Investigation of Antitubercular and Cytotoxic Activities of Fruit Extract and Isolated Compounds from Piper retrofractum Vahl



A bioassay guided fractionation procedure used on the crude methanol extract of Piper retrofractum fruit identified 4 compounds: piperine, methyl piperate, sylvatine, and piperlonguminine. The bioactivities of 4 compounds and the crude methanol extract were examined. The crude methanol extract showed antibacterial activity against Mycobacterium tuberculosis, with a minimum inhibitory concentration (MIC) of 25.00 µg/mL. Piperine and piperlonguminine inhibited M. tuberculosis with MIC values of 50.00 mg/mL, whereas methyl piperate and sylvatine were inactive (% inhibition less than 90 % at a 50.00 mg/mL concentration). The crude extract and all isolated compounds were tested for cytotoxic activity against lung cancer cells (SCLC-H22 and NCI-H187) and human gingival fibroblasts (HGF) in cell cultures. All 4 isolated compounds showed weak cytotoxic activity against lung cancer cells (SCLC-H22 and NCI-H187) and human gingival fibroblasts (HGF) (% inhibition less than 20 % at a 5 mg/mL concentration, or a % inhibition less than 50 % at a 50 mg/mL concentration). However the crude methanol extract showed moderate cytotoxic behavior against lung cancer cells (NCI-H187) and human gingival fibroblasts (HGF), with an IC50 of 20.98 mg/mL and % inhibition = 56.83 at 25 µg/mL concentration, respectively. The present findings suggest that the clinical advantages of the crude extract and isolated compounds of P. retrofractum Vahl lie in combination therapy in order to enhance the efficacy of conventional antitubercular or anticancer drugs.


Piper retrofractum Vahl, antitubercular, tuberculosis, cytotoxic activity

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