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Enzymatic biotransformation of terpenes as bioactive agents

机译:萜类作为生物活性剂的酶促生物转化

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Abstract The plant-derived terpenoids are considered to be the most potent anticancer, anti-inflammatory and anticarcinogenic compounds known. Enzymatic biotransformation is a very useful approach to expand the chemical diversity of natural products. Recent enzymatic biotransformation studies on terpenoids have resulted in the isolation of novel compounds. 14-hydroxy methyl caryophyllene oxide produced from caryophyllene oxide showed a potent inhibitory activity against the butyryl cholinesterase enzyme, and was found to be more potent than parent caryophyllene oxide. The metabolites 3β,7β-dihydroxy-11-oxo-olean-12-en-30-oic acid, betulin, betulonic acid, argentatin A, incanilin, 18β glycyrrhetinic acid, 3,11-dioxo-olean-12-en-30-oic acid produced from 18β glycyrrhetinic acid were screened against the enzyme lipoxygenase. 3,11-Dioxo-olean-12-en-30-oic acid, was found to be more active than the parent compound. The metabolites 3β-hydroxy sclareol 18α-hydroxy sclareol, 6α,18α-dihydroxy sclareol, 11S,18α-dihydroxy sclareol, and 1β-hydroxy sclareol and 11S,18α-dihydroxy sclareol produced from sclareol were screened for antibacterial activity. 1β-Hydroxy sclareol was found to be more active than parent sclareol. There are several reports on natural product enzymatic biotransformation, but few have been conducted on terpenes. This review summarizes the classification, advantages and agents of enzymatic transformation and examines the potential role of new enzymatically transformed terpenoids and their derivatives in the chemoprevention and treatment of other diseases.
机译:摘要植物萜类化合物被认为是已知最有效的抗癌,抗炎和抗癌化合物。酶促生物转化是扩大天然产物化学多样性的非常有用的方法。最近对萜类化合物的酶促生物转化研究导致了新化合物的分离。由氧化石竹烯产生的14-羟甲基氧化石竹烯烯氧化物显示出对丁酰胆碱酯酶的有效抑制活性,并且被发现比母体石竹烯氧化物更有效。代谢产物3β,7β-二羟基-11-氧代-油酸-12-en-30-oic酸,桦木素,倍他宁酸,阿根廷精A,依他尼林,18β甘草次酸,3,11-二氧-油酸-12-en-30针对脂氧合酶筛选了由18β甘草次酸产生的-o酸。发现3,11-二氧代-油烷基-12-en-30-油酸比母体化合物更具活性。筛选了由香紫苏醇产生的代谢物3β-羟基香紫苏醇18α-羟基香紫苏醇,6α,18α-二羟基香紫苏醇,11S,18α-二羟基香紫苏醇和1β-羟基香紫苏醇和11S,18α-二羟基香紫苏醇的抗菌活性。发现1β-羟基香紫苏醇比母体香紫苏醇更具活性。关于天然产物酶促生物转化的报道很多,但是对萜烯的报道很少。这篇综述总结了酶促转化的分类,优势和作用,并考察了新的酶促转化的萜类化合物及其衍生物在化学预防和治疗其他疾病中的潜在作用。

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