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The NOD-like receptor family pyrin domain-containing protein 3 (NLRP3) is a key cytosolic pattern recognition receptor that senses diverse pathogen- and host-originated threat signals. Aberrant activation of NLRP3 inflammasomes is closely associated with the pathogenesis of various complex inflammatory diseases. Nevertheless, the detailed regulation mechanism of NLRP3 inflammasome and its pathogenic roles in the inflammation progression remain to be fully elucidated. Fluorescent imaging with small molecule probe can provide valuable visualization information on the expression, occupancy and bio-distribution of target protein. Herein, we reported a series of diarylsulfonylurea NLRP3 fluorescent inhibitors bearing an amino benzodiazole fluorophore. Compared to the previously reported NLRP3 fluorescent probes, these inhibitors are more structurally concise and membrane permeable due to no additionally appended fluorophore via a linker. Among this series, compound 13a exhibited the most potent cellular NLRP3 inhibitory effect with an IC

Continued chemical investigation on the fruits of Aesculus pavia L. resulted in theisolation and identification of two new oleanolic acid saponins, namely vaccaroside A (1) andvaccaroside B (2). The isolated furostanol saponins were evaluated for cytotoxic activity againsthuman normal amniotic and human lung carcinoma cell lines using neutral red and MTT assays.In vitro experiments showed significant cytotoxicity in a dose dependent manner with IC50 valuesin the range of 27.80–79.02 μM.

Three novel compounds with spiro-5, 6-lactone ring skeleton has been isolated from the fermentation broth of Massrison sp. which could be isolated repeatedly from wild Rehmannia glutinosa. Psetariae oryza P-2b was applied to guide fractionation of bioactive compounds produced by Massrison sp. The molecular structures were established by a variety of one- and two-dimensional NMR experiments and the compounds with similar skeleton were reported for the first time from endophytic fungi of terraneous plant. Antifungal and cytotoxic activities of the compounds were tested, compounds 2 and 3 displayed stronger antifungal and cytotoxic activities. The compounds have the potential to be antibiotic against fungal pathogens and tumor cells.

Constituents of the fruits of Rubus corchorifolius were investigated. A new compound, namely rubusin A (1), along with three known compounds, was isolated and characterized. Among them, the new compound exhibited significant activity against kidney deficiency, and quercetin and kaempferol were isolated from the fruits of R. corchorifolius for the first time.

Two new oleanolic acid saponins, namely celosin C (1) and celosin D (2), were isolated from the ethanol extract of Semen celosiae. Their structures were identified as celosin C (1) and celosin D (2) by spectroscopic and chemical analyses. The hepatoprotective activity of 1 and 2 with oral dose 1.0, 2.0 and 4.0 mg/kg, respectively, were investigated by carbon tetrachloride (CCl(4))-induced hepatotoxicity in mice. The results indicate that they have significant hepatoprotective effects (p

A new triterpenoid saponin, named semenoside A (1), was isolated from Semen Celosia cristatae. Its structure was elucidated on the basis of 1D, 2D NMR, HR-FAB-MS and ESI-MS techniques, and physicochemical properties. The hepatoprotective activity of semenoside A with an oral dose of 1.0, 2.0 and 4.0mg/kg, respectively, were investigated by carbon tetrachloride (CCl(4))-induced hepatotoxicity in mice. The results indicated that it had significant hepatoprotective effects (p < 0.01).

Constituents of the fruits of Peatasites tatewakianus were investigated. A new compound, namely bakkenolide-VI (1), was isolated. The structures was elucidated on the basis of 1D, 2D NMR, TOF-MS and ESI-MS techniques, and physicochemical properties. The neuroprotective activity of the new compound was assayed with primary cultured neurons exposed to oxygen-glucose deprivation and oxidative insults.