Tetrahydropentagamavunon-0 (THPGV-0) and Tetrahydropentagamavunon-1 (THPGV-1), are analogs of a curcumin metabolite, tetrahydrocurcumin, and a derivate of Pentagamavunon-0 (PGV-0) and Pentagamavunon-1 (PGV-1), respectively. THPGV-0 and THPGV-1 have been successfully synthesized and are investigated for their anticancer potency. Cytotoxic assays were performed toward several cancer cell lines to determine values of IC50. Assessing cytotoxicity on Vero normal cell line showed the selectivity of those compound. THPGV-1 showed highest cytotoxic activity in lymphoma Raji cells, a suspension cell line, with an IC50 of 180µM. Both THPGV-0 and THPGV-1 showed similar potencies on T47D breast cancer cell line with IC50 values of 250-270µM. Regardless their high selectivity, however, cytotoxic activities of THPGV-0 and THPGV-1 were lower compared to PGV-0 and PGV-1 on HeLa cervical, T47D breast, and WiDr colon cancer cell lines. Further study using different types of cancer cell lines and confirmation of cell viability by another assays and apoptosis detection may give more benefit.
Chemotherapy is the first-line treatment for triple-negative breast cancer (TNBC), yet toxicity and resistance effects have been the current problems. Curcumin,a natural compound, has been reported to exert anti-proliferative effects on various cancer cells, including breast carcinoma cells. However, the β-diketone moiety influences the stability of curcumin. Curcumin analogs, pentagamavunon-0 (PGV-0), and pentagamavunon-1 (PGV-1) were synthesized to improve the stability and activity of curcumin by modified the β-diketone moiety into mono-ketone pentanone. In this study, we evaluated the cytotoxicity, inhibition of cell cycle progression, and induction of apoptosis of curcumin and its analogs (PGV-0 and PGV-1) in murine triple-negative breast cancer 4T1 cell line. The cytotoxic evaluation was done by MTT assay, while apoptosis induction and cell cycle evaluation was performed by annexin V staining and detected by flow cytometry. Curcumin and its analogs, PGV-0, and PGV-1, significantly inhibit the viability of 4T1 breast cancer cells with an IC50 value of 34.34µg/mL, 13.76µg/mL and 38.21μg/mL, respectively. Apoptosis analysis with a dose of 10µg/mL and 15µg/mL in 4T1 breast cancer cells showed that curcumin and its analogs effectively induce apoptotic in a dose-dependent manner. In cell cycle analysis using a dose of 15µg/mL, curcumin inhibited the cell cycle progression in the S phase, whereas PGV-0 and PGV-1 inhibited the cell cycle in the G2/M phase. It could be concluded that curcumin analogs, PGV-0 and PGV-1, have higher potential to be developed as anti-cancer agents by inducing cell cycle arrest and apoptosis in triple-negative breast cancer.
Synthesis of Tetrahydrohexagamavunon-5 (THHGV-5) and Tetrahydrohexagamavunone-7 (THHGV-7) were prepared by catalytic hydrogenation reaction on Hexagamavunon-5 (HGV-5) and Hexagamavunone-7 (HGV-7) by using gas H 2 as source of hydrogen gas, Pd/C 10 % as metal catalyst and methanol as solvent at room temperature. According to previous study, Pd/C catalyst is more specific than other metal catalyst to reduce α,β-unsaturated double bond without reduction of its carbonyl functional group.
Tuberculosis (TB), in which caused by pathogenic bacteria, Mycobacterium tuberculosis, has become the major causes of death among all of infectious diseases. The increasing incidence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB
ABSTRAK
Tuberkulosis (TB) adalah penyakit yang disebabkan oleh infeksi Mycobacterium tuberculosis dan menjadi penyakit infeksi yang menyebabkan paling banyak kematian di dunia. Daruratnya penyakit TB dan meningkatnya kasus multidrug-resistant tuberculosis (MDR-TB) dan XDR-TB ini mendorong dilakukannya
Objective: The increasing incidence of multidrug-resistant tuberculosis (TB) has created a need to discover a new anti-TB drug candidates. The aim of this study was to screen extract and fractions of Tinospora crispa for activity against Mycobacterium tuberculosis H37Rv.Methods: The dried and pulverized T. crispa stem was extracted by maceration method using ethanol (96%). The anti-TB activity was carried out using mycobacteria growth indicator tube (MGIT) system and agar proportion method with Lowenstein–Jensen (LJ) medium.Result: The result of this study showed that ethanolic extract and fractions of T. Crispa did not exhibit anti-TB activity in the range of 100–1000 μg/ml with MGIT method, while with agar proportion method, there were M. tuberculosis colonies growth on the LJ containing 1000 μg/ml extract slants.Conclusion: The tested extract and fractions of T. crispa have no anti-TB activity against M. tuberculosis until 1000 μg/ml.
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