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  • Shuo YUAN, Yi-fan ZHANG, Peng GAO, Jun LEI, Ying-yuan LU, Peng-fei TU, Yong JIANG
    Acta Pharmaceutica Sinica. 2025, 60(1): 82-95.

    Fecal microbiota transplantation (FMT) technology originated in China during the Eastern Jin Dynasty and has rapidly developed over the past two decades, becoming a primary method for studying the causal relationship between gut microbiota and the occurrence and progression of diseases. At the same time, the therapeutic effects of FMT in the field of gastrointestinal diseases have gained widespread recognition and are gradually expanding into other disease areas. The FMT procedure is relatively complex, and there is currently no standardized method; its success is influenced by various factors, including the donor, recipient, processing of the fecal material, and the method of implantation. Given the increasingly recognized relationship between gut microbiota and various diseases, FMT has become a research hotspot in both scientific studies and clinical applications, achieving a series of significant advancements. To help researchers better understand this technology, this paper will outline the development history of FMT, summarize common operational methods in research and clinical settings, review its application progress, and look forward to future development directions.

  • Li-jun ZHAO, You-fu YANG, Tong-sheng WANG, Yan-li ZHANG, Ya WU
    Acta Pharmaceutica Sinica. 2025, 60(1): 22-36.

    Isosteviol is a tetracyclic diterpenoid compound obtained by hydrolysis of natural stevia glycoside under acidic conditions. It has many pharmacological activities, such as anti-tumor, hypoglycemic, anti-inflammatory and antibacterial. Due to its low water solubility, low activity and low bioavailability, isosteviol has poor performance. In order to overcome these shortcomings, scholars have obtained a large number of isosteviol derivatives with novel structures and excellent activity. In this paper, we review the recent progress in the research on the structure modification, biological activity, structure-activity relationship and microbial transformation of isosteviol, in order to provide a reference for the development of new drugs of isosteviol and its derivatives.

  • Min SUN, Chuan-sheng HUANG, Li-ping WANG, Xu-li RUAN, Yun-li ZHAO, Xin-chun WANG
    Acta Pharmaceutica Sinica. 2025, 60(1): 72-81.

    Due to patient compliance and convenience, oral medication is likely the most common and acceptable method of drug administration. However, traditional dosage forms such as tablets or capsules may lead to low drug bioavailability and poor therapeutic efficiency. Therefore, with advancements in material science and micro/nano manufacturing technology, various carriers have been developed to enhance drug absorption in the gastrointestinal tract. In this context, we initially discuss the key biological factors that hinder drug transport and absorption (including anatomical, physical, and biological factors). Building on this foundation, recent progress in both conventional and innovative oral drug delivery routes aimed at improving drug bioavailability and targeting is reviewed. Finally, we explore future prospects for oral drug delivery systems as well as potential challenges in clinical translation.

  • Li-ke WANG, Bing-yan LI, Zhen-zhu ZHAO, Yan-zhi WANG, Xiao-kun LI, Wei-sheng FENG, Ying-ying SI
    Acta Pharmaceutica Sinica. 2025, 60(1): 191-195.

    Nine compounds were isolated and purified from 90% ethanol extract of Alstonia mairei Lévl by using various chromatographic methods, including silica gel, SephadexLH-20, MCI Gel and ODS column chromatography, combined with semi-preparative liquid phase separation methods. Modern spectroscopic methods (1D and 2D NMR, UV, IR, MS, etc.) were used to identify the structures of the isolated compounds. They were identified as mairoside A (1), 3′, 6-di-O-sinaloylsucrose (2), myristic acid (3), methyl myristate (4), ethyl myristate (5), 3, 4, 5-trimethoxycinnamic acid (6), 3, 4, 5-trimethoxybenzoic acid (7), vinoline (8), kaempferol-3-O-rutinoside (9), among which compound 1 is a new glycoside, compounds 4 and 5 are new natural products, and the nuclear magnetic data of compound 4 were reported for the first time.

  • Shao-jie CHU, Yan ZHENG, Shuang-shuang SU, Xue-song WU, Hong YAN, Shao-xin CHEN, Hong-bo WANG
    Acta Pharmaceutica Sinica. 2025, 60(1): 48-57.

    As the number of patients with compromised immune function increases and fungal resistance develops, so does the risk of contracting deadly fungi in humans. Both fungi and humans are eukaryotes, so identifying unique targets for antifungal drug development is difficult. In addition, the existing antifungal drugs are limited by toxicity, drug interaction and drug resistance in practical application, which leads to the increasing incidence and fatal rate of fungal infections. Therefore, it is urgent to develop new antifungal drugs. The semi-synthetic technology using microbial fermentation products from natural sources as lead compounds has become the most used method in structural modification of antifungal drugs due to its advantages of few reaction steps and easy operation. This paper will introduce the current status of natural antifungal drugs in clinical use, as well as the latest progress in the research and development of new semi-synthetic antifungal drugs, and summarize their mechanism of action, structural modifications, advantages and disadvantages, so as to provide reference for the subsequent development of new antifungal drugs.

  • Xiao-ming ZHANG, Ran MA, Li-jing LÜ, Lü-yin WANG, Ping LÜ, Cheng-gang LIANG, Jing LI
    Acta Pharmaceutica Sinica. 2025, 60(1): 211-217.

