), Mean corpuscular hemoglobin concentration (MCHC), Total glyceride (TG), Very low density lipoprotein (VLDL), Total cholesterol (TC), Low density lipoprotein (LDL), High density lipoprotein (HDL) and 3-Hydroxy-3-methyl-glutaryl-CoA reductase(HMG-CoA).
  2,386 26 -
Traditional herbal formulas to as treatments for musculoskeletal disorders: Their inhibitory effects on the activities of human microsomal cytochrome p450s and udp-glucuronosyltransferases
Seong Eun Jin, Chang-Seob Seo, Hyeun-Kyoo Shin, Hyekyung Ha
Oct-Dec 2016, 12(48):241-252
DOI:10.4103/0973-1296.192205  PMID:27867264
Objective: The aim of this study was to assess the influence of traditional herbal formulas, including Bangpungtongseong-san (BPTSS; Fangfengtongsheng-san, Bofu-tsusho-san ), Ojeok-san (OJS; Wuji-san, Goshaku-san ), and Oyaksungi-san (OYSGS; Wuyaoshungi-san, Uyakujyunki-san ), on the activities of the human cytochrome P450s (CYP450s) and UDP-glucuronosyltransferases (UGTs), which are drug-metabolizing enzymes. Materials and Methods: The activities of the major human CYP450 isozymes (CYP1A2, CYP3A4, CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP2E1) and UGTs (UGT1A1, UGT1A4, and UGT2B7) were investigated using in vitro fluorescence-based and luminescence-based enzyme assays, respectively. The inhibitory effects of the herbal formulas were characterized, and their IC50values were determined. Results: BPTSS inhibited the activities of CYP1A2, CYP2C19, CYP2E1, and UGT1A1 while it exerted relatively weak inhibition on CYP2B6, CYP2C9, CYP2D6, and CYP3A4. BPTSS also negligibly inhibited the activities of UGT1A4 and UGT2B7, with IC50values in the excess of 1000 μg/mL. OJS and OYSGS inhibited the activity of CYP2D6, whereas they exhibited no inhibition of the UGT1A4 activity at doses <1000 μg/mL. In addition, OJS inhibited the CYP1A2 activity but exerted a relatively weak inhibition on the activities of CYP2C9, CYP2C19, CYP2E1, and CYP3A4. Conversely, OJS negligibly inhibited the activities of CYP2B6, UGT1A1, and UGT2B7 with IC50values in excess of 1000 μg/mL. OYSGS weakly inhibited the activities of CYP1A2, CYP2C19, CYP2E1, CYP3A4, and UGT1A1, with a negligible inhibition on the activities of CYP2B6, CYP2C9, and UGT2B7, with IC50values in excess of 1000 μg/mL. Conclusions: These results provide information regarding the safety and effectiveness of BPTSS, OJS, and OYSGS when combined with conventional drugs. Abbreviation used: BPTSS: Bangpungtongseong-san, OJS: Ojeok-san, OYSGS: Oyaksungi-san, CYP450s: cytochrome P450s, UGTs: UDP-glucuronosyltransferases, MSDs: Musculoskeletal disorders, NSAIDs: nonsteroidal anti-inflammatory drugs, EOMCC: 7-ethoxy-methyloxy-3-cyanocoumarin, DBOMF: di(benzyloxymethoxy)fluorescein, BOMCC: 7-benzyloxy-4-trifluoromethylcoumarin, HPLC: High-performance liquid chromatography, PDA: photo diode array, SEM: standard error of the mean, UDPGA: uridine 5'-diphosphoglucuronic acid.
