Two new flavonoids named castilliferol 1 and castillicetin 2, as well as a known compound, isochlorogenic acid 3, were isolated from the whole plant of Centella asiatica. Isolates 1 and 2 exhibited good antioxidant activity using 2,2-diphenyl-1-picryl hydrazyl radical solution with IC(50) values of 23.10 and 13.30, respectively. The structures of these isolates were determined by analytical and spectral data, including 1-D and 2-D NMR spectra.
A sensitive, rapid, simple, and accurate high performance thin layer chromatographic method has been developed to standardize the bark of Grewia tiliaefolia Vahl. (Family: Tiliaceae) using betulin as an analytical marker. Chloroform extracts of bark from five different sources were used for HPTLC on silica gel with toluene-ethyl acetate, 90 + 10 v/v, as mobile phase. Under these conditions, the Rf of betulin was 0.22. The calibration plot was linear in the range of 1000 ng to 1800 ng of betulin and the correlation coefficient, 0.999, was indicative of good linear dependence of peak area on concentration. The mean assay of betulin was 2.596 +/- 0.594 mg g(-1) of bark. The method permits reliable quantification of betulin and good resolution and separation of betulin from other constituents of Grewia tiliaefolia. Recovery values from 96.09 to 98.87% showed that the reliability and reproducibility of the method were excellent. The proposed HPTLC method for quantitative monitoring of betulin in Grewia tiliaefolia can be used for routine quality testing.
We can conclude that isolated 5-hydroxy-1-methylpiperidin-2-one from T. involucrata L. has potent antihistamine agent on histamine-induced guinea pig.
Background Antioxidant and antihistamine agents from Barleria noctiflora L.f. as natural source due to the existing modern medicine give various adverse effects to overcome these problems with natural products. MethodsB. noctiflora leaves extract was fractionated with column chromatography; the homogenized fractions were monitored with thin layer chromatography (TLC) and characterized by using UV-visible, FT-IR, 1H NMR, 13C NMR and mass spectrometry spectral studies. The volatile phytoconstituents of B. noctiflora extract were analysed by gas chromatography-mass spectrometry. Phytoconstituents from B. noctiflora leaves extract were screened for their antioxidant and antihistamine potential in vitro (2,2-diphenyl-1-picrylhydrazyl radical scavenging activity, 2,2'-azinobis-3-ethylbenzothiozoline-6-sulfonic acid radical decolouration assay, nitric oxide radical scavenging activity, superoxide radical scavenging activity and hydrogen peroxide radical scavenging activity) and in silico (molecular docking), respectively. Results Antioxidant and antihistamine barlerinoside has been isolated and characterized from the leaves of B. noctiflora L.f. Barlerinoside revealed their free-radical scavenging ability on OH-, OH•, NO-, O2- and H2O2 radicals and found high percentage inhibition against OH- radical at the IC50 value of 50.45±2.52 µg. The methanol (MeOH) extract of B. noctiflora leaves contains cyclotene; N,N-dimethylglycine; tetrahydrocyclopenta [1,3] dioxin-4-one; phenol, 2-methoxy-; benzofuran, 2-methyl-; 1,4:3,6-dianhydro-α-d-glucopyranose; 2-methoxy-4-vinylphenol; 1,3;2,5-dimethylene-l-rhamnitol; levoglucosan and bicyclo[2.2.2]oct-7-ene-2,5-dione as being the major compounds. Among phytoconstituents present in the extract, the hexestrol; 1,2-benzenedicarboxylic acid, bis(2-methylpropyl) ester; 1-(3,6,6-trimethyl-1,6,7,7a-tetrahydrocyclopenta[c]pyran-1-yl) ethanone; megastigmatrienone; furan interacted with histamine H1 receptor and bind at GLU-177 and ASP-178 with high binding energy score -13.95, -13.41, -12.56, -12.03, and -11.72 kcal/mol, respectively, and the expected hydrolysed products of compound-1a and compound-1b from barlerinoside showed -8.91 and -8.68 kcal/mol binding energy against the histamine H1 receptor. This showed that the active ligands exactly bind with active binding site of the protein. ConclusionsWe can conclude that isolated barlerinoside from B. noctflora L.f. has potent antioxidant activity against synthetic free radicals and antihistamine activity against histamine H1 receptor.
Research background. Obesity increases mortality and morbidity due to its impact on type-2 diabetes, cardiovascular and gastrointestinal diseases, arthritis, and certain cancers. The epidemic of over mass and obesity requires constant endeavor research for improved therapies without undesirable side effects. Therefore, exploring the anti-obesity phytochemicals from food sources is essential. Most pharmacological studies of the anti-obesity potential of Capsicum annuum have been directed with capsaicin and very few with capsanthin. However, these studies utilized uncoated capsaicin and capsanthin. This study was directed to compare the anti-obesity effects of enteric-coated capsaicin and capsanthin in a high-fat diet-induced animal model. Experimental approach. In the current study, we investigated the anti-obesity properties of capsanthin-enriched extract pellets and capsaicin pellets derived from red chili fruit (Capsicum annuum) on high-fat diet (HFD)-induced C57BL/6J obese mice. First, the animals were provided with HFD to induce their obesity. Then, oral supplementation of the test items was provided. The food intake, body mass, and obesity, as well as the clinical biomarkers, were assessed. Results and conclusions. The mice fed with HFD were observed to gain body mass and white adipose tissue mass compared to the mice that consumed a normal diet. The oral administration of capsanthin-enriched extract pellets and capsaicin pellets significantly reduced the body mass gain. Capsanthin-enriched extract pellets and capsaicin pellets have a statistically significant (p<0.05) impact on obesity biomarkers by increasing adiponectin and decreasing leptin, free fatty acids, and insulin levels relative to HFD control. There was no change in the liver mass in all groups, but there was a significant decrease in white adipose tissues. Inguinal adipose tissue reduced by 37.0 % and epididymal adipose tissue reduced by 43.64 % after treatment with capsanthin-enriched extract pellets. These results suggest that capsanthin-enriched extract pellets and capsaicin pellets may be useful in combating metabolic diseases, including obesity, without adverse effects. Novelty and scientific contribution. We increased the content of capsanthin greater than 50 % in capsanthin-enriched extract crystals and enhanced the room temperature stability for more than one year by converting the crystals into capsanthin-enriched extract pellets. This study breaks new ground by examining the potential of capsanthin >50 % in the management of obesity for the first time.
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