Protective effects of 3′‐deoxy‐4‐O‐methylepisappanol from Caesalpinia sappan against glutamate‐induced neurotoxicity in primary cultured rat cortical cells

Abstract

To examine the neuroprotective effects of Caesalpinia sappan L., we tested its protection against the glutamate-induced neurotoxicity in primary cortical cultured neurons. We found that an aqueous extract of this medicinal plant exhibited significant protection against glutamate-induced toxicity in primary cultured rat cortical cells. In order to clarify the neuroprotective mechanism(s) of this observed effect, isolation was performed to seek and identify active fractions and components. By such fractionation, two known compounds - sappanchalcone and 3'-deoxy-4-O-methylepisappanol - were isolated from the methanol extracts from the air-dried and chipped C. sappan. Among these two compounds, 3'-deoxy-4-O-methylepisappanol exhibited significant neuroprotective activities against glutamate-induced toxicity, exhibiting cell viability of about 50%, at concentrations ranging from 0.1 microM to 10 microM. Therefore, the neuroprotective effect of C. sappan might be due to the inhibition of glutamate-induced toxicity by the protosappanin derivative it contains.

PASS-Predicted Hepatoprotective Activity ofCaesalpinia sappanin Thioacetamide-Induced Liver Fibrosis in Rats

“…Several studies have shown that CS has antimicrobial and bactericidal activity [8] and antiallergic [9], neuroprotective [10], and hypoglycaemic effects [11]. Others found that extract from CS can be used for treating ascites, tumour, leukaemia [12], and arteriosclerosis [13].…”

Phenolics

“…9 Toxicodendron vernicifluum (Stokes) F.A. 47 From the same plant, littorachalcone (CS 3.34) doubled the neuritogenic effects of 2 ng/mL of NGF against PC12 cells. Br.)…”

The Genus Caesalpinia L. (Caesalpiniaceae): Phytochemical and Pharmacological Characteristics

“…Other compounds, such as sappanchalcone 19 and 3'-deoxy-4- O -methylepisapanol ( 54 ), which were obtained from the methanol extract from barks of C. sappan , were evaluated in cortical cells of rats injured with glutamate at doses of 0.1 to 10 µM. Only compound 54 showed significant activity, attenuating the toxicity induced by glutamate with cellular viability of 50–70% [ 63 , 64 ]. Other compound isolated from C. sappan , neo-sappanone ( 55 , Figure 4 ), was evaluated for inhibition of xanthine oxidase and showed a dose-dependent inhibitory activity with IC 50 of 29.7 µM, 10-fold less potent than the positive control allopurinol (IC 50 = 2.6 µM).…”