Drug/substance reversal effects of a novel tri-substituted benzoflavone moiety (BZF) isolated from Passiflora incarnata Linn.--a brief perspective

Addict Biol. 2003 Dec;8(4):379-86. doi: 10.1080/13556210310001646385.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Aphrodisiacs / isolation & purification
  • Aphrodisiacs / therapeutic use
  • Aromatase Inhibitors*
  • Benzoflavones / isolation & purification*
  • Benzoflavones / therapeutic use
  • Blood-Testis Barrier / drug effects
  • Humans
  • Illicit Drugs*
  • Libido / drug effects
  • Male
  • Passiflora / chemistry*
  • Phytotherapy*
  • Plant Extracts / isolation & purification*
  • Plant Extracts / therapeutic use
  • Rats
  • Substance-Related Disorders / rehabilitation*
  • Testosterone / blood

Substances

  • Aphrodisiacs
  • Aromatase Inhibitors
  • Benzoflavones
  • Illicit Drugs
  • Plant Extracts
  • Testosterone