Salha M Aljubiri, Eman Abd Elsalam, Faten K Abd El Hady, Mohamed O Radwan, Abdulrahman I Almansour, Kamel H Shaker
{"title":"<i>In vitro</i> acetylcholinesterase, tyrosinase inhibitory potentials of secondary metabolites from <i>Euphorbia schimperiana</i> and <i>Euphorbia balsamifera</i>.","authors":"Salha M Aljubiri, Eman Abd Elsalam, Faten K Abd El Hady, Mohamed O Radwan, Abdulrahman I Almansour, Kamel H Shaker","doi":"10.1515/znc-2021-0178","DOIUrl":null,"url":null,"abstract":"<p><p>Acetylcholinesterase, tyrosinase, and <i>α</i>-glucosidase inhibition activities of <i>Euphorbia schimperiana</i> and <i>Euphorbia balsamifera</i> extracts, fractions, and available pure compounds were evaluated for the first time. Acetylcholinesterase assay revealed a significant inhibitory activity of <i>E. balsamifera</i> total extract and <i>n</i>-hexane fraction with 47.7% and 43.3%, respectively, compared to the reference drug, which was 75%. The <i>n</i>-butanol fraction demonstrated tyrosinase inhibitory activity for <i>E. balsamifera</i> and <i>E. schimperiana</i> with 36.7% and 29.7%, respectively, compared to 60% for the reference drug. Quercetin-3-<i>O-α</i>-glucuronide, quercetin-3-<i>O-β-D</i>-glucuronide-methyl ester, quercetin-3-<i>O-α-L</i>-rhamnoside, 3,3'-di-<i>O</i>-methyl ellagic acid, 3,3'<i>-di-O</i>-methyl-ellagic acid-4-<i>β-D</i>-xylopyranoside, and 4-<i>O</i>-ethyl gallic acid were identified from <i>E. schimperiana</i> while quercetin-3-<i>O</i>-glucopyranoside and isoorientin were determined from <i>E. balsamifera</i>. The AChE inhibitory effect of pure compounds exhibited promising activity, where 4-<i>O</i>-ethylgallic acid demonstrated 51.1%, while the highest tyrosinase inhibition was demonstrated by isoorientin with 50.6% compared to the reference drug (60%). Finally, a molecular docking study was performed for the most promising AChE and tyrosinase inhibitors. The extracts, fractions, and isolated compounds showed no α-glucosidase inhibitory activity.</p>","PeriodicalId":49344,"journal":{"name":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","volume":"78 5-6","pages":"209-216"},"PeriodicalIF":1.8000,"publicationDate":"2023-05-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Zeitschrift Fur Naturforschung Section C-A Journal of Biosciences","FirstCategoryId":"99","ListUrlMain":"https://doi.org/10.1515/znc-2021-0178","RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 1
Abstract
Acetylcholinesterase, tyrosinase, and α-glucosidase inhibition activities of Euphorbia schimperiana and Euphorbia balsamifera extracts, fractions, and available pure compounds were evaluated for the first time. Acetylcholinesterase assay revealed a significant inhibitory activity of E. balsamifera total extract and n-hexane fraction with 47.7% and 43.3%, respectively, compared to the reference drug, which was 75%. The n-butanol fraction demonstrated tyrosinase inhibitory activity for E. balsamifera and E. schimperiana with 36.7% and 29.7%, respectively, compared to 60% for the reference drug. Quercetin-3-O-α-glucuronide, quercetin-3-O-β-D-glucuronide-methyl ester, quercetin-3-O-α-L-rhamnoside, 3,3'-di-O-methyl ellagic acid, 3,3'-di-O-methyl-ellagic acid-4-β-D-xylopyranoside, and 4-O-ethyl gallic acid were identified from E. schimperiana while quercetin-3-O-glucopyranoside and isoorientin were determined from E. balsamifera. The AChE inhibitory effect of pure compounds exhibited promising activity, where 4-O-ethylgallic acid demonstrated 51.1%, while the highest tyrosinase inhibition was demonstrated by isoorientin with 50.6% compared to the reference drug (60%). Finally, a molecular docking study was performed for the most promising AChE and tyrosinase inhibitors. The extracts, fractions, and isolated compounds showed no α-glucosidase inhibitory activity.
首次评价了大戟和香茅提取物、馏分及有效化合物对乙酰胆碱酯酶、酪氨酸酶和α-葡萄糖苷酶的抑制活性。乙酰胆碱酯酶测定结果显示,香茅总提取物和正己烷部位对乙酰胆碱酯酶的抑制活性分别为47.7%和43.3%,而对照药的抑制活性为75%。正丁醇部分对香茅和刺花的酪氨酸酶抑制活性分别为36.7%和29.7%,而对照药为60%。槲皮素-3- o -α-葡萄糖苷、槲皮素-3- o -β- d-葡萄糖苷甲酯、槲皮素-3- o -α- l-鼠李糖苷、3,3'-二- o -甲基鞣花酸、3,3'-二- o -甲基鞣花酸-4-β- d-木pyrano苷和4- o -乙基没食子酸;香茅中槲皮素-3- o -葡萄糖苷和异荭草苷。纯化合物对乙酰胆碱酯酶的抑制效果很有前景,其中4- o -乙基没食子酸的抑制率为51.1%,异荭草苷对酪氨酸酶的抑制率最高,为50.6%,高于参比药的60%。最后,对最有前途的乙酰胆碱酯酶和酪氨酸酶抑制剂进行分子对接研究。提取物、馏分及分离物均无α-葡萄糖苷酶抑制活性。
期刊介绍:
A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) is an international scientific journal and a community resource for the emerging field of natural and natural-like products. The journal publishes original research on the isolation (including structure elucidation), bio-chemical synthesis and bioactivities of natural products, their biochemistry, pharmacology, biotechnology, and their biological activity and innovative developed computational methods for predicting the structure and/or function of natural products. A Journal of Biosciences: Zeitschrift für Naturforschung C (ZNC) welcomes research papers in fields on the chemistry-biology boundary which address scientific ideas and approaches to generate and understand natural compounds on a molecular level and/or use them to stimulate and manipulate biological processes.