Polyketides are a large group of secondary metabolites that have notable variety in their structure and function. Polyketides exhibit a wide range of bioactivities such as antibacterial, antifungal, anticancer, antiviral, immune-suppressing, anti-cholesterol, and anti-inflammatory activity. Naturally, they are found in bacteria, fungi, plants, protists, insects, mollusks, and sponges. Streptomyces is a genus of Gram-positive bacteria that has a filamentous form like fungi. This genus is best known as one of the polyketides producers. Some examples of polyketides produced by Streptomyces are rapamycin, oleandomycin, actinorhodin, daunorubicin, and caprazamycin. Biosynthesis of polyketides involves a group of enzyme activities called polyketide synthases (PKSs). There are three types of PKSs (type I, type II, and type III) in Streptomyces responsible for producing polyketides. This paper focuses on the biosynthesis of polyketides in Streptomyces with three structurally-different types of PKSs.
Andrographis paniculata, Syzygium cumini, and Caesalpinia sappan are used as traditional medicines to treat diabetes mellitus. Therefore, this study aims to examine the antidiabetic effects and the acute toxicity of combined extract (1:1:1) of A. paniculata, S. cumini, and C. sappan (ASCE). The antidiabetic effect was tested using the rats model, induced by a high-fat diet and a double dose of streptozotocin injection of 35 mg/kg BW. Subsequently, diabetic rats in the experimental group were treated with 75 mg/kg BW and 150 mg/kg BW of ASCE, and those in the diabetic control group were treated with metformin 250 mg/kg BW. After seven days of treatment, fasting blood glucose (FBG), pancreatic β-cells numbers, and lipid profiles were used to analyze the antidiabetic effect. The results showed that the administration of 150 mg/kg BW ASCE significantly reduced FBG (p < 0.01), cholesterol levels (p < 0.05), LDL levels (p < 0.05), but not triglycerides, compared to diabetic control, this effect was comparable to metformin treatment. In addition, the pancreatic β-cells numbers were likely increased after ASCE treatment in a dose-dependent manner. The oral administration of a single dose of ASCE was safe up to 5000 mg/kg BW and did not result in any significant difference in body weight, relative organ weight, hematological and biochemical parameters compared with the control group. Therefore, it can be concluded that ASCE has a potential antidiabetic effect and can be safely developed as alternative medicine.
10 November 2020 in Advances in Pharmacological and Pharmaceutical Sciences
Introduction. Researchers usually use herbal combinations to explore and develop traditional medicine to obtain additional benefits in the treatment of diseases, including diabetes. This study aims to evaluate the hypoglycemic effect of the combination of Andrographis paniculata (Burm. f.) Wall ex Nees and Caesalpinia sappan Linn extract (APCSE) on diabetes-induced rats. There has not been sufficient research on this combination; however, single extract studies of these plants have been widely conducted. Materials and Methods. Male Sprague Dawley rats (160–200 g) were induced by injecting a low dose of streptozotocin (35 mg/kg BW) twice and fed with a high-fat diet containing 25% fat, whereas control animals received only standard feed. Rats were treated with APCSE at doses of 100 mg and 200 mg/kg BW for seven days and compared to the APE and CSE groups treated with the extract at 100 mg, respectively. For the control group, rats were treated with metformin with a dose of 250 mg/kg. The antihyperglycemic and antihyperlipidemic effects were determined by measuring blood glucose levels and lipid profiles (cholesterol, triglycerides, HDL, and LDL). To assess the impact of the extract on pancreatic and adipose tissue, the number of pancreatic beta cells and adipocytes was evaluated through histopathological and immunohistochemical study. Results and Discussion. In a nonfasting state, the blood glucose change in APCSE 200 mg was 18.65% and was significantly lower from the DM group. However, a single extract of APE and CSE showed lower fasting blood glucose levels compared to the combined extract. Lipid profiles show no significant differences in cholesterol levels between groups; however, all treatment groups, including metformin, showed higher triglyceride levels. The APE-treated group showed significantly lower HDL and LDL, whereas CSE only showed lower LDL. The β-cell number was significantly higher after treatment with single extract CSE. The CSE and the combined extract groups showed hyperplasia adipocytes. Conclusion. The combined extract of APCSE has a moderate antihyperglycemic effect; however, a single extract may have better potential than the combined extract.
During the course of our ongoing screening for novel biologically active secondary metabolites, the rare Actinobacterium, Nonomuraea sp. 1808210CR was found to produce five unprecedented β-carboline derivatives, nonocarbolines A–E (1–5). Their structures were elucidated from high-resolution mass spectrometry, 1D and 2D nuclear magnetic resonance spectroscopy, and the absolute configuration of 4 was determined by using the modified Mosher method. Nonocarboline B (2) displayed moderate antifungal activity against Mucor hiemalis, while nonocarboline D (4) exhibited significant cytotoxic activity against the human lung carcinoma cell line A-549 with the IC50 value of 1.7 µM.
The antidiabetic activity test through a mechanism of inhibition of α-glucosidase enzyme was studied against ethanol, n-hexane, ethyl acetate and n-butanol fractions of ethanol extract of Artocarpus altilis (Parkinson) Fosberg (Moraceae) leaves and four flavonoid compounds isolated from ethyl acetate extracts of A. altilis. Ethyl acetate fraction has strongest antidiabetic activity compared to ethanol, n-hexane, and n-butanol fractions with IC50values5.98,6.79, 440.18and14.42μg/mL, respectively. Four flavonoid compounds (1-(2,4-dihydroxyphenyl)-3-[8-hydroxy-2-methyl-2-(4-methyl-3-pentenyl)-2H-1-benzopyran-5-yl]-1-propanone (AC-31), 2-geranyl-2',3,4,4'-tetrahydroxy dihydrochalcone (AC-51), 8-geranyl-4',5,7-trihydroxyflavone (AC-33) andcyclocommunol (AA-3), have been isolated from ethylacetate fraction. AC-31 was the strongest antidiabetic compound compared to AC-51, AC-33 and cyclocommunolwithIC50values are 15.73, 24.41,49.49,and72.20μg/mL. Kineticstudies of AC-31 using Lineweaver-Burk method showed that inhibition mechanism of enzymeα-glucosidase was anon-competitivetype.
15 October 2016 in Research Journal of Medicinal Plant