Background:Chukrasia velutina is an enthnomedicinally used plant reported to have significant medicinal values.The present study aimed to explore the pharmacological activities of bark methanol extract using in vitro,...Background:Chukrasia velutina is an enthnomedicinally used plant reported to have significant medicinal values.The present study aimed to explore the pharmacological activities of bark methanol extract using in vitro,in vivo and in silico models.Methods:The study was designed to investigate the pharmacological effects of methanol extract of Chukrasia velutina bark(MECVB)through in vitro,in vivo and in silico assays.Analgesic activity was tested using formalin-i nduced nociception and acetic acid-i nduced writhing assays while the antipyretic effect was tested using yeast-i nduced hyperthermia in mice model.The antioxidant effect was tested using the DPPH and reducing power assay and the cytotoxic screening was tested using the brine shrimp lethality bioassay.In addition,in silico studies were conducted using computer aided methods.Results:In the acetic acid-i nduced writhing assay,the extract showed 28.36%and 56.16%inhibition of writhing for doses of 200 and 400 mg/kg,respectively.Moreover,a dose-dependent formalin-i nduced licking response was observed in both early and late phase.In yeast-i nduced pyrexia,the MECVB exhibited(p<0.05)antipyretic effect.The extract demonstrated an ICvalue of 78.86μg/ml compared with ascorbic acid(IC23.53μg/ml)in the DPPH scavenging assay.The compounds sitosterol,5,7-dimethoxycoumarin and scopoletin were seen be effective in molecular docking scores against COX-I(2OYE),COX-II(6COX)and human peroxiredoxin 5(1HD2).In ADME/T analysis,5,7-dimethoxycoumarin and scopoletin satisfied Lipinski’s rule of five and thus are potential drug candidates.Conclusion:The bark of Chukrasia velutina showed significant analgesic and antipyretic properties and is a potential source of natural anti-oxidative agents.展开更多
Background: Curculigo recurvata(C. recurvata) is an enthnomedicinally important herb reported to have significant medicinal values. The present study aimed to explore the in vivo and in silico anti-nociceptive and ant...Background: Curculigo recurvata(C. recurvata) is an enthnomedicinally important herb reported to have significant medicinal values. The present study aimed to explore the in vivo and in silico anti-nociceptive and anti-diarrheal effects of a C. recurvate rhizome methanol extract(Me-RCR).Methods: The analgesic effects of Me-RCR were assessed using acetic acid-induced writhing and the formalin-induced flicking test. The drugs were administered intraperitoneally(IP) at doses of 200 and 400 mg/kg body weight(bw). Anti-diarrheal activity was evaluated by assessing intestinal motility, hypersecretion, and fecal score in mice at oral doses of 200 and 400 mg/kg·bw. Computer facilitated analyses for anti-nociceptive and anti-diarrheal activities of three isolated compounds from C. recurvata were undertaken to identify the best-fit phytoconstituents.Results: The Me-RCR showed significant(P <.05) peripheral anti-nociception at the highest dose. The extract inhibited both early and late phases of nociception in the formalin-induced writhing test. In the castor oil-induced diarrhoea model, the extract significantly(P <.05) prolonged the onset time of diarrhoea, inhibited percentage of diarrhoea, and decreased both the volume and weight of intestinal contents. Rates of intestinal fluid accumulation inhibition were(33.61 ± 1.00)% and(46.44 ± 0.89)% at Me-RCR doses of 200 and 400 mg/kg·bw, respectively. Moreover, a significant(P <.05) reduction in gastrointestinal motility was observed. An absorption, distribution, metabolism, excretion and/or toxicity(ADME/T) test showed that the selected compounds yielded promising results, satisfying Lipinski's rule of five for predicting drug-like potential. Notably, of the three phytoconstituents curculigine and isocurculigine possessed the highest affinity for the COX-1 and COX-2. Isocurculigine was also identified as the most effective anti-diarrheal compound in the computer-facilitated model.Conclusion: An extract of the plant C. recurvata showed potential analgesic and antidiarrheal activity due to the presence of one or more active secondary metabolite(s).展开更多