  2,239 140 -
A new antifungal isocoumarin from the endophytic fungus Trichoderma Sp. 09 of Myoporum bontioides A. gray
Wensheng Li, Jiaxin Xu, Fenqi Li, Li Xu, Chunyuan Li
Oct-Dec 2016, 12(48):259-261
DOI:10.4103/0973-1296.192204  PMID:27867266
Background: Myoporum bontioides A. Gray is a commonly used medicinal plant in China. Recently, the chemical and bioactive investigations to the endophytic fungi of this plant have led to several new compounds with antimicrobial and cytotoxic activities. To find out more active molecules, the metabolites of an endophytic fungus, Trichoderma sp. 09 from the root of Myoporum bontioides were investigated. Materials and Methods: The metabolites were isolated by column chromatography on silica gel, and their structures were elucidated on the basis of spectroscopic analysis[one-dimensional (1D), two-dimensional (2D)-nuclear magnetic resonance (NMR), Mass spectrometry (MS)], and by comparison with the published data. The dilution method was used for the evaluation of antifungal activity. Results: Four metabolites were isolated and identified as: dichlorodiaportinolide (1), dichlorodiaportin (2), diaportinol (3), and diaportin (4). Compounds1 and 2 showed weak to high antifungal activities against Colletotrichum musae (Berk. and M. A. Curtis) Arx and Rhizoctonia solani Kühn, as compared with the positive control. Conclusions: Compound 1 was a new isocoumarin being worthy of consideration for the development and research of antifungal agents. Abbreviations used: IR: Infrared Radiation, HR-ESI-MS: High resolution electrospray ionization mass spectroscopy, LCMS-IT-TOF: Liquid chromatography mass spectroscopy-Ion trap-Time-of-flight, UV: Ultraviolet-visible, HMBC: Heteronuclear multiple bond correlation, NOE: Nuclear Overhauser effect.
  1,948 60 -
Platyphylloside isolated from Betula platyphylla inhibit adipocyte differentiation and induce lipolysis via regulating adipokines including PPARγ in 3t3-l1 cells
Mina Lee, Sang Hyun Sung
Oct-Dec 2016, 12(48):276-281
DOI:10.4103/0973-1296.192208  PMID:27867269
Background: Obesity causes or aggravates many health problems, both independently and in association with several pathological disorders, including Type II diabetes, hypertension, atherosclerosis, and cancer. Therefore, we screened small compounds isolated from natural products for the development of anti-obesity drugs. Objective: The purpose of this study was to investigate the anti-adipogenic activities of platyphylloside, diarylheptanoid isolated from Betula platyphylla , which was selected based on the screening using 3T3-L1 cells. Materials and Methods: To evaluate the inhibition of adipocyte differentiation and lipolysis, lipid contents of BPP on were measured using Oil Red O staining in 3T3-L1 cells. The mRNA and protein expression levels of various adipokines were measured by Quantitative real-time PCR and Western blotting analysis, respectively. Results: Platyphylloside showed significant inhibitory activity on adipocyte differentiation in 3T3-L1 cells and suppressed adipocyte differentiation even in the presence of troglitazone, a PPARγ agonist. Platyphylloside might suppress adipocyte differentiation through PPARγ, C/EBPα, and SREBP1-induced adipogenesis, which is synergistically associated with downstream adipocyte-specific gene promoters such as aP2, FAS, SCD-1, LPL, and Adiponectin. In addition, platyphylloside affected lipolysis by down-regulating perilipin and HSL and up-regulating TNFα. Conclusion: Taken together, the results reveal that platyphylloside has anti-adipogenic activity and highlight its potential in the prevention and treatment of obesity. Abbreviations used: DMEM: Dulbecco's modified Eagle's medium, FBS: fetal bovine serum, ORO: Oil Red O, PBS: phosphate buffered saline, RT: room temperature, PPAR: peroxisome proliferator-activated receptor, C/EBP: CCAAT/enhancer-binding protein, SREBP1: sterol regulatory element binding protein 1, SCD-1: steroyl-coenzyme A desaturase 1, LPL: lipoprotein lipase, aP2: adipocyte fatty acid binding protein, FAS: fatty acid synthase, HSL: hormone sensitive lipase, Giα1: GPT binding protein, PDE3B: phosphodiesterase 3B, TNFα: tumor necrosis factor α, GAPDH: glyceraldehyde 3-phosphate dehydrogenase, SD: standard deviation, EGCG: epigallocatechin-3-gallate, TZD: thiazolidinediones
  1,877 46 -
