Latest ArticlesRamulus Mori (Sangzhi) alkaloids (SZ-A) are a group of polyhydroxy alkaloids extracted and isolated from the traditional Chinese medicine mulberry twig, which is mainly used for the treatment of type 2 diabetes mellitus (T2DM). In addition to acting as a glycosidase inhibitor in the small intestine after oral administration, SZ-A can also be absorbed into blood and widely distributed to target organs related to diabetes, exerting multiple pharmacological effects. It is important to elucidate the possible pharmacokinetic influences of SZ-A for its clinical rational applications, such as drug interactions, the effects of food and alcohol on the absorption of SZ-A. However, studies in this area are limited. Therefore, the pharmacokinetic interactions between orally administrated SZ-A (50 mg·kg-1) and metformin hydrochloride (Met, 200 mg·kg-1) in Sprague-Dawley (SD) rats were examined. Then, the effect of food (standard feed) on the pharmacokinetics of SZ-A was investigated using fasting administration of SZ-A (50 mg·kg-1) in rats as a control. Finally, we investigated the pharmacokinetic characteristics of SZ-A (50 mg·kg-1) in different concentrations alcohol solutions using aqueous solution of SZ-A administered to rats as a control to evaluate the effect of alcohol on the bioabsorption of SZ-A. The results showed no significant pharmacokinetic interactions between SZ-A and Met after combination treatment. The standard feed had little effect on the pharmacokinetic profile of SZ-A. Alcohol retarded the absorption of SZ-A, resulting in a significant decrease in the Cmax of SZ-A. The decrease was greater at higher alcohol concentrations; however, no significant difference was observed in the AUC0-t. These results support the clinical rational applications of SZ-A. All animal protocols were approved by the Ethics Committee of Kangtai Medical Laboratory Service Hebei Co., Ltd. (Hebei, China) (No. MDL2022-01-17-1).
Protein tyrosine phosphatase (PTP) 1B is a potential therapeutic target for type 2 diabetes. Phosphotyrosine (pTyr) mimetics still dominate the currently available PTP1B inhibitors. The phenoxyacetic acid moiety was taken as a pTyr mimetic herein and phenoxyacetic acid-based compounds 2a-2g and 3a-3c were designed. Among them, compounds 2a-2g exhibited potent inhibition against PTP1B, and compound 2g showed an IC50 of 0.42 μmol·L-1 against PTP1B. Compound 2f exhibited pharmacological profiles similar to that of rosiglitazone, and could improve the insulin sensitivity and the serum total cholesterol level. The results suggest that PTP1B inhibitors might be effective in treating type 2 diabetes as well as associated metabolic syndromes.
Artemisinin is a sesquiterpene lactone natural product that contains an endoperoxide bond. Artemisinin has various biological activities including antimalarial, anti-tumor, antiviral and anti-fibrotic activity. Owing to the poor pharmacokinetic properties of artemisinin, its derivatives are currently used in clinic and frequently reported in literature. Although numerous derivatives of artemisinin have been reported, no study has been carried out yet to study the effect of substituted groups with different acid-base property on the antimalarial activity. Among these derivatives, the C-10 carbon artemisinin derivatives are often reported, and their corresponding 10β epimer show much better antimalarial activity than 10α epimer with large-sized substitute. However, there is currently no stereoselective synthesis to efficiently prepare the privileged 10β epimer of C-10 carba artemisinin. To address these two scientific questions, we herein first report an optimized method to stereoselectively synthesize the 10β epimer of C-10 carba artemisinin (98∶2 d.r.). Second, we employed the optimized method to synthesize a series of C-10 carba artemisinin derivatives with different acid-base properties. The antimalarial examination indicated that those derivatives with neutral groups or basic group of short chain showed similar antimalarial activity as dihydroartemisinin (DHA). The acidic group could dramatically decrease the antimalarial effect and was more than 22-fold less effective than DHA or the neutral ones. This study will shed light on the development of new generation of artemisinin derivatives with potent activity.
Twelve compounds, including 5 new monoterpenes and 7 known derivatives, were isolated from a water decoction of Monochasma savatieri by column chromatography over macroporous adsorbent resin, MCI resin, Sephadex LH-20, and HW-40C, combined with preparative TLC, reversed phase HPLC, and flash column chromatographic techniques. Their structures were elucidated by comprehensive analysis of spectroscopic data, along with enzymatic hydrolysis as well as electronic circular dichroism (ECD) and NMR calculations, the new structures named monochaside Ⅰ (1) and monochairidols A-D (2-5), respectively. The known compounds 6-12 were obtained from the Monochasma plants for the first time.