Background:Many kinds of orchids have significant health benefits although ade-quate research on their biological functions is yet to be carried out.This study inves-tigated the paracetamol-induced liver damage-protec...Background:Many kinds of orchids have significant health benefits although ade-quate research on their biological functions is yet to be carried out.This study inves-tigated the paracetamol-induced liver damage-protecting effect of epiphytic Aerides odorata methanol extract(AODE).Methods:The protective effects of AODE were studied by analyzing its effect on liver function parameters,messenger RNA(mRNA)expression,and tissue histopatho-logical architecture.The results were confirmed by ligand-receptor interaction of molecular docking and multitarget interaction of network pharmacological analyses.Results:AODE significantly(p<0.05)minimized the dose-dependent increase in acid phosphatase,aspartate aminotransferase,alanine aminotransferase,alkaline phos-phatase,γ-glutamyl transferase,lactate dehydrogenase,and total bilirubin compared to the reference drug silymarin.Malondialdehyde level decreased,and the antioxidant genes catalase(CAT),superoxide dismutase(SOD),β-actin,paraoxonase-1(PON1),and phosphofructokinase-1(PFK-1)were upregulated in AODE-treated paracetamol-intoxicated rats.A total of 376 compounds comprising phenols and flavonoids were identified using ultra-high-performance liquid chromatography-quadrupole time-of-flight-mass spectrometry(UPLC-qTOF-MS).The online toxicity assessment using SwissADME and admetSAR exhibited drug-like,nontoxic,and potential pharmaco-logical properties.Additionally,in silico analysis showed that isoacteoside,one of the identified compounds,exhibited the best docking score(−11.42)with the liver pro-tein human pituitary adenylate cyclase-1(Protein Data Bank ID:3N94).Furthermore,network pharmacology analysis identified the top 10 hub genes,namely AKT1(protein kinase B),CTNNB1(catenin beta-1),SRC(proto-oncogene c-Src),TNF(tumor necrosis factor),EGFR(epidermal growth factor receptor),HSP90AA1(heat shock protein 90α),MAPK3(mitogen-activated protein kinase 3),STAT3(signal transducer and activator of transcription 3),CASP3(caspase protein),and ESR1(estrogen receptor 1),which are responsible for hepatoprotective activity.Conclusion:The findings demonstrate that AODE could be a novel hepatoprotective target in drug-induced liver damage with a further single compound-based animal study.展开更多
文摘Background:Chukrasia velutina is an enthnomedicinally used plant reported to have significant medicinal values.The present study aimed to explore the pharmacological activities of bark methanol extract using in vitro,in vivo and in silico models.Methods:The study was designed to investigate the pharmacological effects of methanol extract of Chukrasia velutina bark(MECVB)through in vitro,in vivo and in silico assays.Analgesic activity was tested using formalin-i nduced nociception and acetic acid-i nduced writhing assays while the antipyretic effect was tested using yeast-i nduced hyperthermia in mice model.The antioxidant effect was tested using the DPPH and reducing power assay and the cytotoxic screening was tested using the brine shrimp lethality bioassay.In addition,in silico studies were conducted using computer aided methods.Results:In the acetic acid-i nduced writhing assay,the extract showed 28.36%and 56.16%inhibition of writhing for doses of 200 and 400 mg/kg,respectively.Moreover,a dose-dependent formalin-i nduced licking response was observed in both early and late phase.In yeast-i nduced pyrexia,the MECVB exhibited(p<0.05)antipyretic effect.The extract demonstrated an ICvalue of 78.86μg/ml compared with ascorbic acid(IC23.53μg/ml)in the DPPH scavenging assay.The compounds sitosterol,5,7-dimethoxycoumarin and scopoletin were seen be effective in molecular docking scores against COX-I(2OYE),COX-II(6COX)and human peroxiredoxin 5(1HD2).In ADME/T analysis,5,7-dimethoxycoumarin and scopoletin satisfied Lipinski’s rule of five and thus are potential drug candidates.Conclusion:The bark of Chukrasia velutina showed significant analgesic and antipyretic properties and is a potential source of natural anti-oxidative agents.