Essential oil composition, antimicrobial and pharmacological activities of Lippia sidoides cham. (verbenaceae) from São Gonçalo do Abaeté, Minas Gerais, Brazil
Sandra Ribeiro de Morais, Thiago Levi Silva Oliveira, Lanussy Porfiro de Oliveira, Leonice Manrique Faustino Tresvenzol, Edemilson Cardoso da Conceição, Maria Helena Rezende, Tatiana de Sousa Fiuza, Elson Alves Costa, Pedro Henrique Ferri, José Realino de Paula
Oct-Dec 2016, 12(48):262-270
DOI:10.4103/0973-1296.192197  PMID:27867267
Background: Lippia sidoides (Verbenaceae) is used in Brazilian folk medicine as an antiseptic, and it is usually applied topically on skin, mucous membranes, mouth, and throat, or used for vaginal washings. Objectives: To analyze the chemical composition of the essential oil from L. sidoides collected in São Gonçalo do Abaeté, Minas Gerais and grown in Hidrolândia, Goiás; to evaluate the antimicrobial activity of the essential oil, crude ethanol extract, and hexane, dichloromethane, ethyl-acetate, and aqueous fractions (AFs); to study the antinociceptive, anti-inflammatory, and central nervous system activities of the crude ethanol extract. Materials and methods: The essential oils were obtained by hydro-distillation using a Clevenger-type apparatus and analyzed by GC/MS. The antimicrobial activity in vitro was performed by broth microdilution method. The pharmacological tests were performed using female Swiss albino mice. Results: The major components of the essential oil were isoborneol (14.66%), bornyl acetate (11.86%), α -humulene (11.23%), α -fenchene (9.32%), and 1.8-cineole (7.05%), supporting the existence of two chemotypes of this species. The hexane fraction (HF) had good antifungal activity against Cryptococcus sp. ATCC D (MIC = 31.25 μg/mL) and Cryptococcus gatti L48 (MIC = 62.5 μg/mL). In the pharmacological tests, the crude ethanol extract presented antinociceptive and anti-inflammatory activities. Conclusion: Given that the ethanol extract of L. sidoides is included in the Formulary of Phytotherapeutic Agents of the Brazilian Pharmacopeia as an anti-inflammatory for oral cavities, the present work provides scientific evidence to back this use and highlight the importance of selecting the appropriate chemotype on the basis of the expected biological response. Abbreviations used: UFG: Universidade Federal de Goiás; HF: hexane fraction; DF: dichloromethane fraction; EAF: ethyl acetate fraction; AF: aqueous fraction; MeOH: methanol; MIC: minimum inhibitory concentration; ATCC: American Type Culture Collection; MH: Müller Hinton; DMSO: dimethyl sulfoxide; RPMI: Roswell Park Memorial Institute; NaCl: sodium chloride; μL: microliters; mL: milliliters; μg: microgram; kg: kilogram; h: hour; min: minute; cm: centimeter; COBEA: Brazilian College of Animal Experiments; p.o.:, oral; i.p.: intraperitoneal; s.c.: subcutaneous; SEM: standard error of the mean; RI: retention indices.
  1,630 28 -
Soyasaponin bb protects rat hepatocytes from alcohol-induced oxidative stress by inducing heme oxygenase-1
Lijie Zhu, Ranran Fu, Xiuying Liu, Yutang He, Bo Wang, Tao Ma
Oct-Dec 2016, 12(48):302-306
DOI:10.4103/0973-1296.192203  PMID:27867273
Background: It has been known that oxidative stress induced by alcohol played a crucial role in the formation of alcoholic liver disease. Although the formation mechanisms underlying liver injury induced by alcohol still remained largely unknown, it has been considered that oxidative stress played a core role in the pathogenesis of hepatocyte damage. Objective: The aim of this study was to investigate the effects of soyasaponin Bb (Ss-Bb) on oxidative stress in alcohol-induced rat hepatocyte injury. Results: It has been shown that the administration of Ss-Bb could significantly restore antioxidant activity in BRL 3A cells. Moreover, the impaired liver function and morphology changes resulting from ethanol exposure were improved by Ss-Bb treatment. Treatment with a pharmacological inhibitor of haem oxygenase-1 (HO-1) indicated a critical role of HO-1 in mediating the protective role. Finally, we found that pretreatment with Ss-Bb to ethanol exposure cells increased the expression level of HO-1.Conclusion: It was suggested that Ss-Bb may protect against alcohol-induced hepatocyte injury through ameliorating oxidative stress, and the induction of HO-1 was an important protective mechanism.