    In this study, we constructed a GLP-2R-HEK293 cell line and established a method for the determination of the in vitro biological activity of teduglutide based on HTRF, after optimizing experimental conditions and methodological verification. We also carried out relative potency detection of teduglutide pharmaceutical products using this method. The result showed that there was a quantitative-efficient relationship between the teduglutide activity and cAMP contents in GLP-2R-HEK293 cells, which conformed to four-parameter model. Method verification results of five concentrations of teduglutide (64%, 80%, 100%, 125% and 156%) met the requirements of the General Rules of Chinese Pharmacopoeia, 2020 edition, Volume Ⅳ (9401). We then analyzed the relative potency of three batches of teduglutide drug substances and three batches of drug products. The linearity, regression and parallelism of the obtained curves all fit the system suitability requirements. The relative potency of six batches of teduglutide was from 83% to 105%. In summary, the biological activity detection method established in this study was accurate, precise, simple and time-saving, which can be used for quality control of teduglutide pharmaceutical products.

  • Meng YANG, Zhi-you HAO, Xiao-lan WANG, Chao-yuan XIAO, Jun-yang ZHANG, Shi-qi ZHOU, Xiao-ke ZHENG, Wei-sheng FENG
    Acta Pharmaceutica Sinica. 2025, 60(1): 205-210.

    Eight compounds were isolated and purified from the ethyl acetate part of 70% acetone extract of Rehmannia glutinosa by various chromatographic techniques such as silica gel, MCI gel CHP-20, ODS, Toyopearl HW-40C, combined with TLC and semi-preparative HPLC. Their structures were elucidated by modern spectroscopy techniques (NMR, MS, UV, IR), and identified as neomartynoside A (1), osmanthuside B6 (2), martynoside (3), isomartynoside (4), (E)-p-hydroxycinnamic acid (5), caffeic acid (6), ferulic acid (7), and methyl caffeate (8). Compound 1 is a new phenylethanol glycoside, which was identified as neomartynoside A. Compound 2 was isolated from Rehmannia glutinosa for the first time. In addition, compounds 2, 6 and 7 significantly increased relative glucose consumption, showing potential hypoglycemic activity.

  • Xin-yue HU, Jia-hao KONG, Yue SUN, Lü-yin WANG, Xiao-ming ZHANG, Ping LÜ, Cheng-gang LIANG, Jing LI
    Acta Pharmaceutica Sinica. 2024, 59(12): 3361-3366.

    The Dionex CaboPacTM PA10 BioLCTM Analyical 2 mm × 250 mm column was used with a protective column (Dionex CaboPacTM PA10 BioLCTM Guard 2 mm × 50 mm). 100 mmol·L-1 sodium hydroxide solution was used as eluent; the flow rate was 0.25 mL·min-1. Sample tray temperature: 35 ℃. The pulse amperometric detector was adopted, and the waveform was Gold CWE, Ag-AgCl RE, Carbo, Quad. The samples were cultured with 8 concentrations of glycogen substrates (0.31, 1.25, 2.5, 5, 10, 20, 30, and 40 mg·mL-1). D-Glucose concentrations were measured at 5 different time points (T0, T1, T2, T3 and T4). The glucose concentration from T1 to T4 minus the glucose concentration at T0. The reaction rate was calculated at different glycogen substrate concentrations. These reaction rates are plotted against substrate concentrations using Michaelis-Menten equation. The kinetic parameters were expressed as Vmax (nmol·mg-1·min-1) and Km (mg·mL-1). The RSD of glucose standard curve R2 (n = 6, linear range: 1.25-500 μmol·L-1) was 0.1% and the RSD (n = 6) of the slope of the standard curve was 2.2%. The mean limit of quantitation was 0.14 μmol·L-1, and the mean limit of detection was 0.05 μmol·L-1. The RSD of Km and Vmax were 4.4% and 4.6% respectively in three separate experiments. The durability of the method was good. The method was developed for the on-line automatic determination of the hydrolysis kinetics of acid α-glucosidase (GAA) for injection by ion chromatography. The method has good precision, repeatability and durability, and can be used for the determination of glycogen hydrolysis kinetics of GAA for injection, and could reference value for the enzyme kinetics evaluation of recombinant enzyme replacement therapy.

  • Chao-yuan XIAO, Zhi-you HAO, Meng YANG, Shi-qi ZHOU, Jun-yang ZHANG, Xiao-ke ZHENG, Yan-jun SUN, Wei-sheng FENG
    Acta Pharmaceutica Sinica. 2024, 59(12): 3325-3329.

    The 95% ethanol extract of Poria cocos was separated and purified by ODS, MCI gel CHP20 and silica gel column chromatography combined with the semi-preparative HPLC. The chemical structures of the isolated compounds were identified by NMR, MS, IR, and calculated NMR methods. Seven compounds were isolated from Poria cocos and identified as 20S-2β, 3α, 15α, 19, 20-hydroxy-pregnane-7-ene (1), dehydroeburicoic acid monoacetate (2), eburicoic acid acetate (3), dehydroeburicoic acid (4), eburicoic acid (5), dehydropachymic acid (6), pachymic acid (7). Compound 1 is a new pregnane steroid.

  • Wan-xin CAO, Yi-hui YANG, Hong YANG, Sen ZHANG, Yi-zhi ZHANG, Fang XU, Wan LI, Yue HAO, Xiao-xue LI, Xu ZHANG, Guan-hua DU, Jin-hua WANG
    Acta Pharmaceutica Sinica. 2024, 59(12): 3222-3231.

    The blood-brain barrier (BBB) plays a crucial role in maintaining the homeostasis of the brain's internal environment, which poses challenges to the treatment of central nervous system diseases. Drug carriers can aid in the delivery of therapeutic agents across the BBB to exert their pharmacological effects. The article reviewed the pathways for drug delivery across the BBB, the intracerebral fate and the classification of drug carriers and focuses on the functions and characteristics of liposomes, exosomes, apoptotic bodies, cell-penetrating peptides, and cell-targeting peptides. The review will provide an outlook on the future and challenge of research in the field of drug delivery across the BBB.