Compounds with NO Inhibitory Effect from the Rattan Stems of Sinomenium acutum, a Kind of Chinese Folk Medicine for Treating Rheumatoid Arthritis.

Three new alkaloids (1-3), one new diphenyl ether (4) and fifteen known alkaloids (5-19) were isolated from the rattan stems of Sinomenium acutum. Comprehensive analyses of HR-ESI-MS, 1D (1 H and 13 C), 2D-NMR (1 H-1 H COSY, HSQC, HMBC, NOESY), circular dichroism (CD), UV and IR revealed the structures and absolute configurations of these new compounds. The structures of other compounds were determined by comparison of their 1 H and 13 C-NMR data with previous literature reports. By measuring the amount of NO produced, the anti-inflammatory properties of the isolated compounds were studied. The results showed that compounds 4 and 5 had strong NO inhibitory activity.

Phytochemical Constituents and Biological Activities of Plants from the Genus Cissampelos.

Cissampelos is a significant genus comprising of approximately 21 species of the medicinal plants (Menispermaceae). The plants of this genus are used in traditional medicine for the treatment of various ailments such as asthma, arthritis, dysentery, hyperglycemia, cardiopathy, hypertension and other related problems. These plants are rich in bioactive dibenzylisoquinoline and aborphine as well as small amounts of other ingredients. In recent years, the chemical constituents and pharmacological activities of Cissampelos genus have been paid more and more attention due to their diversity. Herein, we compile the chemical constituents and biological activities on this genus, and summarize the 13 C-NMR data of the main bioactive ingredients. All information comes from scientific databases such as Google Scholar, PubMed, Sci-Finder, ScienceDirect, Web of Science and CNKI. It provides valuable data for the future research and development of Cissampelos genus.

Directed Evolution of Escherichia coli Nissle 1917 to Utilize Allulose as Sole Carbon Source.

Sugar substitutes are popular due to their akin taste and low calories. However, excessive use of aspartame and erythritol can have varying effects. While D-allulose is presently deemed a secure alternative to sugar, its excessive consumption is not devoid of cellular stress implications. In this study, the evolution of Escherichia coli Nissle 1917 (EcN) is directed to utilize allulose as sole carbon source through a combination of adaptive laboratory evolution (ALE) and fluorescence-activated droplet sorting (FADS) techniques. Employing whole genome sequencing (WGS) and clustered regularly interspaced short palindromic repeats interference (CRISPRi) in conjunction with compensatory expression displayed those genetic mutations in sugar and amino acid metabolic pathways, including glnP, glpF, gmpA, nagE, pgmB, ybaN, etc., increased allulose assimilation. Enzyme-substrate dynamics simulations and deep learning predict enhanced substrate specificity and catalytic efficiency in nagE A247E and pgmB G12R mutants. The findings evince that these mutations hold considerable promise in enhancing allulose uptake and facilitating its conversion into glycolysis, thus signifying the emergence of a novel metabolic pathway for allulose utilization. These revelations bear immense potential for the sustainable utilization of D-allulose in promoting health and well-being.

Modeling of drug release from bioerodible polymer matrices.

Models for drug release from bioerodible polymer matrices are proposed in this article. We consider that drug is released continually by diffusion that is influenced by polymer chain degradation, and polymer matrix erosion starts and enhances the drug release at a certain time. The models give excellent reproduction of drug release profiles within the whole release period, and the parameters can be correlated to various factors such as gamma-irradiation dose, copolymer composition, and initial drug loading, this correlation indicates that the new models can be used to predict the effects of various factors on drug release profiles based on limited experimental data.

A QSAR study on inhibitory activities of 1-phenylbenzimidazoles against the platelet-derived growth factor receptor.

A quantitative structure-activity relationship (QSAR) study on inhibitory activities of 1-phenylbenzimidazoles against the platelet-derived growth factor receptor (PDGFR) was carried out in this work, and a QSAR model was developed. It gives an r2 of 0.78 for the training set of 55 active compounds, and an r2 of 0.75 for the test set of 24 active compounds. The new model was further applied to predict inhibitory activities of additional 44 inactive compounds, and very good agreement with experimental observations was obtained. The new model requires only variable connectivity indices and two position indices as input parameters, which is simple and easy to apply. The new model is useful for developing new anticancer drugs, which also demonstrates that the recently developed variable connectivity indices are very useful structural descriptors in the QSAR studies in the fields of pharmaceutics and biochemistry.