  1,604 29 -
Wound healing activity and chemical standardization of Eugenia pruniformis Cambess
Ricardo Diego Duarte Galhardo de Albuquerque, Jamila Alessandra Perini, Daniel Escorsim Machado, Thaís Angeli-Gamba, Ricardo dos Santos Esteves, Marcelo Guerra Santos, Adriana Passos Oliveira, Leandro Rocha
Oct-Dec 2016, 12(48):288-294
DOI:10.4103/0973-1296.192206  PMID:27867271
Background: Eugenia pruniformis is an endemic species from Brazil. Eugenia genus has flavonoids as one of the remarkable chemical classes which are related to the improvement of the healing process. Aims: To evaluate of wound healing activity of E. pruniformis leaves and to identify and quantify its main flavonoids compounds. Materials And Methods: Wound excision model in rats was used to verify the hydroethanolic and ethyl acetate extracts potential. The animals were divided in four groups of six and the samples were evaluated until the 15° day of treatment. Hydroxyproline dosage and histological staining with hematoxilin-eosin and Sirius Red were used to observe the tissue organization and quantify the collagen deposition, respectively. Chemical compounds of the ethyl acetate extract were identified by chromatographic techniques and mass spectrometry analysis and total flavonoids content was determined by spectrophotometric method. The antioxidant activity was determined by oxygen radical absorbing capacity (ORAC) and 2,2-diphenyl-1-picrylhydrazylhydrate radical photometric (DPPH) assays. Results: The treated group with the ethyl acetate extract showed collagen deposition increase, higher levels of hidroxyproline, better tissue reorganization and complete remodeling of epidermis. Quercetin, kaempferol and hyperoside were identified as main compounds and flavonoids content value was 43% (w/w). The ORAC value of the ethyl acetate extract was 0.81± 0.05 mmol TE/g whereas the concentration to produce 50% reduction of the DPPH was 7.05± 0.09 μg/mL. Conclusion: The data indicate a wound healing and antioxidant activities of E. pruniformis. This study is the first report of flavonoids and wound healing activity of E. pruniformis. Abbreviation used: NC: Negative control, PC: Positive control, CH: Crude hydroethanolic extract, EA: Ethyl acetate extract, TE: Trolox equivalent, mg: Milligram, mM: Millimolar, mL: Milliliter, HPLC-PDA: High performance liquid chromatography with a photodiode array detector, HRESI-MS: High-resolution electrospray ionization mass spectrometry analysis, TLC: Thin layer chromatography, ORAC: Oxygen radical absorbance capacity, w/v: Weight per volume
  1,489 25 -
Pharmacognostical analysis and protective effect of standardized extract and rizonic acid from Erythrina velutina against 6-hydroxydopamine-induced neurotoxicity in Sh-Sy5Y cells
Aline H Silva, Francisco Noé Fonseca, Antônia T. A. Pimenta, MaryAnne S Lima, Edilberto Rocha Silveira, Glauce S. B. Viana, Silvânia M. M. Vasconcelos, Luzia Kalyne A. M. Leal
Oct-Dec 2016, 12(48):307-312
DOI:10.4103/0973-1296.192200  PMID:27867274
Background: Erythrina velutina is a tree common in the northeast of Brazil extensively used by traditional medicine for the treatment of central nervous system disorders. Objective: To develop a standardized ethanol extract of E. velutina (EEEV) and to investigate the neuroprotective potential of the extract and rizonic acid (RA) from E. velutina on neuronal cells. Materials and methods: The plant drug of E. velutina previously characterized was used for the production of EEEV. Three methods were evaluated in order to obtain an extract with higher content of phenols. The neuroprotective effect of standardized EEEV (HPLC-PDA) and RA was investigated on SH-SY5Y cell exposure to the neurotoxin 6-hydroxydopamine (6-OHDA). Results: The powder of the plant drug was classified as moderately coarse and several quality control parameters were determined. EEEV produced by percolation gave the highest phenol content when related to others extractive methods, and its HPLC-PDA analysis allowed to identify four flavonoids and RA, some reported for the first time for the species. EEEV and RA reduced significantly the neurotoxicity induced by 6-OHDA in SH-SY5Y cells determined by the MTT assay and the nitrite concentration. EEEV also showed a free radical scavenging activity. Conclusion: This is the first pharmacological study about E. velutina which used