| Autor: |
Utomo, Rohmad Yudi, Wulandari, Febri, Novitasari, Dhania, Lestari, Beni, Susidarti, Ratna Asmah, Jenie, Riris Istighfari, Kato, Jun-ya, Sardjiman, Sardjiman, Meiyanto, Edy |
| Předmět: |
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| Zdroj: |
Advanced Pharmaceutical Bulletin; 2022, Vol. 12 Issue 3, p603-612, 10p |
| Abstrakt: |
Purpose: This study aimed to challenge the anticancer potency of pentagamavunone-1 (PGV-1) and obtain a new compound (Chemoprevention-Curcumin Analog 1.1, CCA-1.1) withimproved chemical and pharmacological properties.Methods: CCA-1.1 was prepared by changing the ketone group of PGV-1 into a hydroxylgroup with NaBH4 as the reducing agent. The product was purified under preparative layerchromatography and confirmed with HPLC to show about 93% purity. It was tested for itssolubility, stability, and cytotoxic activities on several cancer cells. The structure of the productwas characterized using 1HNMR, 13C-NMR, FT-IR, and HR-mass spectroscopy.Results: Molecular docking analysis showed that CCA-1.1 performed similar or better interactionto NF-κB pathway-related signaling proteins (HER2, EGFR, IKK, ER-alpha, and ER-beta) andreactive oxygen species (ROS) metabolic enzymes (NQO1, NQO2, GSTP1, AKC1R1, andGLO1) compared with PGV-1, indicating that CCA-1.1 exhibits the same or better anticanceractivity than PGV-1. CCA-1.1 also showed better solubility and stability than PGV-1 in aqueoussolution at pH 1.0–7.4 under light exposure at room temperature. The cytotoxic activities ofCCA-1.1 against several (10) cancer cell lines revealed the same or better potency than PGV-1.Conclusion: In conclusion, CCA-1.1 performs better chemical and anticancer properties thanPGV-1 and shows promise as an anticancer agent with high selectivity. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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