Glycopentalone, a novel compound from Glycosmis pentaphylla (Retz.) Correa with potent anti-hepatocellular carcinoma activity.

ETHNOPHARMACOLOGICAL RELEVANCE: Glycosmis pentaphylla (Retz.) Correa is used in Indian traditional medicine against various liver ailments, including cancer. AIM OF THE STUDY: Isolation and characterization of the most active anti-hepatocellular carcinoma (HCC) compound from the alcohol extract of G. pentaphylla. MATERIALS AND METHODS: Different chromatographic (HPLC, TLC and column chromatography) and methods like IR, LCMS and NMR were used for the isolation and structural identification of the active anti-HCC compound from G. pentaphylla. Cytotoxic and apoptosis inducing effect of the active compound were assessed in Hep3 B, RAW264.7 and HEK293 cell lines by MTT assay, morphological studies, Hoechst staining and Annexin V FITC assay. RESULTS: The most active compound was isolated as yellow needle shaped crystals. The structure of the compound was identified by IR, LCMS and NMR methods. The structural details show that the isolated compound is a novel chemical and have structural similarity with chalcone. MTT assay, physiological and FACS analysis proved the anti-HCC efficacy of the isolated compound in vitro. CONCLUSION: The study confirmed that the most active anti-HCC compound present in the alcohol extract of G. pentaphylla is a chalcone derivative. This compound showed specific cytotoxicity against Hep3 B with minor cytotoxicity against non HCC cell lines, RAW264.7 and HEK293. The present study, therefore, supports the folklore knowledge for the utility of G. pentaphylla and provides a scientific basis for their traditional usage against liver cancer.

The apoptosis inducing effect of Glycosmis pentaphylla (Retz.) Correa and its influence on gene expression in hepatocellular carcinoma cell line, Hep3 B.

ETHNOPHARMACOLOGICAL RELEVANCE: Glycosmis pentaphylla (Retz.) Correa is used in Indian traditional medicine against jaundice and other liver disorders. AIM OF THE STUDY: The study aims to determine the in vitro anticancer and apoptosis inducing activity of Glycosmis pentaphylla in hepatocellular carcinoma cell line, Hep3 B. MATERIALS AND METHODS: The cytotoxic and apoptosis inducing activity of the crude extract and active fractions were estimated on Hep3 B and RAW264.7 cell lines by MTT assay, Hoechst staining, DNA fragmentation, morphological studies, reverse transcription polymerase chain reaction and anti-poly-(ADP-ribose)-polymerase assays. The phytochemical profiling of active extract was done by TLC and HPTLC methods. RESULTS: Ethanol extract of Glycosmis pentaphylla was more effective than other extracts in reducing the proliferation of Hep3 B cells. As revealed by the results from DNA fragmentation, Hoechst staining, morphological studies, RT-PCR, PARP cleavage and gene expression studies, active extract induced apoptosis on Hep3 B cell line in concentration and time dependent manner with increase in the Bax/Bcl2 gene expression ratio. Chemo profiling data revealed the presence of flavonoid in the active fraction. CONCLUSIONS: The study showed that major active component in the ethanol extract of Glycosmis pentaphylla is a flavonoid which induces apoptosis on cancer cell line, Hep3 B, by increasing the expression ratio of Bax/Bcl2 genes in a time and dose dependent manner.

Cytotoxic and apoptotic activity of Cheilanthes farinosa (Forsk.) Kaulf. against human hepatoma, Hep3B cells.

AIM OF THE STUDY: Cheilanthes farinosa (Forsk.) Kaulf., family: Adianthaceae, is a fern of immense medicinal properties used in ethno-medicine. The Gaddis tribe of Himachal Pradesh, India, has been using this fern to treat liver damage. Aim of the current study was to determine the apoptosis inducing and cytotoxic activity, if any, of this fern towards hepatic cancer cells. MATERIALS AND METHODS: Water extract of the plant was used in the study. MTT assay was performed in hepatocellular carcinoma cell line, Hep3B as well as murine macrophage cell line, RAW264.7 to analyze the cytotoxic activity of the plant. Further, the apoptosis inducing action of water extract of the plant was evaluated using comet assay, DNA fragmentation analysis, DAPI staining of chromatin and Annexin V-FITC staining. RESULTS: This plant was found to produce considerable cytotoxicity in hepatoma cell line, Hep3B without inducing substantial damage to non-cancerous cell line RAW264.7. In addition, this plant was found to induce apoptosis in Hep3B cells. This was substantiated by comet assay, DNA fragmentation analysis, DAPI staining of chromatin and Annexin V-FITC staining for detecting early stage of apoptosis. CONCLUSIONS: This investigation shows that the water extract of Cheilanthes farinosa has antiproliferative and apoptotic activity in human liver cancer cells and is not deleterious towards non-cancerous macrophage cell line.