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
为了解麻楝(Chukrasia tabularis A. Juss)中的生物活性成分,采用柱色谱技术从其枝干乙醇提取物中分离得到10 个化合物,分别鉴定为:3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)propan-1-one (1)、6-hydroxy-1,3,5,7-tetrametho...为了解麻楝(Chukrasia tabularis A. Juss)中的生物活性成分,采用柱色谱技术从其枝干乙醇提取物中分离得到10 个化合物,分别鉴定为:3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)propan-1-one (1)、6-hydroxy-1,3,5,7-tetramethoxy-9-xanthen-9-one(2)、2,6,2′,6′-tetramethoxy-4,4′-bis(2,3-epoxy-1-hydroxypropyl)biphenyl (3)、cleomiscosin D (4)、chuktabularin A (5)、chuktabularin B (6)、chubularisin H (7)、chubularisin I (8)、tabularisin A (9)和tabularisin B (10),其中化合物1~4 为首次从麻楝属中分离得到.对体外α-葡萄糖苷酶的抑制活性进行了测定,结果表明化合物1、2、6、7 和9 对α-葡萄糖苷酶均具有较好的抑制活性.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.
文摘为了解麻楝(Chukrasia tabularis A. Juss)中的生物活性成分,采用柱色谱技术从其枝干乙醇提取物中分离得到10 个化合物,分别鉴定为:3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)propan-1-one (1)、6-hydroxy-1,3,5,7-tetramethoxy-9-xanthen-9-one(2)、2,6,2′,6′-tetramethoxy-4,4′-bis(2,3-epoxy-1-hydroxypropyl)biphenyl (3)、cleomiscosin D (4)、chuktabularin A (5)、chuktabularin B (6)、chubularisin H (7)、chubularisin I (8)、tabularisin A (9)和tabularisin B (10),其中化合物1~4 为首次从麻楝属中分离得到.对体外α-葡萄糖苷酶的抑制活性进行了测定,结果表明化合物1、2、6、7 和9 对α-葡萄糖苷酶均具有较好的抑制活性.