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, 1 HNMR, 13 CNMR and Mass spectroscopy. Based on MTT assay PGB-0 decreased cells viability on MCF-7/HER2 cells with IC 50 value of 270µM 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.
Paracetamol is an analgesic-antipyretic compound derived from p-aminophenol. Though paracetamol has good efficacy and safety on consumption, parasetamol has hepatotoxic effect as its adverse drug reaction. 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxyphenol is one of p-aminophenol derivative that was already been determined in silico using molecular docking PLANTS method, and it was known that 4-[N-(4-hydroxyphenyl) carboxymidoyl]-2-methoxyphenol has analgesic effects more potent and has hepatotoxic adverse effect lower than paracetamol. 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxyphenol can be synthesized through reaction of p-aminophenol with vanillin under acid condition. The synthesized products were recrytalized, dried, and the purity was determined with melting point determination and Thin Layer Chromatography. The structure of pure crystals were elucidated using IR, 1 H-NMR, C-NMR, and Mass Spectroscopy. The analgesic evaluation was carried in vivo using writhing test method. The synthesized compound were divided into three dosage variations, 0,5; 1; and 2mol equivalent to 100mg/kgBB of paracetamol (reference drug). 4-[N-(4-hydroxyphenyl)carboxymidoyl]-2-methoxyphenol with 1mol dosage has analgesic activity better than paracetamol but the difference was not significant.
Synthesis and physicochemistry properties prediction of a potential anti-inflammatory agent, diacetyl pentagamavunon-1 (diacetyl PGV-1), has been done. The synthesis was using pentagamavunon-1 (PGV-1) (2,87x10-3 mole) and anhydride acetic acid (26x10-3 mole; 37x10-3 mole; 49x10-3 mole) as starting materials and NaOH ethanolic as a catalyst. The AM1 semiempirical quantum-chemical calculations using the computational chemistry approach was used to predict and compare the physicochemisty properties of diacetyl PGV-1 to PGV-1. Odorless, light-yellow powder has been obtained. The powder was 0.8512-0.9602 g (2.02 x10-3 - 2.22x10-3 mole; 70.4-77.4%) and the purity of the powder was 92.4%. The purity of the product has been examined by high performance liquid chromatography (HPLC), while the structure elucidation has been done using IR (Infra Red), 1H-NMR (Nuclear Magnetic Resonance) and MS (Mass Spectroscopy). The physicochemisty properties prediction showed that diacetyl PGV-1 was more hydrophobic than PGV-1. Keywords: Anti-inflammatory, PGV-1, diacetyl PGV-1, AM1
In the last decade, Indonesia intensifies the efforts to reduce pharmaceutical imports. One of the initiatives is establishing a paracetamol production facility to start operating in 2024. Kinetics study is needed as a basis to design the paracetamol reactor. This study investigated the optimal temperature, reactant mole ratio, and agitation speed in the reactor for paracetamol production. In this study, aqueous solution of para-aminophenol was reacted with acetic anhydride. The mole ratio of para-aminophenol to acetic anhydride was varied to 1:1, 1:1.2, 1:1.5, and 1:2 while the temperature was varied to 80 °C, 90 °C, and 110 °C. However, due to uncontrolled heat of the reaction and limitation of the mixture’s boiling point, the actual reaction temperatures were 86 °C, 90 °C, and 108 °C. In addition, the agitation speed of 250 RPM and 350 RPM were also studied. Thin layer chromatography (TLC) and densitometry were used to determine the concentration of paracetamol in the reacting mixture. The optimum temperature, reactant mole ratio, and agitation speed in this study were 108 °C, 1:1.5, and 350 RPM, respectively. In addition, a reaction performed under those operating parameters gave the reaction rate constant of 1.95 L mol-1 min-1.Keywords: acetic anhydride; kinetics; para-aminophenol; paracetamol; pharmaceutical industry A B S T R A KDalam sepuluh tahun terakhir ini, Indonesia bertekad mengurangi impor bahan baku farmasi. Salah satu upaya yang dilakukan adalah membangun fasilitas produksi parasetamol yang akan mulai beroperasi pada tahun 2024. Studi kinetika diperlukan sebagai dasar perancangan reaktor parasetamol. Oleh karena itu, penelitian ini mengkaji kondisi operasi optimal pada reaksi produksi parasetamol yang akan dibutuhkan sebagai dasar perancangan pabrik. Pada percobaan ini, para-aminofenol direaksikan dengan anhidrida asetat dengan media air. Rasio mol para-aminofenol terhadap asetat anhidrida divariasikan 1:1 1:1,2, 1:1,5, dan 1:2 sedangkan temperatur divariasikan 80 °C, 90 °C, dan 110 °C. Akan tetapi, karena panas reaksi yang tidak dikontrol dan batasan berupa titik didih dari campuran reaksi, temperatur aktual reaksi menjadi 86 °C, 90 °C, dan 108 °C. Selain itu, kecepatan putaran pengadukan juga divariasikan pada angka 250 RPM dan 350 RPM. Kromatografi lapis tipis (KLT) dan densitometri digunakan untuk menentukan konsentrasi parasetamol dalam campuran reaksi. Temperatur, rasio mol reaktan, dan kecepatan putaran pengadukan yang optimum pada penelitian ini masing-masing adalah 110 °C, 1:1,5, dan 350 RPM. Selain itu, reaksi yang dilakukan dengan kondisi operasi tersebut menghasilkan konstanta laju reaksi 1,95 L mol-1 menit-1.Kata kunci: anhidrida asetat, industri farmasi, kinetika, para-aminofenol, parasetamol
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