Dhawan Kamaldeep
University Institute of Pharmaceutical Sciences, Panjab Univesity, Chandigarh, India.
Addict Biol. 2003 Dec;8(4):379-86. doi: 10.1080/13556210310001646385.
The present work is a mini-review of the author's original work on the plant Passiflora incarnata Linn., which is used in several parts of the world as a traditional medicine for the management of anxiety, insomnia, epilepsy and morphine addiction. A tri-substituted benzoflavone moiety (BZF) has been isolated from the bioactive methanol extract of this plant, which has been proposed in the author's earlier work to be responsible for the biological activities of this plant. The BZF moiety has exhibited significantly encouraging results in the reversal of tolerance and dependence of several addiction-prone psychotropic drugs, including morphine, nicotine, ethanol, diazepam and delta-9-tetrahydrocannabinol, during earlier pharmacological studies conducted by the author. In addition to this, the BZF moiety has exhibited aphrodisiac, libido-enhancing and virility-enhancing properties in 2-year-old male rats. When administered concomitantly with nicotine, ethanol and delta-9-tetrahydrocannabinol for 30 days in male rats, the BZF also prevented the drug-induced decline in sexuality in male rats. Because the BZF moiety isolated from P. incarnata is a tri-substituted derivative of alpha-naphthoflavone (7,8-benzoflavone), a well-known aromatase-enzyme inhibitor, the mode of action of BZF has been postulated to be a neurosteroidal mechanism vide in which the BZF moiety prevents the metabolic degradation of testosterone and upregulates blood - testosterone levels in the body. As several flavonoids (e.g. chrysin, apigenin) and other phytoconstituents also possess aromatase-inhibiting properties, and the IC50 value of such phytomoieties is the main factor determining their biochemical efficacy, by altering their chemical structures to attain a desirable IC50 value new insights in medical therapeutics can be attained, keeping in view the menace of drug abuse worldwide.
本研究是作者对西番莲（Passiflora incarnata Linn.）原创研究的一篇小型综述。西番莲在世界多个地区被用作传统药物，用于治疗焦虑、失眠、癫痫和吗啡成瘾。从该植物的生物活性甲醇提取物中分离出了一种三取代苯并黄酮部分（BZF），作者早期的研究认为该部分是该植物生物活性的原因。在作者早期进行的药理研究中，BZF部分在逆转几种易成瘾精神药物（包括吗啡、尼古丁、乙醇、地西泮和Δ-9-四氢大麻酚）的耐受性和依赖性方面显示出了非常令人鼓舞的结果。除此之外，BZF部分在2岁雄性大鼠中表现出了壮阳、增强性欲和增强性功能的特性。当与尼古丁、乙醇和Δ-9-四氢大麻酚在雄性大鼠中同时给药30天时，BZF还能防止药物引起的雄性大鼠性功能下降。由于从西番莲中分离出的BZF部分是一种著名的芳香酶抑制剂α-萘黄酮（7,8-苯并黄酮）的三取代衍生物，因此推测BZF的作用模式是一种神经甾体机制，即BZF部分可防止睾酮的代谢降解并上调体内血液睾酮水平。由于几种黄酮类化合物（如白杨素、芹菜素）和其他植物成分也具有芳香酶抑制特性，并且此类植物部分的IC50值是决定其生化功效的主要因素，考虑到全球药物滥用的威胁，通过改变其化学结构以获得理想的IC50值，可以在医学治疗方面获得新的见解。
