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SYNTHESIS AND CYTOTOXIC ACTIVITY OF 2,5-BIS(4-BORONIC ACID)BENZYLIDINE CYCLOPENTANONE ON HER2 OVEREXPRESSED-CANCER CELLS Rohmad Yudi Utomo; Herwandhani Putri; Pudjono Pudjono; Ratna Asmah Susidarti; Riris Istighfari Jenie; Edy Meiyanto
Indonesian Journal of Pharmacy Vol 28 No 2, 2017
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (949.546 KB) | DOI: 10.14499/indonesianjpharm28iss2pp74

Abstract

Development of chemotherapeutic agent and boron carrying pharmaceutical based on HER2 specific targeted is important due to its role in enhancing cancer progression. The purpose of this study is to synthesize curcumin analogue, namely Pentagamaboron-0 (PGB-0) or 2,5-bis(4-boronic acid)benzylidine cyclopentanone, and to explore the cytotoxic activity on HER2 overexpressed-cancer cells. MCF-7/HER2 was used as a model of HER2 overexpressed-cancer cells and NIH3T3 as normal cells. PGB-0 bound to ATP binding site of HER2 and EGFR based on molecular docking study. PGB-0 was synthesized resulting in 33% yield and was confirmed by IR, 1HNMR, 13CNMR and Mass spectroscopy. Based on MTT assay PGB-0 decreased cells viability on MCF-7/HER2 cells with IC50 value of 270 µM but performed no effect on NIH3T3 cells. Cell cycle analysis revealed that PGB-0 increased sub-G1 accumulation. PGB-0 decreased HER2 expression in a dose-dependent manner. We conclude that the new compound PGB-0 inhibits cell growth through cell death induction and decreased HER2 expression. Thus, PGB-0 is potential to be developed as a chemotherapeutic agent and boron carrying pharmaceutical targeted on the HER2 receptor.
TOKSISITAS AKUT EKSTRAK ETANOLIK BIJI BUAH PINANG (Areca catechu L.) TERHADAP TIKUS JANTAN GALUR SPRAGUE DAWLEY Sri Handayani; Edy Meiyanto; Riris Istighfari Jenie; Ratna Asmah Susidarti
Jurnal Kimia Terapan Indonesia Vol 14, No 2 (2012)
Publisher : Research Center for Chemistry - LIPI

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (548.977 KB) | DOI: 10.14203/jkti.v14i2.338

Abstract

Ekstrak etanolik biji buah pinang (Areca catechu L.) memperlihatkan aktivitas penghambatan proliferasi selkanker payudara T47D dan MCF-7. Tikus (Rattus norvegicus) jantan galur Sprague Dawley usia 8 minggu dibagidalam lima kelompok, yaitu empat kelompok perlakuan dan satu kelompok kontrol pelarut CMC-Na 5%. Pemejanandosis tunggal peroral dilakukan terhadap subjek uji dengan variasi dosis ekstrak etanolik biji pinang mulai dari dosisyang paling aman hingga dosis tertinggi yang diharapkan toksik pada semua hewan uji (0,1; 0,72; 5,36 dan 10gram/kg berat badan).  Pengamatan dilakukan selama 24 jam terhadap gejala-gejala toksik, wujud dan mekanismeefek  toksik  maupun  patologi  organ  vital.  Pengamatan  mikroskopis  berupa  histopatologi  beberapa  organ  vitaldilakukan dengan pengecatan Hematoxillen&Eosin (H&E). Hasil uji menunjukan bahwa semua kelompok dosisperlakuan tidak mengalami gejala toksik, sama halnya dengan kelompok kontrol. Pemberian dosis tunggal ekstraketanolik biji pinang tidak menimbulkan kematian pada subjek uji, bahkan pada dosis tertinggi sekalipun. Oleh karenaitu  pengamatan  dilanjutkan  hingga  14  hari.  Pada  hari  ke-15  dilakukan  pembedahan  pada  semua  subjek  uji.Pengamatan  mikroskopis  menunjukkan  tidak  ada  perubahan  histopatologis  yang  berarti  pada  seluruh  kelompokperlakuan. Hasil uji ini menambah dasar keamanan penggunaan ekstrak etanolik biji pinang dalam pengembangannyasebagai agen terapi alternatif.  Kata kunci:  Ekstrak etanolik,  Areca catechu, toksisitas akut, tikus
Antioxidant and Anticancer Activity of Dillenia serrata Thunb Ethanol Extract Against MCF-7 Breast Cancer Cell Line Rahmawati Rahmawati; Zulkifli Zulkifli; Tri Rini Nuringtyas; Riris Istighfari Jenie; Laurentius Hartanto Nugroho
Indonesian Journal of Cancer Chemoprevention Vol 13, No 3 (2022)
Publisher : Indonesian Society for Cancer Chemoprevention

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.14499/indonesianjcanchemoprev13iss3pp175-183

Abstract

Women’s breast cancer incidence rate in Indonesia ranks number one with 12 per 100,000 cases, with luminal A as the dominant subtype. Currently, chemotherapeutic agents have limitations that lead to inefficiencies in therapy, therefore it is necessary to develop more effective and efficient chemopreventive agents. Plant secondary metabolites can provide pharmacological effects that can be used as chemoprevention agents. Secondary metabolites of D. serrata may have pharmacological effects as antioxidants and cytotoxic. This study aims to determine the antioxidant properties and cytotoxic activity of D. serrata ethanolic extract on the MCF-7 breast cancer cell line. The leaves of D. serrata were macerated, while the bark and root samples were refluxed with 96% ethanol as solvent. All extracts were evaporated with a rotary evaporator. Qualitative evaluation of the phytochemical content of leaf ethanolic extract, bark ethanolic extract, and root ethanolic extract was done using the standard tube test method. The antioxidant assay was carried out using the DPPH. The cytotoxic activity was determined in vitro using an MTT assay against the MCF-7 cell line with a series of concentrations from 12.5–400 μg/mL. Doxorubicin was the positive control treated at a 3.125–100 μg/mL concentration. The antioxidant activity showed that leaf extract had the highest antioxidant activity, followed by root and bark extract, with IC50 values of 95.66, 270.5, and 335.96 ppm, respectively. Leaf ethanolic extract and root ethanolic extract’s cytotoxic ability is considered moderate cytotoxic with IC50 values of 493.17 and 229.82 μg/mL, respectively. Amongst the ethanolic extract from the leaf, bark, and root of D. serrata, the leaf ethanolic extract has the best anti-oxidant activity and the bark ethanolic extract was the most cytotoxic one against MCF-7 cells.Keywords: Antioxidant, Cytotoxic, Dillenia serrata, MCF-7.