Curcumin, a bioactive compound and vibrant yellow pigment extracted from the rhizome of Curcuma longa, has a well-established safety profile and demonstrates defined pharmacological activities. These activities include regulating glucose and lipid metabolism, exerting anti-oxidant effects, and modulating autophagy. However, its pharmacokinetic limitations-notably low oral bioavailability and insufficient blood concentration-present a dichotomy with its significant biological effects. Research indicates that curcumin undergoes rapid and extensive metabolic transformation in vivo, which suggests that its pharmacological actions may be partially mediated by metabolites. Notably, curcumin metabolites exhibit activity comparable to, or even exceeding, the therapeutic potential of the parent compound in models of glucose and lipid metabolism disorders. Through a systematic review of curcumin's metabolic pathways and the targets of its metabolites, we identified several key conclusions. First, the beneficial effects of curcumin on glucose and lipid metabolism are closely linked to its reduced metabolites dihydrocurcumin, tetrahydrocurcumin, and hexahydrocurcumin. Second, the parent compound curcumin and its metabolites exhibit overlapping actions on core signaling pathways, such as PPARα, NF-κB, and PI3K-AKT, which confirms metabolites as significant contributors to the overall efficacy. Third, preclinical research focusing on these reduced metabolites offers promising new directions for combination therapies targeting glucose and lipid metabolism disorders and their complications. Building upon these conclusions, this paper further synthesizes the structure-activity relationships of the principal reduced metabolite-tetrahydrocurcumin, which is characterized by its high abundance among metabolites and concentrated research focus on its modification, and aims to provide a theoretical foundation for structure optimization and drug development based on metabolites.
Protein kinases (PK) are a class of enzymes that phosphorylate protein molecules and play crucial roles in various biological processes, including cell proliferation, apoptosis, cell cycle regulation, differentiation, and signalling pathways. As essential components of the human body, they have become a major focus in drug development. Consequently, protein kinase inhibitors have emerged as a prominent area of clinical medicine. In recent years, small molecule inhibitors targeting glycogen synthase kinase-3 (GSK3), a representative protein kinase, have been increasingly used in clinical settings. This review comprehensively summarises 26 GSK3β small molecule inhibitors, categorizing them by their therapeutic applications across nine major systemic diseases. It also summarises the structure-activity relationships of several common compounds and examines, through molecular docking, the protein-binding capabilities of highly selective and specific inhibitors, many of which are already in clinical use or nearing clinical entry. By proposing promising research directions and establishing a solid foundation, this work paves the way for developing GSK3β small molecule inhibitors tailored to diverse diseases.
Acute lung injury (ALI) is an intricate clinical disease marked by high mortality and a sudden start. Currently, although there are no specific therapeutics for ALI, the administration of anti-inflammatory drugs is a promising treatment strategy. Curcumol, a terpenoid natural product, has demonstrated significant anti-inflammatory activity. Herein, we designed and synthesised 42 curcumol derivatives using curcumol as the core scaffold. These derivatives underwent in vitro screening for anti-inflammatory activity, and their structure-activity relationship was assessed. Among them, derivative 2 exhibited potent anti-inflammatory potential, inhibiting the expression of inflammatory markers at the nanomolar level. In addition, its water solubility was considerably improved, thereby laying the foundation for enhanced druggability. Derivative 2 also ameliorated lipopolysaccharide (LPS)-induced ALI and reduced pulmonary inflammation at a dose of 5 mg/kg. Proteomics analysis revealed that the anti-inflammatory effect of this compound primarily involved the mTOR signalling pathway. Furthermore, molecular docking and cellular thermal shift assays indicated that GSK3β is a critical target of action of derivative 2, as verified via western blotting. These findings suggest that derivative 2 can be a lead therapeutic compound for ALI, with GSK3β emerging as a promising novel target for the development of specific anti-ALI drugs.
Ideological and political education is a crucial component in talent development,and specialized courses serve as important platforms for implementing this education.This paper focuses on the unique characteristics of the physical chemistry course in traditional Chinese medicine universities and uses the phase diagram of water in the phase equilibrium chapter as an example to explain the design and implementation of ideological and political education in teaching.It explores approaches and methods to effectively integrate ideological and political elements with professional knowledge,aiming to provide valuable insights for incorporating ideological and political education into the teaching of physical chemistry.