a controlled standardized extract since the preparation of the herbal drug. This extract and RA, acting as an antioxidant, presents a neuroprotective effect suggesting that they have potential for future development as a therapeutic agent in neurodegenerative disease as Parkinson. Abbreviations used: ±: More or less, %: Percentage, °C: Degree Celsius, <: Less than, μg: Microgram, μL: Microliter, μM: Micromol, [1D] MNR: One-dimensional nuclear magnetic resonance spectroscopy, [2D] MNR:Two-dimensional nuclear magnetic resonance spectroscopy, 6-OHDA: [6-] Hydroxydopamine. Abs: Absorbance, CFU: Colony forming units, CH2Cl2: Dichloromethane, CHCl3: Chloroform cmCentimeter, DMEM/F12: Dulbecco's Modified Eagle's Medium: Nutrient Mixture F-12. DMSO: Dimethyl sulfoxide, DPPH: 1,1-Diphenyl-2-picrylhydrazyl, EAG: Gallic acid equivalents, EEEV: Ethanolic extract of Erythrina velutina, EtOAc: Ethyl acetate, g: Gram, h: Hour, H2O: Water, HPLC: High-performance liquid chromatography, H REIMS: Hydrogen rapid evaporative ionization mass spectrometry, Kg: Kilogram M: Molar, m: Metro, MeOH: Methanol, mg: Milligram, min: Minute, mL: Milliliter, mm: Millimeter, MTT: Bromide 3 [4,5-dimethylthiazol-2-yl] -2,5-diphenyltetrazolium, N: Normal, NBT: Nitroblue tetrazolium, nm: Nanometer, PDA: Photodiode array detector, TPC: Total polyphenol content, RA: Rizonic acid, RP: Reverse phase, SOD: Superoxide dismutase, v/v: Volume per volume, Vs: Versus W: Watts
  1,430 29 -
Ursolic acid, a natural pentacylcic triterpene from Ochrosia elliptica and its role in the management of certain neglected tropical diseases
Rola M Labib, Sherif S Ebada, Fadia S Youssef, Mohamed L Ashour, Samir A Ross
Oct-Dec 2016, 12(48):319-325
DOI:10.4103/0973-1296.192207  PMID:27867276
Background: Leishmaniasis and African trypanosomiasis are recognized as the leading causes of mortality and morbidity with the greatest prevalence in the developing countries. They affect more than one billion of the poorest people on the globe. Objective: To find a cheap, affordable, safe, and efficacious antileshmanial and antitrypanosomal natural drug and to elucidate its probable mode of action. Materials and Methods: Phytochemical investigation of the non-polar fraction of the methanol extract of leaves of Ochrosia elliptica Labill. (Apocyanaceae) resulted in the isolation of ursolic acid, which was unambiguously determined based on HR-ESI-FTMS, extensive 1D and 2D NMR spectroscopy. It was further tested for its cytotoxicity, antimicrobial, antimalarial, antileishmanial, and trypanocidal potency. in-silico molecular modeling studies were conducted on six vital parasitic enzymes including farnesyl diphosphate synthase, N -myristoyl transferase, pteridine reductase 1, trypanothione reductase, methionyl-tRNA synthetase, and inosine–adenosine–guanosine nucleoside hydrolase to discover its potential mode of action as antitrypanosomal and antileishmanial agent. Results: Ursolic acid displayed considerable antitrypanosomal and antileishmanial activities with IC50 values ranging between 1.53 and 8.79 μg/mL. It showed superior antitrypanosomal activity as compared to the standard drug difluoromethylornithine (DFMO), with higher binding affinities towards trypanothione reductase and pteridine reductase 1. It displayed free binding energy of -30.73 and -50.08 kcal/mole towards the previously mentioned enzymes, respectively. In addition, ursolic acid exhibited considerable affinities to farnesyl diphosphate synthase, N -myristoyl transferase and methionyl-tRNA synthetase with free binding energies ranging from -42.54 to -63.93 kcal/mole. Conclusion: Ursolic acid offers a safe, effective and cheap antitrypanosomal and antileishmanial candidate acting on several key parasitic enzymes. Abbreviations used: AHT: African Human Trypanosomiasis, ATCC: American type cell culture, BuOH: n -butanol, DCM: dichloromethane, DFMO: difluoromethylornithine, EtOAc: ethyl acetate, FCS: fetal calf serum, HMBC: Heteronuclear Multiple Bond Correlation, HMQC: Heteronuclear Multiple-Quantum Correlation, HR-ESI-FTMS: High Resolution Electrospray ionozation Mass Spectrometry, MENA: Middle East and North Africa, MeOH: Methanol, MRSA: Methicillin-resistant Staphylococcus aureus , NTDs: Neglected tropical diseases, TLC: Thin layer chromatography, UA: Ursolic acid, UV: Ultra violet, WHO: World Health Organization.
