Purification and characterization of pure curcumin, desmethoxycurcumin, and bisdemethoxycurcumin from North-East India Lakadong turmeric (Curcuma longa).

Lakadong turmeric has been outlined for its high content of curcuminoids across the globe. Three significant molecular markers are widely present in turmeric viz, curcumin, desmethoxycurcumin, and bisdemethoxycurcumin, and they are present very high amount in Lakadong turmeric. Curcuminoids have been reported for structural and spectrum similarity of 3 to 4 nm (432, 434, and 436 nm, respectively). Current purification methods are based on recrystallisation where it is difficult to get highly pure material and preparative methods associated with tedious separation with high cost. Lakadong turmeric has not been explored commercially since long time. No reports are available in the literature with highly pure reference materials with in-depth characterization data and purity assessment. Curcumin, desmethoxycurcumin, and bisdemethoxycurcumin were characterized using different analytical techniques viz, UV-Visible Spectroscopy, Fourier Transform Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Proton Nuclear Magnetic Resonance (1HNMR), Carbon-13 Nuclear Magnetic Resonance (13CNMR), High-Resolution Mass Spectrometry (HR-MS) and Inductive Coupled Plasma Mass Spectrometry (ICP-MS). Purified 3 markers has shown High-Performance Liquid Chromatography-Diode Array Detector (HPLC-DAD) purity more than 99.5%. DSC the melting peaks of curcumin, desmethoxycurcumin and bisdemethoxycurcumin were observed at 168 °C, 165 °C, and 210 °C, respectively. These plant-based markers have high commercial potential as reference material for routine Quality Assurance and Quality Control (QAQC) in herbal industries.

Development of thiazole-appended novel hydrazones as a new class of α-amylase inhibitors with anticancer assets: an in silico and in vitro approach.

Hyperamylasemia is reported to be associated with numerous chronic diseases, including diabetes and cancer. Considering this fact, we developed a series of thiazole-clubbed hydrazones. The derivatives were explored for their in vitro α-amylase inhibitory activity, which was further corroborated with their anticancer assets using a panel of cancer cells, including colon cancer (HCT-116), lung cancer (A549), and breast cancer (MDA-MB-231). To better understand pharmacokinetics, the synthetic derivatives were subjected to in silico ADMET prediction. The in vitro based biological investigation revealed that compared to the reference drug acarbose (IC50 = 0.21 ± 0.008 µM), all the synthesized compounds (5a-5aa) exhibited in vitro α-amylase inhibitory response in the range of IC50 values from 0.23 ± 0.003 to 0.5 ± 0.0 µM. Along with this, the proliferations of the HCT-116, A549 and MDA-MB-231 cells were inhibited when treated with the synthesized compounds. Notable cancer cell growth inhibition was observed for compounds 5e, 5f and 5y, which correlated with their α-amylase inhibition. Additionally, the kinetics investigation revealed that 5b, 5e, 5f and 5y exhibit uncompetitive inhibition. 5b was found to be the least cytotoxic and most potent α-amylase inhibitor and was further validated by absorption and fluorescence quenching technique.