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Unveiling bioactive components in Sargassum fusiforme via phytochemical and biological evaluation: A heterogeneous information ensemble approach 通过植物化学和生物学评价揭示马尾藻的生物活性成分:一种异构信息集成方法
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2025.08.002
Yue Zhu , Yuting Ai , Jianfu Zhou , Xiaozhuan Jia , Shuying Liu , Bo Zhu , Yimin Qin , Jianping Jiang , Zhenzhong Yang

Objective

Sargassum fusiforme (SF), a brown algae, is a marine traditional Chinese medicine with nutritional value. However, studies on the bioactive components in SF are limited. The aim of this study is to investigate phytochemical and biological properties of SF from different geographical origins and botanical parts, as well as to explore bioactive components within SF.

Methods

SF from different origins and botanical parts were collected for integrated phytochemical analyses using ultra-high performance liquid chromatography-tandem quadrupole time of flight mass spectrometry (UPLC-Q-TOF-MS), mass spectral molecular networking and liquid chromatography-single quadrupole mass spectrometry (LC-MSD), etc., followed by the systematic chemical profile evaluation. Subsequently, the glycolipid metabolism regulation and anticoagulation of SF were examined. Furthermore, the overall information acquired was assembled using multivariate analysis and machine learning to discover bioactive components.

Results

A total of 123 compounds in SF were identified with the assistance of mass spectral molecular networking. The variations in the content of amino acids, fucoidan, alginate, phlorotannin, alkaloids, terpenoids, etc. were observed in SF from different origins and botanical parts. SF possessed the hypolipidemic, hypoglycemic and anticoagulant effects, and SF from Dongtou, Wenzhou, Zhejiang, was outstanding among origins in both phytochemical and biological evaluations. A heterogeneous information ensemble approach was adopted to discover the bioactive components in SF, namely 3-indoleacrylic acid, phlorotannin and fucoidan.

Conclusion

This study evaluated the phytochemical and biological properties of SF, revealed the bioactive components using heterogeneous information and provided a reference for the rational consumption and further development of SF.
目的褐藻褐藻是一种具有营养价值的海洋中药。然而,对顺丰中生物活性成分的研究有限。本研究的目的是研究不同地理来源和植物部位的顺丰的植物化学和生物学特性,并探索顺丰的生物活性成分。方法采用超高效液相色谱-串联四极杆飞行时间质谱(UPLC-Q-TOF-MS)、质谱分子网络和液相色谱-单四极杆质谱(LC-MSD)等方法对不同来源和植物部位的ssf进行综合分析,并进行系统化学谱分析。观察SF对糖脂代谢的调节作用和抗凝作用。此外,使用多变量分析和机器学习来组装获得的总体信息,以发现生物活性成分。结果通过质谱分子网络鉴定出SF中123个化合物。不同产地、不同植物部位的木香中氨基酸、褐藻聚糖、海藻酸盐、绿藻单宁、生物碱、萜类化合物等含量存在差异。顺丰具有降血脂、降血糖和抗凝血作用,浙江温州东头顺丰在植物化学和生物学评价方面均表现优异。采用异构信息集成方法发现了SF中的生物活性成分,即3-吲哚丙烯酸、褐藻单宁和岩藻聚糖。结论本研究评价了顺丰的植物化学和生物学特性,利用异构信息揭示了顺丰的生物活性成分,为顺丰的合理消费和进一步开发提供了参考。
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引用次数: 0
Therapeutic potential and mechanisms of traditional Chinese medicine in regulating energy metabolism imbalance in heart failure 中药调节心力衰竭能量代谢失衡的治疗潜力及机制
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2025.07.002
Ailian Li , Xuexi Wang , Ruoyu Yang , Jingping Zhang , Xiaotong Jiang
Heart failure (HF) is a disease in which the heart fails to efficiently pump blood due to diminished cardiac function, which seriously affects the quality of life and prognosis of patients. In recent years, traditional Chinese medicine (TCM), as a national treasure of China, has been shown to regulate cardiac energy metabolism and has been widely used in the treatment of HF. This article summarised commonly used TCMs for the treatment of HF, mainly from the perspective of improving energy metabolism. The results showed that TCMs can enhance the cardiac energy supply and improve cardiac function by altering the heart’s preference for metabolic substrates, regulating the activity of key metabolic enzymes and the expression of related proteins, and attenuating impaired mitochondrial function. Among them, Astragali Radix (Huangqi in Chinese), Ginseng Radix et Rhizoma (Renshen in Chinese), Salviae Miltiorrhizae Radix et Rhizoma (Danshen in Chinese), and their extracts can exert significant cardioprotective effects. In addition, some TCM herbal formulas, such as Shengmai San and Zhenwu Tang, have been widely used in the treatment of HF. The application of these herbal extracts and formulas provides an effective option for the treatment of HF, but further studies are needed to clarify their mechanisms of action and clinical applications.
心衰(Heart failure, HF)是一种由于心功能下降导致心脏不能有效泵血的疾病,严重影响患者的生活质量和预后。近年来,中药作为中国的国宝,已被证明具有调节心脏能量代谢的作用,并被广泛应用于心衰的治疗。本文主要从改善能量代谢的角度,对治疗心衰的常用中药进行综述。结果表明,中药可通过改变心脏对代谢底物的偏好、调节关键代谢酶的活性和相关蛋白的表达、减弱线粒体功能受损,从而增强心脏能量供应,改善心功能。其中,黄芪、人参、丹参及其提取物具有显著的心脏保护作用。此外,生脉散、真武汤等中药方剂已被广泛应用于心衰的治疗。这些草药提取物和配方的应用为治疗心衰提供了一种有效的选择,但其作用机制和临床应用尚需进一步研究。
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引用次数: 0
Jiaotaiwan activates serum SCFAs and upregulates cAMP-PKA-CREB-BDNF signaling pathway for antidepressant effects: A multicenter, randomized, controlled study 交台活化血清SCFAs及上调cAMP-PKA-CREB-BDNF信号通路的抗抑郁作用:一项多中心、随机对照研究
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2025.03.002
Mengnan Huang , Yuanyuan He , Tong Yang , Lu Yu , Qina Lei , Lina Gao , Shan Gao , Lin Li , Chunquan Yu