  1,423 29 -
Composition of the essential oil from danggui-zhiqiao herb-pair and its analgesic activity and effect on hemorheology in rats with blood stasis syndrome
Yuanqing Wang, Jianye Yan, Shunxiang Li, Wei Wang, Xiong Cai, Dan Huang, Limin Gong, Xin Li
Oct-Dec 2016, 12(48):271-275
DOI:10.4103/0973-1296.192195  PMID:27867268
Background: Angelica sinensis and Aurantii fructu used in a pair, named Danggui-Zhiqiao herb-pair (DZHP), which was rich in essential oil and has been adopted to promote blood circulation, dispel blood stasis, and relieve pain in traditional Chinese medicine (TCM) Objective: To analyze the composition and pharmacological effects of essential oil from DZHP Materials and Methods: The composition of the essential oil from DZHP was analyzed by gas chromatography/mass spectrometry (GC/MS). Its analgesic activity was evaluated by acetic acid-induced writhing test and hot plate test. The hemorheology test was carried out to evaluate the effect on hemorheology in rats with blood stasis syndrome Results: Twenty-eight components were identified and the main components were α-pinene (3.07%), β -pinene (2.0%), β -myrcene (3.71%), D-limonene (49.28%), γ -terpinen (9.53%), α -terpinolene (1.80%), α -terpineol (2.02%), β -bisabolene (1.13%), butylidenephthalide (1.43%), and Z-ligustilide (16.08%). The pharmacology test showed that the essential oil significantly inhibited the number of writhes induced by acetic acid with inhibition rate of 44.64% and significantly increased hot-plate latency compared with control group from 30 to 90 min after oral administration of drugs in mice. It could significantly decrease plasma viscosity, whole blood relative index at high and low shear rate, whole blood reduced viscosity at high and low shear rate, and erythrocyte rigidity index in hemorheology test Conclusion: The composition of the essential oil of DZHP was determined successfully and it had analgesic and promoting blood circulation activities. Abbreviations used: DZHP: Danggui-Zhiqiao herb-pair; TCM: traditional Chinese medicine; GC/MS: gas chromatography /mass spectrometry; PV: plasma viscosity; WBRI: whole blood relative index; WBRV: whole blood reduced viscosity; ERI: erythrocyte rigidity index
  1,399 34 -
Oryza sativa (Rice) hull extract inhibits lipopolysaccharide-induced inflammatory response in RAW264.7 macrophages by suppressing extracellular signal-regulated kinase, c-jun n-terminal kinase, and nuclear factor-κb activation
Sang Keun Ha, Jeehye Sung, Inwook Choi, Yoonsook Kim
Oct-Dec 2016, 12(48):295-301
DOI:10.4103/0973-1296.192198  PMID:27867272
Background: Rice (Oryza sativa ) is a major cereal crop in many Asian countries and an important staple food source. Rice hulls have been reported to possess antioxidant activities. Materials and Methods: In this study, we evaluated the antiinflammatory effects of rice hull extract and associated signal transduction mechanisms in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Results: We found that rice hull extract inhibited nitric oxide (NO) and prostaglandin E2 by suppressing the expression of inducible NO synthase and cyclooxygenase-2, respectively. The release of interleukin-1β and tumor necrosis factor-α was also reduced in a dose-dependent manner. Furthermore, rice hull extract attenuated the activation of nuclear factor-kappa B (NF-κB), as well as the phosphorylation of mitogen-activated protein kinases, extracellular signal-regulated kinase (ERK), and c-Jun N-terminal kinase (JNK), in LPS-stimulated RAW264.7 cells. Conclusion: This suggests that rice hull extract decreases the production of inflammatory mediators by downregulating ERK and JNK and the NF-κB signal pathway in RAW 264.7 cells. Abbreviation used: COX-2: cyclooxygenase-2, ERK: extracellular signal-regulated kinase, IκB: inhibitory kappa B, IL-1β: interleukin-1β, iNOS: inducible NO synthase, JNK: c-Jun N-terminal kinase, LPS: lipopolysaccharide, MAPKs: mitogen-activated protein kinases, NF-κB: nuclear factor-κB, NO: nitric oxide, PGE2: prostaglandin E2, RHE: rice hull extract, ROS: reactive oxygen species, TNF-α: tumor necrosis factor-α