A balance between the development and suppression of inflammation can always be found in the body. When this balance is disturbed, a strong inflammatory response can damage the body. It sometimes is necessary to use drugs with a significant anti-inflammatory effect, such as nonsteroidal anti-inflammatory drugs and steroid hormones, to control inflammation in the body. However, the existing anti-inflammatory drugs have many adverse effects, which can be deadly in severe cases, making research into new safer and more effective anti-inflammatory drugs necessary. Currently, numerous types of natural products with anti-inflammatory activity and distinct structural features are available, and these natural products have great potential for the development of novel anti-inflammatory drugs. This review summarizes 260 natural products and their derivatives with anti-inflammatory activities in the last two decades, classified by their active ingredients, and focuses on their structure-activity relationships in anti-inflammation to lay the foundation for subsequent new drug development. We also elucidate the mechanisms and pathways of natural products that exert anti-inflammatory effects via network pharmacology predictions, providing direction for identifying subsequent targets of anti-inflammatory natural products.
OBJECTIVE To evaluate the evidence of domestic progesterone soft capsules for vaginal administration and investigate the melting time, so as to provide basis and reference for prescription review.METHODS The guideline database, Chinese and English literature database and drug administration government websites were systematically searched, and the corresponding literature quality was evaluated according to the Evidence-based Evaluation Specification of Off-label Medication Use. According to the standard of Chinese Pharmacopoeia(2020 Edition), the melting time of domestic progesterone soft capsules was investigated.RESULTS Twenty-nine articles were included in this study. There were 5 guidelines/expert consensus, of which 2 were with high quality(A) and 3 were with low quality(C) assessed by AGREE Ⅱ. There were 6 systematic reviews/Meta-analysis, of which 2 were high-quality, 3 were medium-quality and 1 was low-quality literature evaluated by ASMTAR. The 16 clinical research literature were evaluated by Jadad or NOS scale, of which 10 were high-quality and 6 were low-quality. All the literature confirmed the effectiveness and safety of progesterone vaginal administration. The imported drug description contained the usage and dosage of vaginal administration. The melting time of domestic drug was in accord with the demands of Chinese Pharmacopoeia.CONCLUSION The vaginal administration of domestic progesterone soft capsules has passed the evidence-based medical evidence investigation, and the melting time conforms to the provisions of Chinese Pharmacopoeia. The vaginal administration of domestic progesterone soft capsules should be approved by prescription review.
By reviewing the literature on the efficacy of tannins in traditional Chinese medicine in the last decade or so, we have classified the anti-tumor mechanism of tannins in conjunction with the latest mechanism exploration in the field of oncology. Tannins, a class of multi-phenolic compounds widely present in the diet, have been studied by scholars worldwide in recent years because of their relatively outstanding pharmacological activities. The mechanisms of anti-tumor action of tannins can be summarized as follows: the arrest of the cell cycle, arrest of tumor migration, enhancement of immune competence, induction of apoptosis, and antioxidant effects.
With the rapid development of modern Chinese medicine, basic chemistry experiments have been paid much attention, especially the teaching reform of comprehensive chemical experiments is important. Layered Double Hydroxide(LDH) is a novel type of inorganic functional material, which has become a kind of important drug carrier widely used in the research and development of new dosage forms of active ingredients of Chinese medicine. It has many excellent properties such as acid-base properties, interlayer ion exchange performance and structure memory effect. The preparation and characterization of a novel MgAl LDH colloidal material was introduced.
In recent years, biologically active natural products have gradually become important agents in the field of drug research and development because of their wide availability and variety. However, the target sites of many natural products are yet to be identified, which is a setback in the pharmaceutical industry and has seriously hindered the translation of research findings of these natural products as viable candidates for new drug exploitation. This review systematically describes the commonly used strategies for target identification via the application of probe and non-probe approaches. The merits and demerits of each method were summarized using recent examples, with the goal of comparing currently available methods and selecting the optimum techniques for identifying the targets of bioactive natural products.
2020年春季学期响应党中央疫情期间"停课不停教"的号召,学校有机化学课程采用灵活多样的形式进行线上授课,文章主要介绍腾讯课堂、雨课堂、腾讯会议、钉钉等教学平台在有机化学理论课教学中的应用,以及线上线下混合教学模式在有机化学实验课程教学的探索,全面分析了线上教学方式在有机化学理论以及实验课程中的优劣.
乌氏粘度计法测定高聚物摩尔质量的实验过程中存在的一些不足,本文针对该实验存在的问题进行了改进,设计了一种简单的新型乌氏粘度计组合装置.实践证明,使用改良后的粘度测量装置进行聚乙烯醇的摩尔质量实验时,操作更加便捷,实验误差更小,可获得准确度相对更好的结果.