Objective

Jiaotaiwan (JTW) is a classic traditional Chinese medicine (TCM) prescription for treating depression, but its potential mechanisms are not fully understood. The aim of this study is to detect the levels of serum Short-chain fatty acids (SCFAs) and cyclic adenosine monophosphate (cAMP)-protein kinase A (PKA)-cAMP-response element binding protein (CREB)-brain derived neurotrophic factor (BDNF) signaling pathway, further revealing the scientific connotation of the antidepressant effect of JTW.

Methods

In this multicenter, randomized, controlled study, 120 patients with depression were divided into the JTW (16.5 g/d) group, JTW (16.5 g/d) + selective serotonin reuptake inhibitors (SSRIs) group, and SSRIs group. Hamilton depression Scale-24 (HAMD-24) and Self-rating depression scale (SDS) were used for efficacy evaluation. Enzyme linked immunosorbent assay (ELISA) and reverse transcription-polymerase chain reaction (RT-PCR) were used to evaluate the expression levels of cAMP-PKA-CREB-BDNF signaling pathway. Serum SCFAs concentrations were analyzed using liquid chromatograph-mass spectrometer (LC-MS) targeted metabolomics.

Results

After eight weeks of treatment, HAMD score and SDS score were significantly decreased in the three groups, and HAMD score in JTW + SSRIs group was significantly lower than that in SSRIs group. After treatment, the expression levels of cAMP-PKA-CREB-BDNF signaling pathway were significantly increased in the three group, with the JTW + SSRIs group showing more significant increase. After treatment, the levels of isobutyric, butyric, isovaleric, and valeric acids in the JTW + SSRIs groups were significantly higher than that before treatment, and the levels of isobutyric, and isovaleric acids in the JTW + SSRIs group was significantly higher than that in the JTW group and SSRIs groups.

