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All Journal Indonesian Journal of Chemistry Jurnal Biosense
Nurlaili Nurlaili
Akademi Kesehatan Kartini Batam
Agriculture, Biological Sciences & Forestry Biochemistry, Genetics & Molecular Biology Chemical Engineering, Chemistry & Bioengineering Chemistry Immunology & microbiology Medicine & Pharmacology Public Health

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Microwave Assisted Synthesis and Evaluation of Toxicity and Antioxidant Activity of Pyrazoline Derivatives Jasril Jasril; Hilwan Yuda Teruna; Aisyah Aisyah; Nurlaili Nurlaili; Rudi Hendra
Indonesian Journal of Chemistry Vol 19, No 3 (2019)
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (281.72 KB) | DOI: 10.22146/ijc.34285

Abstract

Four pyrazoline analogues, 3-(4-methoxyphenyl)-5-naphthalene-1-yl-1-phenyl-4,5-dihydro-pyrazole (3), 3-(4-methoxyphenyl)-5-naphthalene-1-yl-4,5-dihydro-1H-pyrazole (4), 3-(2-methoxyphenyl)-5-naphthalene-1-yl-1-phenyl-4,5-dihydro-pyrazole (5) and 3-(2-methoxyphenyl)-5-naphthalene-1-yl-4,5-dihydro-1H-pyrazole (6) were synthesized via intermolecular cyclization between substituted chalcones and hydrazine derivatives. The compounds were synthesized in two steps. In the first step, the chalcones were synthesized by Claisen-Schmidt reaction. In the second step, they were cyclized with some hydrazine derivatives to form pyrazolines by using glacial acetic acid as a catalyst and assisted by microwave irradiation. The toxicity analysis showed that compound 1 and 2 were toxic with LC50 values of 11.47 and 0.97 μg/mL, respectively. Furthermore, only compound 6 showed high antioxidant activity by using DPPH with an IC50 value of 4.47 μg/mL.
PENAMBATAN MOLEKUL SENYAWA VOLATIL EKSTRAK DIKLOROMETANA SAMBILOTO TERHADAP JALUR PENSINYAL EPIDERMAL GROWTH FACTOR RECEPTOR: Penambatan Molekul Senyawa Volatil Ekstrak Diklorometana Sambiloto Terhadap Onkoprotein Human Epidermal Growth Factor Receptor Muhammad Faisal; Nurlaili Nurlaili; Potchanapond Graidist; Varomyalin Tipmanee
JURNAL BIOSENSE Vol 5 No 01 (2022): Edisi Juni 2022
Publisher : Program Studi Biologi, Fakultas Matematika dan Ilmu Pengetahuan Alam, Universitas PGRI Banyuwangi, Jalan Ikan Tongkol No 01, Telp (0333) 421593, 428592 Banyuwangi 68416

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (298.581 KB) | DOI: 10.36526/biosense.v5i01.1948

Abstract

EGFR oncoprotein has been commonly studied in combating cell cancer development. However, until this moment the EGFR inhibitors were reported to cause other health issues. Plant extracts are trusted as the potential inhibitor of EGFR expression level without affect our health. We previously observed seventeen volatile compounds in the dichloromethane extract of Andrographis paniculata. Our objective was to analyze the interaction of volatile compounds from the dichloromethane extract of Andrographis paniculata on human EGFR pathway. In silico technique with ligand-receptor molecular docking was used in this study. The structure of volatile compounds was set as the ligands. EGFR, PIK3CA, KRAS-GTP, BRAF V600E, and AKT protein structures were assigned as the receptors. PyRx and Biovia Discovery Studio were used in this docking study. Drug-likeness and lead-likeness properties were appraised by SwissADME and Pre-ADME/Tox web tools. Beta-amyrin and stigmasterol showed the highest binding affinity to EGFR oncoproteins. PIK3CA, AKT, and KRAS-GTP, BRAF V600E was bound to beta-amyrin and stigmasterol, respectively. Those compounds structurally showed drug-likeness and non-mutagenic. Briefly, beta-amyrin and stigmasterol will be potentially used as the inhibitors of selected oncoproteins. In vitro technique and animal model are suggested to be performed to validate the mutagenic mechanisms of beta-amyrin and stigmasterol
Co-Authors Aisyah Aisyah Hilwan Yuda Teruna Jasril Jasril Muhammad Faisal Potchanapond Graidist Rudi Hendra Varomyalin Tipmanee