  1,349 25 -
Improved oral bioavailability of total flavonoids of Dracocephalum moldavica via composite phospholipid liposomes: preparation, in-vitro drug release and pharmacokinetics in rats
Cheng Zeng, Wen Jiang, Meie Tan, Jianguo Xing, Chenghui He
Oct-Dec 2016, 12(48):313-318
DOI:10.4103/0973-1296.192201  PMID:27867275
Background: Dracocephalum moldavica L is a traditional Uygur medicine for centuries, total flavonoids extracted from Dracocephalum moldavica are the major active ingredients of herbs, which possesses significant medicinal values to treat coronart disease and hypertension, due to the glycosyl group on the ring, total flavonoids of Dracocephalum moldavica has low hydrophilic and poorly absorbed after oral administration, so one way is the formulation of poorly water soluble and permeabledrugs with lipids containing formulations such as Composite phospholipid liposomes to improve the absorption profile of drug. Objectives: To prepare composite phospholipid liposome (CPL) encapsulatetotal flavonoids extract from Dracocephalum moldavica (TFDM), determine its physicochemical properties,investigate its in-vitro release and evaluate the pharmacokinetics in Sprague-Dawley (SD) rats to increase the bioavailability of TFDM-CPL. Material and Methods: The TFDMCPL was prepared by the method of ammonium sulfate transmembrane gradients. The CPL and TFDM were separated by Sephadex-G50 chromatography. The concentration of TFDM in the CPL was detected by HPLC, then the entrapment efficiency (EE) was evaluated. And the shape, particle size, zeta potential, drug release in vitro of TFDMCPL were investigated, and the pharmacokinetics was evaluated by rat jugular vein intubation tube in SD rats. Results: The EE of TFDM was 84.17±2.2%, mean size of TFDMCPL was 136.2±3.7nm, polymey disperse index (PDI) was 0.158±0.015 and zeta potential was -19.8±1.2mV. TFDM-CPLwere found to enhance the release of drugs more effectively than TFDM based on the in vitro model and Following oral administration of TFDM, the plasma exposures of TFDM-CPL was significantly extended, and the mean concentration of TFDM-CPL was significantly higher compared to TFDM-solution . TheCmax, t1/2, AUC0-12 h values of TFDM for group of TFDM-CPL were siginificantly increased. Conclusion: The method of ammonium sulfate transmembrane gradients is suitable for preparingTFDM-CPL. And TFDM-CPL have potential to be used to improve the bioavailability of poorly soluble drugs after oral administration. Abbreviations Used: CPL: composite phospholipid liposome.; TFDM: Total Flavonoids Extract from Dracocephalum moldavica ; SD:Sprague-Dawley; EE:entrapment efficiency; PDI: polymey disperse index; TFDM-CPL: Total flavonoid extract from Dracocephalum moldavica – composite phospholipid liposome; DM:Dracocephalum moldavica L.; SPC: Soybean phospholipid; HSPC: Hydrogenated soya phosphatide; PBS: phosphate buffered saline; HPLC: high performance liquid chromatography; TEM: transmission electron microscopy; CMC-Na: Carboxy Methyl Cellulose-Natrium; AUC: area under the curve
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Characterization and bioavailability study of baicalin-mesoporous carbon nanopowder solid dispersion
Li Cui, E Sune, Jie Song, Jing Wang, Xiao-bin Jia, Zhen-hai Zhang
Oct-Dec 2016, 12(48):326-332
DOI:10.4103/0973-1296.192199  PMID:27867277