Conclusion

JTW can alleviate symptoms in patients with depression, and its antidepressant mechanism may be related to regulating serum SCFAs and cAMP-PKA-CREB-BDNF signaling pathway.
目的交台是治疗抑郁症的经典中药方剂,但其作用机制尚不完全清楚。本研究旨在检测血清短链脂肪酸(SCFAs)水平及环磷酸腺苷(cAMP)-蛋白激酶A (PKA)-cAMP-反应因子结合蛋白(CREB)-脑源性神经营养因子(BDNF)信号通路水平,进一步揭示JTW抗抑郁作用的科学内涵。方法采用多中心随机对照研究方法,将120例抑郁症患者分为JTW (16.5 g/d)组、JTW (16.5 g/d) +选择性5 -羟色胺再摄取抑制剂(SSRIs)组和SSRIs组。采用汉密尔顿抑郁量表-24 (HAMD-24)和抑郁自评量表(SDS)进行疗效评价。采用酶联免疫吸附法(ELISA)和逆转录聚合酶链反应(RT-PCR)检测cAMP-PKA-CREB-BDNF信号通路的表达水平。采用液相色谱-质谱(LC-MS)靶向代谢组学分析血清SCFAs浓度。结果治疗8周后,三组患者HAMD评分和SDS评分均显著降低,且JTW + SSRIs组HAMD评分显著低于SSRIs组。治疗后,三组cAMP-PKA-CREB-BDNF信号通路表达水平均显著升高,其中JTW + SSRIs组升高更为显著。治疗后,JTW + SSRIs组的异丁酸、丁酸、异戊酸、戊酸水平均显著高于治疗前,且JTW + SSRIs组的异丁酸、异戊酸水平显著高于JTW组和SSRIs组。结论jtw可缓解抑郁症患者的症状,其抗抑郁机制可能与调节血清SCFAs及cAMP-PKA-CREB-BDNF信号通路有关。
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引用次数: 0
Natural compounds from traditional Chinese medicine regulating stem cell fate: Identification and therapeutic potential 调节干细胞命运的中药天然化合物:鉴定和治疗潜力
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2025.05.002
Zhigao Zhao , Yu Ma , Shizhe Wang , Mengyuan Zhou , Yang Tian , Li Yang , Jian Gu , Rui Tan
The problems of uncontrolled stem cell differentiation and the limited number of cells available represent significant obstacles to the advancement of stem cell research in the medical field. It is therefore imperative to control the potential of stem cells and to develop effective methods to regulate stem cell fate. A number of natural products derived from TCM have been shown to provide valuable insights into the regulation of biological signals and epigenetic mechanisms in stem cells. Furthermore, the structural modification of these natural products by synthetic means promises to unlock a wealth of possibilities in the field of precision regenerative medicine. However, a systematic and comprehensive review of these natural products has yet to be conducted. This article presents an overview of the natural products that have been identified as regulating the fate of stem cells. It includes a discussion of the classification, mechanism of action, and current prospects for the application of these natural products as lead compounds. This provides valuable insights for the advancement of TCM modernization and internationalization, precision regenerative medicine involving natural products and stem cells, the discovery of green lead compounds, and the development of new drugs.
干细胞分化不受控制和可用细胞数量有限的问题是医学领域干细胞研究进展的重大障碍。因此,控制干细胞的潜力和开发有效的方法来调节干细胞的命运是势在必行的。许多来自中药的天然产物已被证明对干细胞的生物信号调控和表观遗传机制提供了有价值的见解。此外,通过合成手段对这些天然产物进行结构修饰,有望在精密再生医学领域开启丰富的可能性。然而,对这些天然产物的系统和全面的审查尚未进行。这篇文章介绍了已经确定的调节干细胞命运的天然产物的概述。它包括对这些天然产物作为先导化合物的分类、作用机制和目前应用前景的讨论。这为推进中医药现代化和国际化、涉及天然产物和干细胞的精准再生医学、绿色先导化合物的发现和新药的开发提供了宝贵的见解。
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引用次数: 0
Exploration of chemical components and Rac1-dependent anti-hepatic fibrosis mechanism by total flavonoids derived from Tetrastigma hemsleyanum 赤柱总黄酮化学成分及rac1依赖性抗肝纤维化机制的探索
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2024.12.003
Xin Wu , Cuiwei Chen , Hongyan Zhang , Keda Lu , Gang Cao

Objective

This study is mainly to elucidate the characteristic components, hepatoprotective effect, and the underlying anti-hepatic fibrosis molecular mechanism of the total flavonoids of Tetrastigma hemsleyanum Diels & Gilg (SYQTF).

