Capsaicin Entrapment in Metal-Organic Framework Material Derived from γ-Cyclodextrin

Capsaicin, a pungent molecule from red chilli is known for its therapeutic benefits. However, poor aqueous solubility coupled with inherent pungency has limited its applications. We envisaged, encapsulation of capsaicin in biocompatible MOF material derived from γ-cyclodextrin (γ-CD) to overcome solubility and pungency attributes. Encapsulation of capsaicin was accomplished via crystal growth achieved by vapour diffusion of ethanol to synthesis solution consisting of γ-CD, KOH and capsaicin.The accomplished MOF Caps@γ-CDMOF was thoroughly characterized in solid state by powder X-ray diffraction (PXRD), IR, DSC, SEM and in solution by UV, fluorescence, NMR spectroscopic techniques. The encapsulation of capsaicin was found to be slightly higher than 3:1 (γ-CD: capsaicin ratio) in Caps@γ-CDMOF.</p

Flavone-based dual PARP-Tubulin inhibitor manifesting efficacy against endometrial cancer

AbstractStructural tailoring of the flavone framework (position 7) via organopalladium-catalyzed C–C bond formation was attempted in this study. The impact of substituents with varied electronic effects (phenyl ring, position 2 of the benzopyran scaffold) on the antitumor properties was also assessed. Resultantly, the efforts yielded a furyl arm bearing benzopyran possessing a 4-fluoro phenyl ring (position 2) (14) that manifested a magnificent antitumor profile against the Ishikawa cell lines mediated through dual inhibition of PARP and tubulin [(IC50 (PARP1) = 74 nM, IC50 (PARP2) = 109 nM) and tubulin (IC50 = 1.4 µM)]. Further investigations confirmed the ability of 14 to induce apoptosis as well as autophagy and cause cell cycle arrest at the G2/M phase. Overall, the outcome of the study culminated in a tractable dual PARP-tubulin inhibitor endowed with an impressive activity profile against endometrial cancer

A reference tissue atlas for the human kidney.

Kidney Precision Medicine Project (KPMP) is building a spatially specified human kidney tissue atlas in health and disease with single-cell resolution. Here, we describe the construction of an integrated reference map of cells, pathways, and genes using unaffected regions of nephrectomy tissues and undiseased human biopsies from 56 adult subjects. We use single-cell/nucleus transcriptomics, subsegmental laser microdissection transcriptomics and proteomics, near-single-cell proteomics, 3D and CODEX imaging, and spatial metabolomics to hierarchically identify genes, pathways, and cells. Integrated data from these different technologies coherently identify cell types/subtypes within different nephron segments and the interstitium. These profiles describe cell-level functional organization of the kidney following its physiological functions and link cell subtypes to genes, proteins, metabolites, and pathways. They further show that messenger RNA levels along the nephron are congruent with the subsegmental physiological activity. This reference atlas provides a framework for the classification of kidney disease when multiple molecular mechanisms underlie convergent clinical phenotypes