A Bioassay for Inhibition of Serotonin Release from Bovine Platelets

Abstract

A bioassay was developed to study agents capable of inhibiting the release of serotonin from bovine blood platelets. It is a simple, inexpensive, and reproducible high-throughput bioassay suitable for quality control of feverfew, Tanacetum parthenium, a crude drug with proven migraine prophylactic activity that is being considered for governmental registration and regulation. The bioassay, which requires no experimental animals or human subjects, was used to assess the in vitro activity of T. parthenium samples grown from seed obtained from 10 different regions of Europe. The activity was found to vary significantly within and between samples, with no geographical correlation. Serotonin release inhibition was shown to be significantly correlated with the content of the germacranolide sesquiterpene lactone, parthenolide, although other sesquiterpene lactones from this plant and other members of the Asteraceae were also shown to be active. The activities of six other species of Tanacetum, as well as of Artemisia absinthium (wormwood) and Zingiber officinale (ginger), and two commercial drugs for migraine prophylaxis, verapamil hydrochloride and propranolol hydrochloride, were also assessed. The relevance of the bovine platelet serotonin release inhibition bioassay to antimigraine research is discussed.

Herbal medicine: Is it an alternative or an unknown? A brief review of popular herbals used by patients in a pain and symptom management practice setting

“…This was felt to be due to variation in content and lack of standardization in different preparations. Marles et al [69] found wide variation in the amount of the active ingredient, parthenolide, from a variety of samples from 10 different regions of Europe. Feverfew inhibits serotonin release from aggregating platelets [69,70], as well as possibly inhibiting cell phospholipases, which prohibit release of arachadonic acid as part of the inflammatory response [71].…”

“…Marles et al [69] found wide variation in the amount of the active ingredient, parthenolide, from a variety of samples from 10 different regions of Europe. Feverfew inhibits serotonin release from aggregating platelets [69,70], as well as possibly inhibiting cell phospholipases, which prohibit release of arachadonic acid as part of the inflammatory response [71]. Although it has been found to reduce 86% to 88% of prostaglandin production, it is not found to inhibit cyclooxygenase [72].…”

Inhibition by hydroxyachillin, sesquiterpene lactone fromTanacetum microphyllum, of PMA-induced mouse ear oedema

“…Sesquiterpene lactones containing an c~-methylene butyrolactone unit, including parthenolide isolated from Tanacetum parthenium, caused changes in AA metabolism, through a mechanism probably not involving phospholipase inactivation. These data suggest a possible interaction of these compounds with PKC [18,19].…”

Neural Networks as Valuable Tools To Differentiate between Sesquiterpene Lactones’ Inhibitory Activity on Serotonin Release and on NF-κB

“…After centrifugation the supernatant was subjected to scintillation counting. 31 Structure Representations. Single low-energy 3D conformations were generated by CORINA.…”