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All Journal VALENSI Chemistry Indonesian Journal of Chemical Research Jurnal Kartika Kimia
Hermawati, Elvira
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Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Chemistry Education Engineering Environmental Science

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Synthesis and Biological Evaluation of N'-Arylidene-4-Hydroxybenzohydrazides against α-Glucosidase Enzyme Danova, Ade; Hermawati, Elvira; Chavasiri, Warinthorn
Jurnal Kartika Kimia Vol 6 No 2 (2023): Jurnal Kartika Kimia
Publisher : Department of Chemistry, Faculty of Sciences and Informatics, University of Jenderal Achmad Yani

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.26874/jkk.v6i2.210

Abstract

Hydrazides have been reported to have a broad spectrum of bioactivities, such as anticancer, antifungal, antibacterial, and antidiabetic. Thus, our work aimed to synthesize N'-arylidene-4-hydroxybenzohydrazides and investigate their α-glucosidase inhibition. Three compounds (AD-H1-3) were synthesized with a yield of product from 33 to 65% and then characterized using 1H-and 13C-NMR spectroscopy. The in vitro α-glucosidase inhibition demonstrated that AD-H2 possessing two hydroxy groups on arylidene moiety showed the best inhibitory activity against α-glucosidase enzyme with an IC50 value of 14.4 µM compared with acarbose as a positive control with IC50 value of 93.6 µM. Thus, AD-H2 could be a candidate as a lead compound for antidiabetics.
Synthesis, Evaluation, and Molecular Docking Study of 4-Monoacyl Resorcinol Against Tyrosinase Enzyme Danova, Ade; Maulana, Yusuf Eka; Hermawati, Elvira; Chavasiri, Warinthorn
Indonesian Journal of Chemical Research Vol 11 No 2 (2023): Edition for September 2023
Publisher : Jurusan Kimia, Fakultas Matematika dan Ilmu Pengetahuan Alam, Universitas Pattimura

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.30598//ijcr.2023.11-nov

Abstract

Tyrosinase is a crucial enzyme in melanin production to protect the skin from ultraviolet, leading to skin cancers. This study synthesized eight compounds of acyl resorcinol with long-chain carbon (1-8) and structurally elucidated by 1H and 13C NMR. The in vitro evaluation of eight synthesized compounds against tyrosinase enzyme showed that 4-heptanoyl resorcinol (6) exhibited high inhibitory activity compared with the kojic acid as standard. In addition, the molecular docking study demonstrated that 6 showed lower binding energy (-7.3 kcal/mol) than kojic acid (-6.9 kcal/mol) and possessed interaction with crucial residues in the active site.
Garciniaxanthone E and 12b-Hydroxy-des-D-garcigerrin A from The Tree Bark Garcinia dulcis and their Inhibitory Properties against Receptor Tyrosine Kinases Kurniadewi, Fera; Aqilah, Amadita Shafa; Kartika, Irma Ratna; Nurjayadi, Muktiningsih; Hermawati, Elvira; Danova, Ade
Jurnal Kimia Valensi Jurnal Kimia VALENSI, Volume 10, No. 1, May 2024
Publisher : Syarif Hidayatullah State Islamic University

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.15408/jkv.v10i1.38159

Abstract

Two xanthone derivatives, garciniaxanthone E (1) and 12b-Hydroxy-des-D-garcigerrin A (2) have been isolated from ethyl acetate extract of the tree bark of Garcinia dulcis. The Ultraviolet (UV), Infrared (IR), Nuclear Magnetic Resonance (NMR), and Mass Spectrometry (MS) data analysis elucidated the structure of the isolated compounds. This study represents the first evaluation of compounds 1 and 2 in terms of their efficacy against receptor tyrosine kinases. The results showed that compound 1 exhibited weak activity with 12% inhibition against Insulin Receptor (InsR), while compound 2 showed moderate activity with 29% inhibition against epidermal growth factor receptor (EGFR). A molecular docking study targeting EGFR-TK suggests that the hydroxyl group at C-4 on compound 2 can be demolished to raise the inhibitory activity in future research.
Co-Authors Ade Danova Aqilah, Amadita Shafa Chavasiri, Warinthorn Kartika, Irma Ratna Kurniadewi, Fera Maulana, Yusuf Eka Muktiningsih Nurjayadi