Methods

The components of SYQTF were confirmed based on global natural products social molecular networking (GNPS) as well as the hepatoprotective effect on CCl4-induced acute liver injury. Cell toxicity and viability, cell cycle, and apoptosis analyses were then performed to determine the effects of SYQTF in transforming growth factor-β1 (TGF-β1) (10 ng/mL)-induced HSC-T6 hepatic fibrosis cell model. Finally, the lentiviral particles to package recombinant Ras-related C3 botulinum toxin substrate 1 (Rac1) over-expression and Rac1 knockdown plasmids were transfected into TGF-β1-induced HSC-T6 cells to elucidate the mechanism of anti-hepatic fibrosis of SYQTF targeting Rac1, respectively.

Results

Our findings demonstrated that 86 components in SYQTF were identified in MSE and FastDDA mode with the aid of GNPS. Moreover, S15-ZJ, the genuine functional food and medicinal materials of T. hemsleyanum, was significantly different from other regions by multivariate statistical methods based on progenesis QI. Remarkably, kaempferol-3-O-furananose7-O-rhamnosyl-glucoside, the highest response intensity in S15-ZJ, may act as the potential Q-marker of genuine functional food and medicinal materials of T. hemsleyanum in Zhejiang Province distinguished from other areas. In addition, the in vivo experiments revealed that SYQTF greatly alleviated CCl4-induced acute liver injury. Furthermore, SYQTF can reversible the activation and proliferation of HSC-T6 cells, block the cell cycle in the G0/G1 phase, and promote cell apoptosis. Remarkably, the study is the first to reveal that SYQTF exhibited the anti-hepatic fibrosis effect through targeting Rac1 in the hedgehog signaling pathway.