基金Center for Research and Publication,Grant/Award Number 180111International Islamic University Chittagong。
文摘Background: Curculigo recurvata(C. recurvata) is an enthnomedicinally important herb reported to have significant medicinal values. The present study aimed to explore the in vivo and in silico anti-nociceptive and anti-diarrheal effects of a C. recurvate rhizome methanol extract(Me-RCR).Methods: The analgesic effects of Me-RCR were assessed using acetic acid-induced writhing and the formalin-induced flicking test. The drugs were administered intraperitoneally(IP) at doses of 200 and 400 mg/kg body weight(bw). Anti-diarrheal activity was evaluated by assessing intestinal motility, hypersecretion, and fecal score in mice at oral doses of 200 and 400 mg/kg·bw. Computer facilitated analyses for anti-nociceptive and anti-diarrheal activities of three isolated compounds from C. recurvata were undertaken to identify the best-fit phytoconstituents.Results: The Me-RCR showed significant(P <.05) peripheral anti-nociception at the highest dose. The extract inhibited both early and late phases of nociception in the formalin-induced writhing test. In the castor oil-induced diarrhoea model, the extract significantly(P <.05) prolonged the onset time of diarrhoea, inhibited percentage of diarrhoea, and decreased both the volume and weight of intestinal contents. Rates of intestinal fluid accumulation inhibition were(33.61 ± 1.00)% and(46.44 ± 0.89)% at Me-RCR doses of 200 and 400 mg/kg·bw, respectively. Moreover, a significant(P <.05) reduction in gastrointestinal motility was observed. An absorption, distribution, metabolism, excretion and/or toxicity(ADME/T) test showed that the selected compounds yielded promising results, satisfying Lipinski's rule of five for predicting drug-like potential. Notably, of the three phytoconstituents curculigine and isocurculigine possessed the highest affinity for the COX-1 and COX-2. Isocurculigine was also identified as the most effective anti-diarrheal compound in the computer-facilitated model.Conclusion: An extract of the plant C. recurvata showed potential analgesic and antidiarrheal activity due to the presence of one or more active secondary metabolite(s).
文摘Background:Many kinds of orchids have significant health benefits although ade-quate research on their biological functions is yet to be carried out.This study inves-tigated the paracetamol-induced liver damage-protecting effect of epiphytic Aerides odorata methanol extract(AODE).Methods:The protective effects of AODE were studied by analyzing its effect on liver function parameters,messenger RNA(mRNA)expression,and tissue histopatho-logical architecture.The results were confirmed by ligand-receptor interaction of molecular docking and multitarget interaction of network pharmacological analyses.Results:AODE significantly(p<0.05)minimized the dose-dependent increase in acid phosphatase,aspartate aminotransferase,alanine aminotransferase,alkaline phos-phatase,γ-glutamyl transferase,lactate dehydrogenase,and total bilirubin compared to the reference drug silymarin.Malondialdehyde level decreased,and the antioxidant genes catalase(CAT),superoxide dismutase(SOD),β-actin,paraoxonase-1(PON1),and phosphofructokinase-1(PFK-1)were upregulated in AODE-treated paracetamol-intoxicated rats.A total of 376 compounds comprising phenols and flavonoids were identified using ultra-high-performance liquid chromatography-quadrupole time-of-flight-mass spectrometry(UPLC-qTOF-MS).The online toxicity assessment using SwissADME and admetSAR exhibited drug-like,nontoxic,and potential pharmaco-logical properties.Additionally,in silico analysis showed that isoacteoside,one of the identified compounds,exhibited the best docking score(−11.42)with the liver pro-tein human pituitary adenylate cyclase-1(Protein Data Bank ID:3N94).Furthermore,network pharmacology analysis identified the top 10 hub genes,namely AKT1(protein kinase B),CTNNB1(catenin beta-1),SRC(proto-oncogene c-Src),TNF(tumor necrosis factor),EGFR(epidermal growth factor receptor),HSP90AA1(heat shock protein 90α),MAPK3(mitogen-activated protein kinase 3),STAT3(signal transducer and activator of transcription 3),CASP3(caspase protein),and ESR1(estrogen receptor 1),which are responsible for hepatoprotective activity.Conclusion:The findings demonstrate that AODE could be a novel hepatoprotective target in drug-induced liver damage with a further single compound-based animal study.
