Several studies have shown that pure compounds from west sumatera medicinal plants have beneficial therapeutic effects so that they are potential candidates for active pharmaceutical ingredients (API). Andalas Sitawa Fitolab has been able to produce 10 pure isolates. The development of a new drug candidate requires an in silico study to predict physicochemical properties, potential target, and toxic properties. The purpose of this study was to initially screen the structure of candidates to predict the potential the compound as an API by using big data and machine learning. The chemical structure were analyzed using software and servers. The Software used was Marvin Sketch, QSAR Toolbox, Swiss Potential Target and ChemBioDraw. Results showed that log P of compounds revealed in a range of -0.54 to 4.64, Polar Surface Area (PSA) in range of 20.23 to 315.21. Asiaticoside did not meet Lipinski's rules. Compounds with high potential hazard were catechin, curcumin, andrographolide, asiaticoside deoxyelephantopin, ethylmethoxycinnamate, alpha-mangostin and piperine. The compounds such as curcumin, alpha mangostin, plumbagin, and piperine were predicted to have spesific target proteins. This study concluded that asiaticoside compounds have a high potential hazard, if it was developed as an API.Keywords: analysis of physical-chemical properties, in silico, pure isolate, toxicology
Objective: The aim of this study was to investigate in vitro anti-inflammatory activity of tinocrisposide using lipopolysaccharides (LPS)-stimulated RAW 264.7 macrophage cells. Tinocrisposide is a furano diterpene glycoside that was isolated in our previous study from Tinospora crispa.Methods: Anti-inflammatory effect was quantified spectrometrically using Griess method by measuring nitric oxide (NO) production after the addition of Griess reagent.Results: The sample concentrations of 1, 5, 25, 50, and 100 μM and 100 μM of dexamethasone (positive control) have been tested against the LPS-stimulated RAW 264.7 cells, and the results showed NO level production of 39.23, 34.00, 28.9, 20.25, 16.3, and 13.68 μM, respectively, and the inhibition level of 22.67, 33.00, 43.03, 60.10, 68.00, and 73%, respectively.Conclusions: From the study, it could be concluded that tinocrisposide was able to inhibit the formation of NO in the LPS-stimulated RAW 264.7 cells in concentration activity-dependent manner, with half-maximal inhibition concentration 46.92 μM. It can be developed as anti-inflammatory candidate drug because NO is a reactive nitrogen species which is produced by NO synthase. The production of NO has been established as a mediator in inflammatory diseases.
One of the plants that can be used as traditional medicine is mahogany (Sweitenia mahagoni). The presence of flavonoid compounds in mahogany seeds is suspected as a compound that serves to inhibit bacterial growth. One of the antibacterial effects is to treat diarrhea diseases caused by Shigella dysenteriae. Diarrhea is infectious intestinal disease a public health problem in developing countries. The aim of this research is to know and measure the inhibition zone of ethanol extract of mahogany seed to the growth of Shigella dysenteriae bacteria with concentration 25%, 50%, 75%, 100%. This research is a descriptive study in vitro using disc method. The result of the research has found that the average inhibition zone diameter at 25%, 50%, 75%, 100% concentration is 6mm, 8mm, 8.33mm, 10.33mm. Negative controls do not provide inhibition and positive control yields an average diameter of 21.33 mm. Based on the above results, it can be concluded mahogany seed extract provides resistance to Shigella dysenteriae.
Objective: The aim of this study is to investigate the antihyperglycemic activity of tinocrisposide by stimulating 3T3-L1 adipocyte cell differentiation. Tinocrisposide is a furanoditerpene glycoside that was isolated from Tinospora crispa (Menispermaceae).Methods: Adipocyte cell differentiation activity of tinocrisposide in interval concentrations of 50, 25, 12.5, and 6.25 μg/ml has been investigated on 3T3-L1 cell line using insulin of 1 μg/ml as a positive and Dulbecco’s modified Eagle media (DMEM) as a negative control group. The effect of tinocrisposide was quantified with oil red O staining method by measuring an absorbance of lipid solution in isopropanol at a wavelength (λ) of 520 nm.Results: Tinocrisposide in the concentrations of 50, 25, 12.5, and 6.25 μg/ml insulin of 1 μg/ml and DMEM groups showed absorbance value of 0.7669, 0.7253, 0.6563, 0.6481, 0.954, and 0.2653, respectively. It was found that there was a significant difference statistically in lipid droplets accumulation among all groups (p<0.05) and tinocrisposide at a concentration of 50 μg/ml showed the highest lipid droplets accumulation in 3T3-L1 adipocyte cells.Conclusion: From the study, it could be concluded that tinocrisposide was able to stimulate the differentiation of adipocyte cell and had antihyperglycemic activity.
Kulit buah G. Mangostana kaya akan senyawa antioksidan yang dapat menghambat radikal bebas. Terdapat hubungan antara pemanasan dan aktivitas antioksidan suatu bahan alam, dikarenakan pengaruhnya terhadap komposisi senyawa bioaktif antioksidan. Tujuan penelitian ini adalah untuk melihat pengaruh suhu pengeringan terhadap aktivitas antioksidan kulit buah G. Mangostana. Pengeringan dilakukan pada suhu 30, 60 dan 900C selama 72 jam. Pengukuran aktivitas antioksidan dilakukan dengan metode DPPH dan hasil pengamatan dianalisis menggunakan ANOVA dua arah. Hasil penelitian menunjukkan bahwa suhu pengeringan berpengaruh nyata terhadap aktivitas antioksidan kulit buah G. Mangostana (P < 0,05). Kulit buah G. Mangostana perlakuan terbaik adalah pengeringan pada suhu 300C. Dengan nilai IC50 20,349 µg/mL.
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