Conclusion

Rac1 is an important signaling molecule for the activation of the hedgehog pathway in HSC-T6. Importantly, SYQTF exerted its anti-hepatic fibrosis effect by inhibiting the Rac1-hedgehog signaling pathway. Furthermore, kaempferol-3-O-furananose7-O-rhamnosyl-glucoside could be a potential Q-marker of T. hemsleyanum in Zhejiang Province distinguished from other areas.
目的研究赤藓总黄酮(Tetrastigma hemsleyanum Diels & Gilg, SYQTF)的特征成分、肝保护作用及抗肝纤维化分子机制。方法基于全球天然产物社会分子网络(GNPS)对SYQTF的成分进行确认,并对ccl4诱导的急性肝损伤进行肝保护作用。通过细胞毒性、细胞活力、细胞周期和细胞凋亡分析,确定SYQTF对转化生长因子-β1 (TGF-β1) (10 ng/mL)诱导的HSC-T6肝纤维化细胞模型的影响。最后,将包装重组ras相关C3肉毒毒素底物1 (Rac1)过表达质粒和Rac1敲低质粒的慢病毒颗粒转染TGF-β1诱导的HSC-T6细胞,分别阐明SYQTF靶向Rac1抗肝纤维化的机制。结果利用GNPS在MSE和FastDDA模式下共鉴定出86个SYQTF成分。此外,基于子代气的多元统计方法显示,正品功能性食药药材赤柱S15-ZJ与其他地区差异显著。值得注意的是,山奈酚-3- o -呋喃糖- 7- o -鼠李糖-葡萄糖苷在S15-ZJ中响应强度最高,可作为浙江省区别于其他地区正品功能食品和药材的潜在q标记物。此外,体内实验显示SYQTF可显著减轻ccl4诱导的急性肝损伤。SYQTF可逆转HSC-T6细胞的活化和增殖,阻断G0/G1期细胞周期,促进细胞凋亡。值得注意的是,本研究首次发现SYQTF通过靶向hedgehog信号通路中的Rac1发挥抗肝纤维化作用。结论rac1是HSC-T6中激活hedgehog通路的重要信号分子。重要的是,SYQTF通过抑制Rac1-hedgehog信号通路发挥其抗肝纤维化作用。山奈酚-3- o -呋喃葡萄糖- 7- o -鼠李糖糖苷可能是浙江省与其他地区区分的潜在q标记。
{"title":"Exploration of chemical components and Rac1-dependent anti-hepatic fibrosis mechanism by total flavonoids derived from Tetrastigma hemsleyanum","authors":"Xin Wu ,&nbsp;Cuiwei Chen ,&nbsp;Hongyan Zhang ,&nbsp;Keda Lu ,&nbsp;Gang Cao","doi":"10.1016/j.chmed.2024.12.003","DOIUrl":"10.1016/j.chmed.2024.12.003","url":null,"abstract":"<div><h3>Objective</h3><div>This study is mainly to elucidate the characteristic components, hepatoprotective effect, and the underlying anti-hepatic fibrosis molecular mechanism of the total flavonoids of <em>Tetrastigma hemsleyanum</em> Diels &amp; Gilg (SYQTF).</div></div><div><h3>Methods</h3><div>The components of SYQTF were confirmed based on global natural products social molecular networking (GNPS) as well as the hepatoprotective effect on CCl<sub>4</sub>-induced acute liver injury. Cell toxicity and viability, cell cycle, and apoptosis analyses were then performed to determine the effects of SYQTF in transforming growth factor-<em>β</em>1 (TGF-<em>β</em>1) (10 ng/mL)-induced HSC-T6 hepatic fibrosis cell model. Finally, the lentiviral particles to package recombinant Ras-related C3 botulinum toxin substrate 1 (Rac1) over-expression and Rac1 knockdown plasmids were transfected into TGF-β1-induced HSC-T6 cells to elucidate the mechanism of anti-hepatic fibrosis of SYQTF targeting Rac1, respectively.</div></div><div><h3>Results</h3><div>Our findings demonstrated that 86 components in SYQTF were identified in MS<sup>E</sup> and FastDDA mode with the aid of GNPS. Moreover, S<sub>15</sub>-ZJ, the genuine functional food and medicinal materials of <em>T. hemsleyanum</em>, was significantly different from other regions by multivariate statistical methods based on progenesis QI. Remarkably, kaempferol-3-<em>O</em>-furananose7-<em>O</em>-rhamnosyl-glucoside, the highest response intensity in S<sub>15</sub>-ZJ, may act as the potential Q-marker of genuine functional food and medicinal materials of <em>T. hemsleyanum</em> in Zhejiang Province distinguished from other areas. In addition, the <em>in vivo</em> experiments revealed that SYQTF greatly alleviated CCl<sub>4</sub>-induced acute liver injury. Furthermore, SYQTF can reversible the activation and proliferation of HSC-T6 cells, block the cell cycle in the G<sub>0</sub>/G<sub>1</sub> phase, and promote cell apoptosis. Remarkably, the study is the first to reveal that SYQTF exhibited the anti-hepatic fibrosis effect through targeting Rac1 in the hedgehog signaling pathway.</div></div><div><h3>Conclusion</h3><div>Rac1 is an important signaling molecule for the activation of the hedgehog pathway in HSC-T6. Importantly, SYQTF exerted its anti-hepatic fibrosis effect by inhibiting the Rac1-hedgehog signaling pathway. Furthermore, kaempferol-3-<em>O</em>-furananose7-<em>O</em>-rhamnosyl-glucoside could be a potential Q-marker of <em>T. hemsleyanum</em> in Zhejiang Province distinguished from other areas.</div></div>","PeriodicalId":9916,"journal":{"name":"Chinese Herbal Medicines","volume":"17 4","pages":"Pages 837-849"},"PeriodicalIF":8.9,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145339827","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
NLRP3 inflammasome in acute lung injury: Cumulative evidence for traditional Chinese medicine and natural products 急性肺损伤中的NLRP3炎性体:中药和天然产物的累积证据
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2025.06.002
Yiman Liu , Junyu Meng , Jia Liu, Fan Zhang, Chen An, Jian Yang
Acute lung injury (ALI) and its more severe manifestation, acute respiratory distress syndrome (ARDS), continue to pose a substantial challenge for contemporary society. Having been linked to the processes of injury and inflammation, NLRP3 inflammasome is activated by various stimuli, including inhaled allergens, pathogens, and environmental pollutants, subsequently contributing to the dysfunction of the innate immune system. Understanding how the innate immune NLRP3 inflammasome is altered during ALI may facilitate the identification of new therapeutic targets. To further enrich the role of NLRP3 inflammasome in treating ALI with traditional Chinese Medicine (TCM), this review aims to thoroughly summarize the latest scientific research achievements on the effects of NLRP3 inflammasome in ALI, and the existing underlying therapeutic targets from TCM and natural products.
急性肺损伤(ALI)及其更严重的表现——急性呼吸窘迫综合征(ARDS),继续对当代社会构成重大挑战。NLRP3炎性小体与损伤和炎症过程有关,可被各种刺激激活,包括吸入的过敏原、病原体和环境污染物,从而导致先天免疫系统功能障碍。了解先天免疫NLRP3炎症小体在ALI期间是如何改变的,可能有助于确定新的治疗靶点。为了进一步丰富NLRP3炎性小体在中药治疗ALI中的作用,本文旨在全面总结NLRP3炎性小体在ALI中作用的最新科学研究成果,以及现有中药和天然产物的潜在治疗靶点。
{"title":"NLRP3 inflammasome in acute lung injury: Cumulative evidence for traditional Chinese medicine and natural products","authors":"Yiman Liu ,&nbsp;Junyu Meng ,&nbsp;Jia Liu,&nbsp;Fan Zhang,&nbsp;Chen An,&nbsp;Jian Yang","doi":"10.1016/j.chmed.2025.06.002","DOIUrl":"10.1016/j.chmed.2025.06.002","url":null,"abstract":"<div><div>Acute lung injury (ALI) and its more severe manifestation, acute respiratory distress syndrome (ARDS), continue to pose a substantial challenge for contemporary society. Having been linked to the processes of injury and inflammation, NLRP3 inflammasome is activated by various stimuli, including inhaled allergens, pathogens, and environmental pollutants, subsequently contributing to the dysfunction of the innate immune system. Understanding how the innate immune NLRP3 inflammasome is altered during ALI may facilitate the identification of new therapeutic targets. To further enrich the role of NLRP3 inflammasome in treating ALI with traditional Chinese Medicine (TCM), this review aims to thoroughly summarize the latest scientific research achievements on the effects of NLRP3 inflammasome in ALI, and the existing underlying therapeutic targets from TCM and natural products.</div></div>","PeriodicalId":9916,"journal":{"name":"Chinese Herbal Medicines","volume":"17 4","pages":"Pages 703-719"},"PeriodicalIF":8.9,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145340097","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ganoderic acid a derivative induces apoptosis of cervical cancer cells by inhibiting JNK pathway 灵芝酸 A 衍生物通过抑制 JNK 通路诱导宫颈癌细胞凋亡
IF 8.9 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-10-01 DOI: 10.1016/j.chmed.2024.07.002
Mengchen Wang , Qin Han , Xuelian Zhang , Xi Dong , Jiadong Ran , Fei Wei , Yun Luo , Xiaobo Sun

