Streblus asper

Abstract: Bactericidal activity was found in the 50% ethanol (v/v) extract of Streblus asper leaves. The extract possessed a selective bactericidal activity towards Streptococcus, especially to Streptococcus mutans which has been shown to be strongly associated with dental caries. The extract had no effect on cultures of Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, Staphylococcus coagulase positive, Staphylococcus coagulase negative, Serratia marcescens, Klebsiella pneumoniae, Enterobacter, Pseudomonas aeruginosa, Burkholderia pseudomeallei and Candida albicans. The minimum growth inhibitory concentration and the minimum bactericidal concentration of S. asper extract against 10(8) CFU/mL of S. mutans was 2 mg/mL. The active compound is partially polar, partially heat labile, precipitated by 80% ammonium sulphate, and possesses a molecular weight larger than 10 000 Da. The potential for using S. asper extract as a natural product for controlling dental caries is discussed.

Abstract: Three new (1–3) and two known (4 and 5) cytotoxic cardiac glycosides were isolated and characterized from a medicinal plant, Streblus asper Lour. (Moraceae), collected in Vietnam, with six new analogues and one known derivative (5a–g) synthesized from (+)-strebloside (5). A preliminary structure–activity relationship study indicated that the C-10 formyl and C-5 and C-14 hydroxy groups and C-3 sugar unit play important roles in the mediation of the cytotoxicity of (+)-strebloside (5) against HT-29 human colon cancer cells. When evaluated in NCr nu/nu mice implanted intraperitoneally with hollow fibers facilitated with either MDA-MB-231 human breast or OVCAR3 human ovarian cancer cells, (+)-strebloside (5) showed significant cell growth inhibitory activity in both cases, in the dose range 5–30 mg/kg.