Search

At present, clinical interventions for chronic kidney disease are very limited, and most patients rely on dialysis to sustain their lives for a long time. However, studies on the gut–kidney axis have shown that the gut microbiota is a potentially effective target for correcting or controlling chronic kidney disease. This study showed that berberine, a natural drug with low oral availability, significantly ameliorated chronic kidney disease by altering the composition of the gut microbiota and inhibiting the production of gut-derived uremic toxins, including p -cresol. Furthermore, berberine reduced the content of p -cresol sulfate in plasma mainly by lowering the abundance of g_Clostridium_sensu_stricto_1 and inhibiting the tyrosine– p -cresol pathway of the intestinal flora. Meanwhile, berberine increased the butyric acid producing bacteria and the butyric acid content in feces, while decreased the renal toxic trimethylamine N -oxide. These findings suggest that berberine may be a therapeutic drug with significant potential to ameliorate chronic kidney disease through the gut–kidney axis. Berberine ameliorates chronic kidney disease through the gut–kidney axis by regulating the metabolism of nephrotoxins such as p -cresol by the gut microbiota. [Display omitted] [ABSTRACT FROM AUTHOR]

Six new compounds including two azaphilones, lunatoic acids D–E (1 , 2), three isocoumarins, lunatinins B–D (3 - 5), and one α-pyrone derivative, lunatinin E (6), as well as four known ones, lunatoic acid A (7), lunatinin (8), penicipyran D (9) and chaetoquadrin F (10) were isolated from the rice medium of the gut fungus Paraphaeosphaeria sp. XZD2-1. Six new compounds including two azaphilones, lunatoic acids D–E (1 , 2), three isocoumarins, lunatinins B–D (3 - 5), and one α-pyrone derivative, lunatinin E (6), as well as four known ones, lunatoic acid A (7), lunatinin (8), penicipyran D (9) and chaetoquadrin F (10) were isolated from the rice medium of the gut fungus Paraphaeosphaeria sp. XZD2-1. Their planar structures were elucidated by analysis of 1D and 2D NMR as well as HRESIMS spectroscopic data. The absolute configurations of compounds 1 - 3 were assigned by experimental and calculated ECD data and an ester hydrolysis reaction. Compounds 4 and 5 were a pair of enantiomeric excess mixture. Structure of compound 6 was further confirmed by comparing optical rotation with known compounds according to literature. The antimicrobial activity and cytotoxicity of compounds 1 - 10 were examined. • The first report about lunatoic acids from a marine-derived Paraphaeosphaeria sp. fungus. • Four new isocoumarin and α-pyrone derivatives from the fungus. • Experimental and calculated ECD were used to elucidate the absolute configurations of new compounds. • The antimicrobial activity and cytotoxicity of isolated compounds were examined. [ABSTRACT FROM AUTHOR]

Abstract: 2-Methylallylidene diacetate (DMA) was synthesis between methacrolein (MAL) and acetic anhydride using a mesoporous strong acidic cation-exchange resin as the catalyst. The effects of the molar ratio of the reactants, catalyst loading and stirring rate were investigated. The reaction kinetic equations were established under conditions that eliminated both internal and external diffusions. Kinetic constants such as the pre-exponential factor and the activation energy were also determined. The mechanism is proposed according to the kinetic study. [Copyright &y& Elsevier]

Colon cancer is still a major disease plaguing humans. In this study, we evaluated the synergistic antitumor effects of the combination of BRD4 inhibitor JQ1 and docosahexaenoic acid (DHA) in colon cancer. We demonstrated that simultaneous exposure to JQ1 and DHA resulted in strong synergistic antiproliferative and proapoptotic effects related to inhibition of expression of c-Myc and activation of NF-κB in colon cancer cell lines. At the same time, the synergetic anticancer effect had been confirmed in vivo. For in vivo experiments, JQ1 and DHA resulted in more significant tumor growth inhibition (53.7%) in a human colon cancer HCT116 xenograft model, comparing with the moderate inhibition in JQ1-treated (31.9%) or DHA-treated groups (20.3%). Because DHA is the predominant component of fish oil, our data suggest that this nontoxic dietary supplement could be administered with BRD4 inhibitor during therapy for CRC, which lay an important foundation for the development of therapeutic regimens for CRC. [ABSTRACT FROM AUTHOR]

Abstract Alokicenones A-H (1–8), eight new tetrahydroanthracenes and one known okicenone (9) were identified from the secondary metabolites of mangrove-derived Streptomyces sp. HN-A101. Their structures were elucidated by HRESIMS and NMR spectroscopic data. The absolute configurations of them were determined by the calculated and experimental ECD curves. Compounds 1–2 and 9 showed moderate cytotoxicity against HCT116 and SW620 cancer cell lines with IC 50 values from 0.63 to 7.73 μ M. In addition, compounds 1 – 3 and 7 – 9 also exhibited inhibitory activities against ROCK2 or BRD4. Graphical abstract Image 1 [ABSTRACT FROM AUTHOR]