Objective

Ganoderic acid A can inhibit the proliferation and promotes the apoptosis of cancer cells. Surprisingly, the molecular mechanisms underlying the anti-cancer effects of ganoderic acid A still remain poorly defined. Ganoderic acid A derivative (GaAD19) is an effective ingredient obtained by structural modification of ganoderic acid A. The purpose of this study was to evaluate the anti-proliferation effect of GaAD19 on cervical cancer cells.

Methods

Through the HeLa cervical cancer cell model, the drug target of GaAD19 was predicted using the SwissTargetPrediction database and molecular docking. Subsequently, computer analysis results were verified by a series of molecular biology experiments, such as flow cytometry, Western blot, immunocytochemical staining, terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL), quantitative real time polymerase chain reaction (qPCR), and so on. Then, pathway agonists and inhibitors were used to investigate the mechanism of GaAD19. Finally, the mouse model of cervical cancer was established to evaluate the inhibitory effect of GaAD19 on tumor growth in U14 cervical cancer mice.

Results

GaAD19 induced apoptosis and inhibited the growth of tumors. It also blocked the transition from the G1 to the S phase of the cell cycle. However, in the presence of a c-Jun N-terminal kinase (JNK)agonist, the effects of GaAD19 on the proliferation, apoptosis, and cell cycle transition of cancer cells were suppressed.

