Modular synthesis of fluorinated 2H-thiophenes via [4 + 1] cyclization of enaminothiones.

An efficient and straightforward synthetic method for constructing trifluoromethyl 2H-thiophenes through [4 + 1] cycloaddition of enaminothiones with trifluoromethyl N-tosylhydrazones has been disclosed. The cycloaddition platforms were found to be compatible with a broad substrate scope and to show high regio- and stereo-selectivities under very mild reaction conditions such as room temperature, neutral media and low loading of catalyst.

Understanding of Diabetes in Tibetan, Mongolian, Miao, Dai, Uygur, and Yi Medicine and Collation of Prevention and Cure Medicines.

Diabetes seriously endangers human health and causes a huge economic burden. With the improvement of people's living standard, the prevalence of diabetes is getting higher and higher, and age is becoming younger. It is an increasingly serious global problem. Therefore, it is imperative to find the drugs to treat diabetes. Ethnic medicine is an important part of the world's medicinal treasure house and has its own unique system. This study systematically combined the theoretical understanding of the prevention and treatment of diabetes of Tibetan, Mongolian, Miao, Dai, Uygur, and Yi people by searching the existing literature studies published until 2021, library collection resources (related ethnic monographs, medical books, standards of medicinal materials, etc.), CNKI, PubMed, and other databases and collected and sorted the relevant medicines. A total of 112 kinds of ethnic medicines for the prevention and treatment of diabetes have been discovered, including plant medicines (105 kinds), animal medicines (6 kinds), and fungal medicines (1 kind). The composition of family and genus, medicinal parts, and life forms of medicinal plants were analyzed, and the number of drugs used in the prevention and treatment of diabetes in each ethnic group was statistically analyzed. The results showed that Rosaceae was at the top of the list, and the drugs used in underground parts accounted for 33.90% of the total, and the medicinal plants were mainly herbaceous, and the Mongolians have the largest number of diabetes medicines. In addition, CNKI, PubMed, and other databases selected "medicinal materials name," "diabetes," and "hypoglycemia" as keywords, the top 30 medicinal materials reported in existing literature were listed, and their Chinese name, the Latin name of the original plant, family and genus, nationality used, medicinal parts, and active ingredients related to the prevention and treatment of diabetes were introduced in detail. Among the 30 medicines, Astragalus membranaceus, Pueraria lobata, and Coptis chinensis are the most commonly used. Through literature research, this study summarized the existing theories of ethnic medicine for the prevention and treatment of diabetes, collected and sorted out ethnic medicine, clarified the potential mechanism of ethnic medicine, and provided effective data compilation. Ethnic medicine has a long history of treating diabetes, and there are abundant medicinal materials, to provide a new idea and basis for treating diabetes.

[Determination of six alkaloids in six types of Coptidis Rhizoma pieces by RP-HPLC and spectrum-effect relationships with anti-diabetes pharmacodynamics data].

To establish a method for determining the contents of six alkaloids (jatrorrhizine hydrochloride, columbamine hydrochloride, epiberberine hydrochloride, coptisine hydrochloride, palmatine hydrochloride, berberine hydrochloride) in six types of Coptidis Rhizoma pieces (crude pieces, ginger juice stir-fried pieces, vinegar stir-fried pieces, wine steamed pieces, wine stir-fried pieces, evodiae juice stir-fried pieces) by RP-HPLC, and explore the relationship with the curative effect of traditional Chinese medicine (TCM) and pharmacodynamics results. The chromatographic column was Welch XtimateTM C18 (4.6 mm×250 mm, 5 µm), with 0.1% triethylamine solution (adjust pH at 10 with ammonium bicarbonate and ammonia) as mobile phase A and acetonitrile as mobile phase B for gradient elution (0-15 min, 10%-25%B; 15-25 min, 25%-30%B; 25-40 min, 30%-45%B) at a rate of 1.0 mL•min⁻¹. The column temperature was set at 30 ℃, and the wavelength was set at 270 nm. The six alkaloids showed a good linear relationship within the range of 0.85-16.96 mg•L⁻¹ (r=0.999 7), 1.25-24.96 mg•L⁻¹ (r=0.999 9), 2.05-40.96 mg•L⁻¹ (r=0.999 9), 3.65-72.96 mg•L⁻¹ (r=0.999 9), 2.88-57.60 mg•L⁻¹ (r=0.999 8), and 13.25-264.96 mg•L⁻¹ (r=0.999 6) respectively. The average recoveries (n=9) of the six alkaloids were 102.4% (RSD 1.2%), 101.8% (RSD 1.3%), 100.3% (RSD 1.8%), 100.7%(RSD 1.8%), 101.2% (RSD 1.5%) and 97.90% (RSD 2.0%) respectively, and their average contents were 3.55, 4.49, 9.12, 19.17, 15.69, 62.56 mg•g⁻¹, respectively. This determination method was accurate and repeatable, which could be used for the content determination in six types of Coptidis Rhizoma pieces. Data analysis on contents determination and preliminary pharmacodynamics results was conducted by using principal component analysis (PCA) and hierarchical clustering analysis (HCA). The analysis results showed that three types of Coptidis Rhizoma pieces (wine steamed pieces, wine stir-fried pieces, and evodiae juice stir-fried pieces) had significant differences with crude pieces, and the wine steamed Coptidis Rhizoma pieces showed most difference with crude pieces especially, mainly related to triglyceride (TG) and fasting blood glucose levels (FBG) in serum. In addition, columbamine hydrochloride was most affected among the six alkaloids. Those three types of Coptidis Rhizoma pieces (wine steamed pieces, wine stir-fried pieces, and evodiae juice stir-fried pieces), had more advantages for "anti-diabetes" in TCM clinical application, especially in the treatment of diabetic hyperlipidemia.