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大麻素的真菌生物转化:新型有效药物的潜力。

Fungal biotransformation of cannabinoids: potential for new effective drugs.

作者信息

Saxena Sanjai

机构信息

Natural Products and Drug Discovery, Department of Biotechnology and Environmental Sciences, Thapar University, Thapar Technology Campus, Patiala, Punjab 147004, India.

出版信息

Curr Opin Drug Discov Devel. 2009 Mar;12(2):305-12.

PMID:19333876
Abstract

Phytocannabinoids from the plant Cannabis sativa induce a variety of physiological and pharmacological responses in living systems, including anti-inflammatory, antinociceptive, anti-ulcer and antitumor activities. The discovery of the cannabinoid receptors CB1 and CB2 led to the development of agonists and antagonists of these receptors for the treatment of a variety of diseases. Nabilone, a synthetic derivative of Delta9-tetrahydrocannabinol (Delta9-THC), which is the main natural psychotropic constituent of C sativa, was approved by the US FDA for the treatment of nausea and as an anti-emetic for patients undergoing chemotherapy. Delta9-THC and related cannabinoids are involved in a variety of signal transduction pathways; thus, reducing or removing the psychotropic effects of these compounds would enhance their therapeutic spectra. Compound synthesis and qualitative SAR studies are time-consuming activities; however, microbes are effectively the most inventive synthetic chemists because of their metabolic plasticity. This review discusses the potential of C sativa mycoflora, which is pathogenic as well as endophytic, to remove the psychotropic effects of Delta9-THC and related cannabinoids, and describes the development of a model system for the rapid and cost-effective commercial production of cannabinoids through fermentation pathways.

摘要

来自植物大麻的植物大麻素在生物系统中可引发多种生理和药理反应,包括抗炎、抗伤害感受、抗溃疡和抗肿瘤活性。大麻素受体CB1和CB2的发现促使人们开发这些受体的激动剂和拮抗剂来治疗多种疾病。纳布隆是Δ9-四氢大麻酚(Δ9-THC)的合成衍生物,Δ9-THC是大麻的主要天然精神活性成分,它已被美国食品药品监督管理局批准用于治疗恶心,并作为化疗患者的止吐药。Δ9-THC及相关大麻素参与多种信号转导途径;因此,降低或消除这些化合物的精神活性作用将扩大其治疗范围。化合物合成和定性构效关系研究耗时费力;然而,微生物因其代谢可塑性实际上是最具创造性的合成化学家。本文综述了致病性和内生性大麻真菌群去除Δ9-THC及相关大麻素精神活性作用的潜力,并描述了通过发酵途径快速且经济高效地商业化生产大麻素的模型系统的开发。

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