Conclusion

This study showed that GaAD19 can play an anti-cervical cancer role by inhibiting the JNK signaling pathway. These results will be helpful in further exploring the mechanism of GaAD19 in the treatment of cervical cancer.
目的:阳极酸A具有抑制肿瘤细胞增殖、促进肿瘤细胞凋亡的作用。令人惊讶的是,灵芝酸A抗癌作用的分子机制仍然不明确。Ganoderic acid A衍生物(GaAD19)是对Ganoderic acid A进行结构修饰得到的一种有效成分。本研究的目的是评价GaAD19对宫颈癌细胞的抗增殖作用。方法通过HeLa宫颈癌细胞模型,利用SwissTargetPrediction数据库和分子对接预测GaAD19的药物靶点。随后,通过流式细胞术、Western blot、免疫细胞化学染色、末端脱氧核苷酸转移酶介导的dUTP缺口末端标记(TUNEL)、定量实时聚合酶链反应(qPCR)等一系列分子生物学实验验证计算机分析结果。然后,利用途径激动剂和抑制剂研究GaAD19的作用机制。最后建立宫颈癌小鼠模型,评价GaAD19对U14宫颈癌小鼠肿瘤生长的抑制作用。结果gaad19诱导细胞凋亡,抑制肿瘤生长。它还阻断了细胞周期从G1期到S期的转变。然而,在c-Jun n -末端激酶(JNK)激动剂存在下,GaAD19对癌细胞增殖、凋亡和细胞周期转变的影响被抑制。结论GaAD19可通过抑制JNK信号通路发挥抗宫颈癌作用。这些结果将有助于进一步探索GaAD19在宫颈癌治疗中的作用机制。
{"title":"Ganoderic acid a derivative induces apoptosis of cervical cancer cells by inhibiting JNK pathway","authors":"Mengchen Wang ,&nbsp;Qin Han ,&nbsp;Xuelian Zhang ,&nbsp;Xi Dong ,&nbsp;Jiadong Ran ,&nbsp;Fei Wei ,&nbsp;Yun Luo ,&nbsp;Xiaobo Sun","doi":"10.1016/j.chmed.2024.07.002","DOIUrl":"10.1016/j.chmed.2024.07.002","url":null,"abstract":"<div><h3>Objective</h3><div>Ganoderic acid A can inhibit the proliferation and promotes the apoptosis of cancer cells. Surprisingly, the molecular mechanisms underlying the anti-cancer effects of ganoderic acid A still remain poorly defined. Ganoderic acid A derivative (GaAD19) is an effective ingredient obtained by structural modification of ganoderic acid A. The purpose of this study was to evaluate the anti-proliferation effect of GaAD19 on cervical cancer cells.</div></div><div><h3>Methods</h3><div>Through the HeLa cervical cancer cell model, the drug target of GaAD19 was predicted using the SwissTargetPrediction database and molecular docking. Subsequently, computer analysis results were verified by a series of molecular biology experiments, such as flow cytometry, Western blot, immunocytochemical staining, terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL), quantitative real time polymerase chain reaction (qPCR), and so on. Then, pathway agonists and inhibitors were used to investigate the mechanism of GaAD19. Finally, the mouse model of cervical cancer was established to evaluate the inhibitory effect of GaAD19 on tumor growth in U14 cervical cancer mice.</div></div><div><h3>Results</h3><div>GaAD19 induced apoptosis and inhibited the growth of tumors. It also blocked the transition from the G<sub>1</sub> to the S phase of the cell cycle. However, in the presence of a c-Jun <em>N</em>-terminal kinase (JNK)agonist, the effects of GaAD19 on the proliferation, apoptosis, and cell cycle transition of cancer cells were suppressed.</div></div><div><h3>Conclusion</h3><div>This study showed that GaAD19 can play an anti-cervical cancer role by inhibiting the JNK signaling pathway. These results will be helpful in further exploring the mechanism of GaAD19 in the treatment of cervical cancer.</div></div>","PeriodicalId":9916,"journal":{"name":"Chinese Herbal Medicines","volume":"17 4","pages":"Pages 756-767"},"PeriodicalIF":8.9,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141839901","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Coptis chinensis shows distinct effects on hyperlipidemia and gut microbiota in high-fat diet induced mice with cold or hot syndrome 黄连对高脂饮食引起的寒、热证小鼠高脂血症和肠道菌群有明显的影响
IF 4.7 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-07-01 DOI: 10.1016/j.chmed.2025.04.009
Yanan Yang , Jiaguo Zhan , Jiale Cheng , Ying Cao , Chongming Wu

Objective

Coptis chinensis (Huanglian in Chinese, HL) is commonly utilized in clinical settings to counteract dyslipidemia in patients with hot syndrome. Its lipid-reducing efficacy has been consistently demonstrated in high-fat diet (HFD)-induced hyperlipidemic animal models. However, whether HL’s efficacy differs in HFD-fed animals with hot or cold syndromes remains unclear. This study aims to discern the variations in the anti-hyperlipidemic effects of HL in HFD-fed mice with hot or cold syndromes.

