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Synthesis of 3-carbethoxy-4(3’-chloro-4’-hydroxy) phenyl-but-3-en-2-one and its cytotoxicity evaluation against cancer cell carrying mutant p53 Julianus, Jeffry; Mustofa; Jumina
Indonesian Journal of Pharmacology and Therapy Vol 2 No 1 (2021)
Publisher : Faculty of Medicine, Public Health, and Nursing Universitas Gadjah Mada and Indonesian Pharmacologist Association or Ikatan Farmakologi Indonesia (IKAFARI)

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22146/ijpther.1211

Abstract

Overexpression of mutant p53 in cancer cell inactivates the p53 pathways to execute apoptosis and cell cycle arrest. This study aimed to synthesize new kardiena derivative compound, 3-carbethoxy-4(3’-chloro-4’-hydroxy)phenyl-but-3-en-2-one, to reactivate the p53 pathways to execute apoptosis and cell cycle arrest. Characterization of the synthetic compound employing melting point, IR, EI-MS, 1H-NMR, and 13C-NMR spectra revealed 3-carbethoxy-4(3’-chloro-4’-hydroxy)phenyl-but-3-en-2-one was successfully synthesized from 3-chloro-4-hydroxybenzaldehyde and ethyl acetoacetate using dimethylamine as a catalyst. This compound had antiproliferative activity against the WiDr cells which carried mutant p53. Its antiproliferative activity was better than 5’-FU as a reference standard to treat colon cancer. Increasing WiDr cell accumulation in the G2-M phase, the active form of caspase-3, and inducing apoptosis demonstrated the ability of 3-carbethoxy-4(3’-chloro-4’-hydroxy)phenyl-but-3-en-2-one to reactivate p53 pathways to execute apoptosis and cell cycle arrest in cancer cells carrying mutant p53.
Molecular docking study of Indonesian phytochemicals as inhibitor of 6-HB formation by binding to HR1 subunit of SARSCOV-2 S2 protein Julianus, Jeffry; Phebe Hendra; Maywan Hariono; Nico Frederick; Satrio Ardyantoro; Mustofa; Jumina
Indonesian Journal of Pharmacology and Therapy Vol 2 No 3 (2021): Special Issue: COVID-19
Publisher : Faculty of Medicine, Public Health, and Nursing Universitas Gadjah Mada and Indonesian Pharmacologist Association or Ikatan Farmakologi Indonesia (IKAFARI)

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.22146/ijpther.2392

Abstract

Coronavirus disease 2019 (COVID-19) is still as global pandemic. No officially drugs to treat COVID-19 are available until now. Increasing number of patients and deaths trigger new antiCOVID-19 discovery efforts. In this study, we have conducted in silico screening employing molecular docking for Indonesian phytochemicals. Docking process was performed by employing AutoDock4 software on crystal structure 6VSB. Based on molecular docking results, several compounds had potential as antiCOVID-19 drugs, such as β-carotene, veramiline, ecliptalbine, betulinic acid, and lupeol. β-carotene was the most potential compound to treat COVID-19.