Taken together, these results demonstrated for the first time that Calebin-A suppressed adipocyte differentiation, prevented HFD-induced obesity, and improved hepatic steatosis, suggesting a novel application for the prevention and treatment of obesity and associated nonalcoholic fatty liver disease.
Calebin-A is a curcuminoid compound reported to be present in Curcuma longa rhizome. The current study was aimed to isolate and characterize calebin-A from Curcuma caesia rhizome and its production through biotransformation approach using endophytic fungus. C. caesia rhizomes of different ages were subjected to analysis in order to investigate the age at which maximum calebin-A content is present. HP-TLC profiles, HPLC retention times and mass spectrometry detector confirmed the occurrence of calebin-A in C. caesia rhizomes of 12 to 14 months of age but not in rhizomes younger to 12 months. Furthermore, an endophytic fungus strain, EPE-10 that was isolated from the medicinal plant C. caesia was identified as Ovatospora brasiliensis based on morphological and molecular characteristics. This strain O. brasiliensis was deposited to the culture collected centre, MTCC Chandigarh, India under the Budapest treaty and was designated with the Accession Number MTCC 25236. Biotransformation process was carried out at 37 ± 0.5 °C with shaking for 7 days after addition of 0.01% w/v curcumin. Extraction of biotransformed products was done by following partition method and the extracts obtained were analyzed using HPTLC, HPLC and LCMS. The data of the study suggested that O. brasiliensis MTCC 25236 was found to convert curcumin to calebin-A in a time dependant manner with optimum conversion at 48 h. Furthermore, O. brasiliensis MTCC 25236 was found to be positive for the Baeyer–Villiger monooxygenase (BVMOs) enzyme activity which could possibly be the mechanism of this bioconversion. The results of this study for the first time indicated that the endophytic fungus identified as O. brasiliensis MTCC 25236 isolated from the C. caesia rhizome could be a possible source for naturally producing calebin-A.
Background Type 2 diabetes mellitus (T2DM) is a major public health concern with growing prevalence with multiple debilitating complications. GlycaCare-II is a proprietary herbal formulation supplement for T2DM containing extracts of Cinnamomum cassia, Momordica charantia, Pterocarpus marsupium, Gymnema sylvestre, Salacia reticulata, Eugenia jambolana, and a bioavailability enhancer piperine from Piper nigrum. Objective The antihyperglycemic potential of GlycaCare-II was compared against metformin in a double-blind study. Design It was a randomized, two-arm design on prediabetic (N = 29; 12 in metformin and 17 in GlycaCare-II arm, respectively) and newly diagnosed diabetic (N = 40; 16 in metformin and 24 in GlycaCare-II) patients for 120 days. Outcome measures Changes in diabetic panel glycosylated hemoglobin (HbA1c), fasting blood sugar (FBS), and postprandial blood sugar (PBS) were the primary endpoints. Lipid profile, liver profile, thyroid-stimulating hormone, bilirubin and creatinine were the secondary endpoints. Result Twice a day treatment for 120 days with GlycaCare-II led to a statistically significant change in HbA1c (p < 0.001), FBS (p < 0.001), PBS (p < 0.001) on both prediabetic and newly diagnosed diabetic patients. GlycaCare-II showed a similar potential as metformin in the treatment of T2DM. In the prediabetic group, both GlycaCare-II and metformin were comparable for all the hyperglycemic index parameters. In the case of newly diagnosed diabetic patients, GlycaCare-II showed a significantly better reduction for PBS (p = 0.026) as compared to metformin, while all other parameters in the diabetic panel were comparable. No adverse events were reported throughout the trial period. Conclusion These results suggest that GlycaCare-II is effective in managing T2DM in both newly diagnosed diabetic and prediabetic patients.
The synthesis of Calebin-A (10a) and analogues (10b-d), which are minor but pharmacologically active components (<0.01% of the oleoresin) of curcuma longa, is described. This flexible synthesis is achieved under near neutral conditions in water/solvent biphasic medium at room temperature without involving any protecting groups.Key words Calebin-A, Curcuma longa, ferulic acid ester, phase-transfer catalyst (PTC), green synthesis Curcuma longa has been a traditional remedy for several disease conditions and is described extensively in Indian (Ayurvedic) and traditional Chinese medicine. Several active constituents have been isolated from this plant but prime among them are the curcuminoids. 1 The high popularity of curcuminoids and their pleiotropic activity have relegated to practically obscurity several minor compounds that occur in Curcuma longa, which have not been considered to merit any detailed study. 2 Park and Kim 3 first isolated and identified Calebin-A (10a) from Curcuma longa in 2001 through a tedious isolation. The isolation itself was performed by repeated normal column chromatography over silica gel followed by semipreparative HPLC. The content of Calebin-A (10a) is ca. 0.01% of the turmeric oleoresin. The structure of Calebin-A was characterized as an ester of ferulic acid, contrasting with the dynamic pair of ketoenol forms that characterize curcuminoid structures. Esters of ferulic acid are a ubiquitous structural type occurring in several diverse plant varieties. 4 Demethoxycalebin-A1 (10b) and demethoxycalebin-A2 (10c) have been isolated as an inseparable pair from Curcuma longa by Qiu and co-workers 5 in 2007, again through a laborious procedure using repeated chromatography over normal phase, reversed phase and preparative HPLC. The total content of isomeric demethoxycalebin-A1 (10b) and demethoxycalebin-A2 (10c) amounts to ca. 0.002% of the turmeric oleoresin. Calebin-A (10a) and demethoxycalebin-A1 (10b) protect PC12 rat pheocromocytoma and IMR-32 human neuroblastoma cells from β-amyloid(25-35) damage in in vitro models. 6
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