Background: Baicalin is the main bioactive constitute of the dried roots of Scutellaria baicalensis and possesses various biological activities. However, the poor water solubility and low oral bioavailability limit its efficacy. Objective: The present study was conducted to enhance the dissolution and oral bioavailability of baicalin (BA) through a novel mesoporous carbon nanopowder (MCN) drug carrier. Materials and Methods: Solid dispersions (SDs) of BA with MCN were prepared using a solvent evaporation method. The physical state of the formulations was investigated using SEM, differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). The pharmaceutical performance of pure BA, physical mixture (PM) and SDs was evaluated by performing an in-vitro dissolution test. The pharmacokinetic studies were conducted in SD rats and the analysis of the biological samples was performed on an Acquity UPLC–MS system. The intestinal and renal toxicity test of MCN was also evaluated. Results: The drug release profile indicated that the BA dissolution rate from SDs with a BA/MCN ratio of 1:6 greatly increased in comparison with that of the pure crystalline drug. Furthermore, a pharmacokinetic analysis in rats showed that the BA area under the concentration–time curve for SDs of MCN/BA was 1.83 times larger than that of pure BA. In comparison with the pure drug, the MCN–BA system significantly shortened the time to T max and generated higher C max. There was no intestinal and renal toxicity of MCN. Conclusion: These results indicated that the oral bioavailability of BA was remarkably improved by the MCN carrier. Additionally, intestinal toxicity test showed that MCN produced no toxicity in the gastrointestinal tract. Our results show that MCN-based SDs could be used to enhance the bioavailability of drugs with poor water solubility. Abbreviations used: BA: baicalin, MCN: mesoporous carbon nanopowder, SDs: solid dispersions, SEM: scanning electron microscopy, DSC: differential scanning calorimetry, XRD: powder X-ray diffraction, HPLC: high-performance liquid chromatography, PM: physical mixture, S.D.: standard deviation, ANOVA: analysis of variance, RSD: relative standard deviation, ESI: electrospray ionization, IS: internal standard, MRM: multiple reaction monitoring
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Preparation of sesquiterpenoids from Tussilago farfara L. by high-speed counter-current chromatography
Kun Cao, Yi Xu, Tian-Ming Zhao, Qing Zhang
Oct-Dec 2016, 12(48):282-287
DOI:10.4103/0973-1296.192196  PMID:27867270
Background: Sesquiterpenoids, such as tussilagone, has effects of raising blood pressure, antiplatelet aggregation, and anti-inflammation activities, which is regarded as index compound for quality control of Tussilago farfara L. Objective: This study was aimed to obtain an effective method for fast isolation of sesquiterpenoids from T. farfara L. by high-speed counter-current chromatography (HSCCC). Materials and Methods: A solvent optimization method for HSCCC was presented, i.e., the separation factors of compounds after the K values of solvent system should be investigated. Results: A ternary solvent system of n-hexane:methanol:water (5:8:2, v/v/v) was selected and applied for the HSCCC, and 56 mg of tussilagone (2) was isolated from T. farfara L., along with two other sesquiterpenoids 5.6 mg of 2,2-dimethyl-6-acetylchromanone (1) and 22 mg of 14-acetoxy-7 β-(3'-ethyl cis-crotonoyloxy)-lα-(2'-methylbutyryloxy)-notonipetranone (3) by HSCCC with high purities. Their chemical structures were elucidated by liquid chromatography-mass spectrometry and nuclear magnetic resonance experiments. Conclusion: These results offered an efficient strategy for preparation of potentially health-relevant phytochemicals from T. farfara L., which might be used for further chemical research and pharmacological studies by preparative HSCCC. Abbreviations used: HSCCC: High-Speed Counter-Current Chromatography; LC-MS: Liquid Chromatograph-Mass Spectrometer; NMR: Nuclear Magnetic Resonance; TCM: Traditional Chinese Medicine; HPLC: High Performance Liquid Chromatography; ESI-MS: Electrospray Ionization Mass Spectrometry; PE: petroleum ether
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