Organosilicon compounds are widely used in materials science, medicinal chemistry and synthetic chemistry. Recently, significant progress has been achieved in transition metal‐catalyzed dehydrogenative C−H silylation. Particularly, recently developed monohydrosilane and dihydrosilane mediated C−H silylation have emerged as powerful tools in constructing C−Si bonds. Besides, dihydrosilane‐mediated enantioselective asymmetric C−H silylation has successfully enabled the construction of central and helical silicon chirality. In addition, chiral organosilicon compounds have exhibited excellent photoelectric material properties and broad application prospects. Furthermore, organosilicon compounds could under a series of functional group transformations to enrich the diversity of silicon chemistry. This review will present a comprehensive picture of the development of transition metal‐catalyzed hydrosilane‐mediated intramolecular C(sp2)−H and C(sp3)−H silylation organized by their reaction types and mechanisms. In addition, dihydrosilane‐mediated enantioselective asymmetric C−H silylation to construct central and helical silicon chirality will also be highlighted in the review.

Picroside II, an iridoid glycoside, has anti‐cancer, anti‐virus, anti‐apoptotic, nervous and myocardial protection effects and so on. However, the oral bioavailability of Picroside II is low, and the half‐life in vivo is short, so it is limited to use in clinic. Triazole is a highly stable heterocyclic ring, which can be interacted with various enzymes or receptors in the organism through non‐covalent interactions, and many of its good pharmacological activities in vitro and in vivo have been reported. Based on the advantages of triazole and Picroside II, a series of triazole‐modified Picroside II derivatives (5 a–5 i) were synthesized by using drug combination principles for the first time. The structures were confirmed by different spectroscopic techniques including 1H NMR, 13C NMR and HRMS, and the primary biological evaluation of anti‐breast cancer, anti‐colorectal cancer, the effect on SARS‐CoV‐2 3CLpro inhibitor, and CD47‐SIRPα protein were screened as well. Compound 5 e has anti‐breast cancer activity, and compounds 3 and 5 i have anti‐colorectal cancer activity.

Catalpol and its derivatives were found in a variety of Chinese medicinal plants and possess various biological activities, such as anti-inflammatory, anti-oxidant, neuroprotective, cardiovascular protective, anti-tumor and hypoglycemic and so on. The extensive pharmacological activities of catalpol have been attracted much attention to researchers, but the clinical applications are limited by poor lipid solubility, low bioavailability and short half-life, so pharmacologists have made various structural modifications to catalpol, such as increasing lipid solubility to enhance its biological activities in the hope that it can be widely used in clinical applications. In this paper, using "Catalpol" and "Catalpol derivatives" as the keywords, more than 200 articles from 1965 to 2021 were obtained from databases, such as CNKI, PubMed, Scifinder and so on. Finally, 93 articles were selected to systematically analyze the structure and efficacy of catalpol and its derivatives according to pharmacological activity, which will provide ideas for the development of new catalpol drugs in the future.

Iridoids, an important active ingredient, are widely distributed in varieties of Chinese herbal medicines and have varieties of pharmacological activities, such as anti-tumor, hypoglycemic, anti-inflammatory and so on, most of which exist in the form of glycosides in nature. However, its clinical application is limited by poor lipid solubility, low bioavailability and short half-life. It is necessary to optimize the structure of iridoids. It is hard to modify the hydroxyl groups at specific sites because iridoid glycosides are polyhydroxy compounds and very complex. In this paper, the words of ‘Iridoid glycosides’ and ‘Hydroxyl protection’ were used as the keywords, more than 200 articles from 1965 to 2021 were obtained from databases, such as CNKI, PubMed, Scifinder and so on. Finally, 60 articles were selected to summarize the hydroxyl protection of iridoid glycosides, which will provide a theoretical basis for their structural modification and stimulate their application potential in the field of drug research and development.

Catalpol has gained increasing attention for its potential contributions in controlling glycolipid metabolism and diabetic complications, which makes used as a very promising scaffold for seeking new anti-diabetic drug candidates. Acylation derivatives of catalpol crotonate (CCs) were designed as drug ligands of glutathione peroxidase (GSH-Px) based on molecular docking (MD) using Surfex-Docking method. Catalpol hexacrotonate (CC-6) was synthesized using microwave assisted method and characterized by FT-IR, NMR, HPLC and HRMS. The MD results indicate that with the increasing of esterification degree of hydroxyl, the C log P of CCs increased significantly, and the calculated total scores (Total_score) of CCs are all higher than that of catalpol. It shows that CCs maybe served as potential lead compounds for neuroprotective agents. It was found that the maximum Total_score of isomers in one group CCs is often not that the molecule with minimum energy. MD calculations show that there are five hydrogen bonds formed between CC-6 and the surrounding amino acid residues. Molecular dynamics simulation results show that the binding of CC-6 with GSH-Px is stable. CC-6 was screened for SH-SY5Y cells viability by MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) assay, the result indicates CC-6 can effectively reverse SZT induced cells apoptosis with dose-dependent manner, which can indirectly show that CC-6 is a potential neuroprotective agent.