[Efficient synthesis of polydatin by a two-enzyme coupled with one-pot method].

Traditional Chinese medicine of has been utilized in China for thousands of years. Its primary active compound, polydatin, exhibits a variety of pharmacological effects including the regulation of glucose and lipid metabolism, suppression of cough and asthma, as well as antibacterial and anti-inflammatory properties. However, conventional methods for polydatin production are inadequate to satisfy the market demand.

Engineering regioselectivity of glycosyltransferase for efficient polydatin synthesis.

Resveratrol is a promising functional ingredient applied in food products. However, low bioavailability and poor water solubility, which can be improved by glycosylation, hinder its application. A uridine diphosphate-dependent glycosyltransferase (UGT) from Bacillus subtilis 168 (named UGT) presents potential application for resveratrol glycosylation; nonetheless, imprecise regioselectivity renders the synthesis of resveratrol-3-O-β-D-glucoside (polydatin) difficult.

Mutability landscape guided engineering of a promiscuous microbial glycosyltransferase for regioselective synthesis of salidroside and icariside D2.

Microbial glycosyltransferases efficiently synthesize glucosides and have garnered increasing interest. However, limited regioselectivity has impeded their broad application, particularly in the pharmaceutical industry. In this study, the UDP-glycosyltransferase YjiC from Bacillus licheniformis (BlYjiC) was engineered to achieve the bidirectional regioselective glycosylation of tyrosol and its derivatives.

Improvement in organic solvent resistance of keratinase BLk by directed evolution.

Keratinase, a vital enzyme in hair degradation, requires enhanced stability for industrial applications in the harsh reaction environment used for keratin hydrolysis. Previous studies have focused on improving keratinase thermostability. In this study, directed evolution was applied to enhance the organic solvent stability of the keratinase BLk from Bacillus licheniformis.

Highly efficient biosynthesis of salidroside by a UDP-glucosyltransferase-catalyzed cascade reaction.

Objective: Salidroside is an important plant-derived aromatic compound with diverse biological properties. The main objective of this study was to synthesize salidroside from tyrosol using UDP-glucosyltransferase (UGT) with in situ regeneration of UDP-glucose (UDPG).

Results: The UDP-glucosyltransferase 85A1 (UGT85A1) from Arabidopsis thaliana, which showed high activity and regioselectivity towards tyrosol, was selected for the production of salidroside.

TiCl-mediated deoxygenative reduction of aromatic ketones to alkylarenes with ammonia borane.

A rapid and mild protocol for the exhaustive deoxygenation of various aromatic ketones to corresponding alkanes was described, which was mediated by TiCl and used ammonia borane (AB) as the reductant. This reduction protocol applies to a wide range of substrates in moderate to excellent yields at room temperature. The gram-scale reaction and syntheses of some key building blocks for SGLT2 inhibitors demonstrated the practicability of this methodology.

Discovery of a Novel Macrocyclic ATP Citrate Lyase Inhibitor.

ATP citrate lyase (ACLY) is an important metabolic enzyme involved in the synthesis of fatty acid and cholesterol. The inhibition of ACLY is considered as a promising therapeutic strategy for various metabolic diseases and numerous malignancies. In this study, a novel macrocyclic compound has been identified as a potent ACLY inhibitor with the "ring closing" strategy for conformational restriction based on -.

Diversity synthesis of indole derivatives catalyst control cyclization reaction of 2-indolylmethanols and azonaphthalene.

A series of indole-fused scaffolds and derivatives was synthesized the cyclization reaction of 2-indolylmethanols with azonaphthalene. These reactions were realized under mild reaction conditions through catalyst control, providing structurally diverse indole derivatives with moderate to excellent yields. This protocol also shows good substrate adaptability, especially in six-membered ring products.

Simultaneous determination of 16 important biologically active phytohormones in Dendrobium huoshanese by pressurized capillary electrochromatography.

A rapid pressurized capillary electrochromatography (pCEC) method has been successfully developed for the simultaneous determination of 16 phytohormones in Dendrobium huoshanense. Effects of wavelength, mobile phase, the flow rate, pH value, concentration of buffer and applied voltage were investigated, respectively. The results showed that the 16 phytohormones could be baseline-separated rapidly in less than 21 min on a reversed-phase EP-100-20/45-3-C18 capillary column (total length of 45 cm, effective length of 20 cm, diameter of 100 μm, ODS packing inside for 3 μm) with ACN/5.

Rapid quantification of polysaccharide and the main onosaccharides in Dendrobium huoshanense by near-infrared attenuated total reflectance spectroscopy.

A rapid, green, low cost and nondestructive attenuated total reflection near infrared (ATR NIR) method was developed to quantify the total polysaccharide and the main monosaccharides mannose and glucose in Dendrobium huoshanense. Total 100 D. huoshanense samples from different places were analyzed using ATR NIR method.