Three new anthraquinones were isolated from the 80% ethanol extract of Prismatomeris tetrandra by silica gel, MCI, ODS column chromatography and high performance preparative liquid chromatography (HPLC). The structures of the new compounds were identified by mass spectrometry, nuclear magnetic resonance and other spectroscopic methods as 6-hydroxy-1,2,3-trimethoxy-7-methylanthracene-9,10-dione (1), 6-(hydroxymethyl)-1,2,3-trimethoxyanthracene-9,10-dione (2) and 7-hydroxy-6-(hydroxymethyl)-1,2-dimethoxyanthracene-9,10-dione (3). Compounds 1, 2 and 3 showed protective effects against monosodium glutamate-induced damage in SH-SY5Y neuroblastoma cells, with the cell survival rates elevated 18.45%, 4.31%, and 7.65%, respectively.
This study aimed to prepare silk fibroin nanoparticles (SF-NPs) and assess the physicochemical properties and biocompatibility of the formulation. An optimized and simplified solvent displacement method was employed to obtain SF-NPs. Single-factor prescription screening, such as silk fibroin (SF) solution concentration, the ratio of SF solution to organic solvent, ultrasonication power and time, and different types of organic phases, was used to optimize the formulation. The characterization of the optimal formulation included particle size, polydispersity index (PDI), zeta potential, morphology, and stability. The in vitro cell compatibility of the nanoparticles was evaluated using CCK-8 and Calcein-AM/PI cell viability staining. The results showed that when SF concentration was 20 mg·mL-1, volume ratio of aqueous phase to acetone was 1∶6, ultrasonic power was 80 W and ultrasonic time was 3 min, the best SF-NPs was obtained. The nanoparticles prepared in this study exhibit a near-spherical shape, with a uniform size distribution, having an average size of 144.8 nm, a PDI of 0.174, and a zeta potential of -27.35 mV. Results from in vitro cell experiments demonstrate excellent cell compatibility of SF-NPs, showing the ability to promote cell proliferation. The SF-NPs which were successfully prepared in this study exhibit uniform particle size and excellent biocompatibility.
The taste of oral dosage forms has become a critical factor affecting the drug compliance and adherence to the treatment, and clinical application of the drug product may seriously restricted due to its bad taste. On the basis of the statement for the basic principle and specific performance of existing instruments, the application progress of electronic tongue on drug taste evaluation is addressed in detail. In view of its objective, fatigue-free, less harmful and accurate advantages, electronic tongue has been widely and meaningfully applied in the aspects of bitterness masking, and quality assessment and assurance of drug products. In addition, the reasons limiting the popularization of electronic tongue are mentioned in the paper, and some suggestions might be useful to enlarge the further application in the future.
Recent years, China has released a series of policies to encourage drug research and development in pediatric populations, aiming to meet pediatric populations' medical needs. Because of the physical and psychological developmental characteristics, tolerance of aversive feelings when taking medications are different between pediatric population and adults. So pediatric populations are at a relatively higher risk of not taking medications as prescribed when the medication tasted unpleasant. Therefore, sound design and evaluation of oral sensory features have important clinical significance and value in developing pediatric medications. "Technical guidance for the design and evaluation of the oral sensory features of pediatric drugs (trial version) " was released in November 2022, by Centre for Drug Evaluation, National Medical Products Administration of China. Based on the guidance, this article will introduce the drafting background and review considerations, hoping to provide reference for the design and evaluation of oral sensory features, and promote drug developing in pediatric population.
Electronic tongue is one kind of bionic detection technologies, which can objectively reflect the taste of drugs based on electrochemical principle. In this paper, the development histories of electronic tongue both of potential type and voltammetry type were introduced, including their detection principles and key innovation technologies. In order to comprehensively improve the understanding of electronic tongue, its technological progresses, such as the study of dedicated sensors or biosensors for specific tastes, and the development of miniaturized or hybrid devices, were also discussed in detail. And the challenges and countermeasures in the application of electronic tongue were analyzed to provide some suggestions for its further technology promotion.
Good palatability of pediatric drugs improves the accuracy of dosing and adherence to dosing regimens. Many active pharmaceutical ingredients have an undesirable taste, so effective taste masking methods need to be developed to improve the palatability of pediatric medicines. This article mainly introduces the commonly taste masking techniques and taste evaluation methods, and puts forward suggestions on the concerns and general principles of the pharmaceutical evaluation of taste masking effects based on cases, in order to provide reference for the development of drug taste masking technology in children.
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