Background: Plant-phenolics and flavonoids, including gallic acid, quercetin and rutin, are considered as safe inhibitors for α-glucosidase. This study aimed to compare antioxidant and α-glucosidase inhibitory activities of gallic acid (GA), quercetin (QUE) and rutin (RUT).Materials and Methods: Pure compounds of GA, QUE, and RUT were used. Their antioxidant and inhibitory activity on α-glucosidase were investigated spectroscopically, including their kinetic analysis and interaction mechanism by docking simulation.Results: All the tested compounds (GA, QUE, and RUT) showed good antioxidant activity better than the standards ascorbic acid (AA) and butylated hydroxytoluene (BHT), with QUE showing the highest antioxidant activity based on 2,2-diphenyl1-picrylhydrazyl (DPPH) radical scavenging activity. Based on their reducing properties, the activities of the compounds follow the following order: AA > GA > BHT > QUE > RUT. Both GA and RUT induced a competitive type of inhibition, with activities stronger than acarbose (IC50 = 823 μg/mL), whereas QUE inhibited in a mixed type manner. The IC50 of GA, QUE, and RUT were 220.12, 65.52, and 224.55 μg/mL respectively. The results obtained from molecular docking indicate that all compounds have affinity in the active site pocket of α-glucosidase, with the hydrogen bond being the major force involved in each compound binding to the enzyme.Conclusion: In conclusion, QUE has better antioxidant and α-glucosidase inhibitory activity than GA and RUT. This work provides insights into the interactions between GA, QUE, and RUT and α-glucosidase.Keywords: docking, gallic acid, α-glucosidase, rutin, quercetin

Breast cancer stem cells (BCSCs) express high levels of the anti-apoptotic protein, survivin. This study aimed to discover a natural active compound with anti-cancer properties that targeted survivin in human breast cancer stem cells. From the seven examined compounds, andrographolide was selected as a lead compound through in silico molecular docking with survivin, caspase-9, and caspase-3. We found that the affinity between andrographolide and survivin is higher than that with caspase-9 and caspase-3. Human CD24-/CD44+ BCSCs were treated with andrographolide in vitro for 24 hours. The cytotoxic effect of andrographolide on BCSCs was compared to that on human mesenchymal stem cells (MSCs). The expression of survivin, caspase-9, and caspase-3 mRNA was analyzed using qRT-PCR, while Thr34-phosphorylated survivin and total survivin levels were determined using ELISA and Immunoblotting assay. Annexin-V/PI flow cytometry assays were performed to evaluate the apoptotic activity of andrographolide. Our results demonstrate that the CC50 of andrographolide in BCSCs was 0.32mM, whereas there was no cytotoxic effect in MSCs. Moreover, andrographolide decreased survivin and Thr34-phosphorylated survivin, thus inhibiting survivin activation and increasing survivin mRNA in BCSCs. The apoptotic activity of andrographolide was revealed by the increase of caspase-3 mRNA and protein, as well as the increase in both the early and late phases of apoptosis. In conclusion, andrographolide can be considered an anti-cancer compound that targets BCSCs due to its molecular interactions with survivin, caspase-9, and caspase-3, which induce apoptosis. We suggest that the binding of andrographolide to survivin is a critical aspect of the effect of andrographolide.

Diabetes mellitus is a disease that is quite common among the people. The causes of diabetes mellitus vary depending on the classification of this group of diseases. If diabetes mellitus is not handLed properly and correctly, there will be chronic hyperglycemia that causes oxidative stress, so patients will complain of some complications from diabetes mellitus that is actually caused by free radicals. Star anise (Illicium Verum) is one of the plants that are often used, one of which is as a spice in food. The star anise  has several compounds, one of which is flavonoid which is as an easily oxidized compound (antioxidant), so it is often used as a traditional medicine to treat many diseases. In several studies in vitro this star anise plant has also been proven to have antioxidant levels such as flavonoids and phenolic which are high enough so that it can be used as a source of exogenous antioxidants that can help endogenous antioxidants such as glutathione (GSH) to reduce free radicals that enter and remain keep body cells in normal condition. The study was carried out experimentally and conducted on rats in diabetes mellitus to see the effect of giving star anise extracts on glucose levels and blood levels of endogenous antioxidants (glutathione). Male rats with 2-3 months of age as many as 24 animals were divided into 6 groups, namely the negative control group (mice only given distilled water), diabetic rats without treatment group (positive control), diabetic rats treated with rootbose (positive control), and diabetic rats by treating the extract of star anise of 50, 100, and 150 mg/kg body weight of rats. This research was conducted for 7 days. GSH levels were measured on days 0 and 7. To analyze the differences in the average data of glucose and GSH, statistics were used. Results of the Wilcoxon test showed that there were significant differences (with p < 0.05) in blood sugar levels between the control group and the diabetic rats treated with star anise extract group. There was a significant decrease in blood sugar levels in diabetic rats given an extract of star anise. The greatest decrease in blood sugar levels occurred in the group of diabetic rats who were given an extract of star anise at 150 mg/kg bw. It is also known that there are difference in GSH levels between the control group and the diabetic rat group with the treatment of extract of star anise, but statistically the difference is not significant. GSH levels increased 0.03 µM/mL by administering an extract of star anise at 50 mg/kg bw.

Aterosklerosis adalah penyakit kardiovaskuler yang menempati urutan pertama penyebab mortalitas dan morbiditas global.  Penyakit ini ditandai dengan perubahan pada dinding pembuluh darah arteri yaitu terjadi penebalan dan kekakuan. Salah satu faktor penyebab terjadinya aterosklerosis adalah mengkonsumsi makanan berlemak dan tinggi kolesterol. Daun Binahong (Anredera cordifolia (Ten.)Steenis) dipercaya oleh masyarakat dapat menurunkan kadar kolesterol. Untuk mendapatkan zat dan bahan aktifnya maka daun binahong dibuat dalam bentuk ekstrak. Pada penelitian ini daun binahong diekstrak dalam etanol 96% dan untuk pengukuran kadar kolesterol total digunakan easy touch GCU. Penelitian ini menggunakan hewan coba tikus putih (Rattus norvegicus). Tikus dibagi menjadi 4 kelompok yaitu kelompok tikus hiperkolesterolemia tanpa perlakuan (kontrol), kelompok tikus hiperkolesterolemia dengan pemberian simvastatin (kontrol positif), kelompok tikus hiperkolesterolemia dengan pemberian ekstrak daun binahong (1.000 mg/kgbb dan 1.500 mg/kgbb).  Dari hasil uji statistik disimpulkan bahwa pemberian ekstrak daun binahong 1.500 mg/kgbb memiliki efek dalam penurunan kadar kolesterol total darah secara signifikan pada hari ke-14.

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