Methods

HFD-induced C57BL/6 mice were subjected to cold or hot syndrome via two weeks of ice water (0 °C) and levothyroxine sodium (240 µg/kg) treatment, respectively. Then, an aqueous extract of HL was administered to the mice via oral gavage over the following four-week period. Lipid levels in the serum and liver were gauged to determine the lipid-reducing effects of HL. Furthermore, gut microbiota composition was elucidated using full-length 16S rRNA gene sequencing.

Results

HL notably reduced lipid levels in HFD-induced hyperlipidemic mice. Its efficacy was amplified in hyperlipidemic mice with a hot syndrome but was markedly reduced in those with a cold syndrome. HL treatment led to a decline in alpha-diversity (characterized by ACE, Chao1, Shannon and Simpson index) of the gut microbiota in both sets of mice but affected specific microbial populations based on the syndrome. Specifically, while HL led to a notable increase in Eubacterium, Robinsoniella, and Lachnoclostridium genera, along with the enhancement of Clostridium innocuum and Bacteroides thetaiotaomicron species across all conditions, it syndrome-dependently stimulated Romboutsia ilealis and Parabaceroides_sp_HGS0025 species in mice with hot syndrome.

Conclusion

HL shows stronger lipid-lowering effect on hyperlipidemic mice with hot syndrome, which is in accordance with its traditional usage in clinic. The therapeutic outcomes of HL are intrinsically tied, at least in part, to its modulatory effects on the gut microbiota, offering fresh insights into the foundational principles of traditional Chinese medicine.
目的黄连中药是临床治疗热证患者血脂异常的常用中药。其降脂功效已在高脂饮食(HFD)诱导的高脂血症动物模型中得到一致证明。然而,hfd喂养的热证或寒证动物是否有不同的疗效尚不清楚。本研究旨在探讨HL在热证和寒证小鼠中抗高脂血症作用的变化。方法将shfd诱导的C57BL/6小鼠分别以冰水(0°C)和左旋甲状腺素钠(240µg/kg)处理2周,形成冷证和热证。然后,在接下来的四周时间里,通过灌胃给小鼠HL的水提取物。测定血清和肝脏中的脂质水平,以确定HL的降脂作用。此外,利用16S rRNA基因全长测序技术对肠道菌群组成进行了分析。结果shl可显著降低hfd诱导的高脂血症小鼠的脂质水平。它的功效在热证高脂血症小鼠中被放大,但在寒证小鼠中被显著降低。HL治疗导致两组小鼠肠道菌群α -多样性(以ACE、Chao1、Shannon和Simpson指数为特征)下降,但基于综合征的特定微生物种群受到影响。具体而言,在所有条件下,HL均能显著增加真菌菌属、Robinsoniella属和Lachnoclostridium属,以及无毒梭菌属(Clostridium innocuum)和拟杆菌属(Bacteroides thetaiotaomicron)属的数量,但在热证小鼠中,HL可刺激回肠Romboutsia和Parabaceroides_sp_HGS0025种。结论黄芪对高脂血症热证小鼠有较强的降脂作用,符合其临床传统用法。HL的治疗结果本质上与它对肠道微生物群的调节作用有关,至少在一定程度上,这为传统中医的基本原理提供了新的见解。
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引用次数: 0
Curcumae Rhizoma: An anti-cancer traditional Chinese medicine 姜黄:一种抗癌中药
IF 4.7 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-07-01 DOI: 10.1016/j.chmed.2025.04.006
Yu Luo , Lin Zhu , Zhengyu Ren , Jian Xiao , Erwei Hao , Jiahong Lu , Jinmin Zhao , Chun Yao , Yitao Wang , Hua Luo
Curcumae Rhizoma, derived from the rhizome of Curcuma phaeocaulis, Curcuma kwangsiensis and Curcuma wenyujin, was called Ezhu in China. In the past, Curcumae Rhizoma extracts were obtained through water decoction or alternative methods, which showed significant anti-cancer effects. However, the mixed extracts contain various compound components of Curcumae Rhizoma, leading to an ambiguous mechanism of action for Curcumae Rhizoma extracts anti-cancer. Contemporary researchers have extracted the chemical components of Curcumae Rhizoma separately for experimental verification of its active ingredients in the anti-cancer field. Numerous studies demonstrated that curcumol, germacrone, β-elemene, and curcumin in Curcumae Rhizoma extracts have significant governing effects in anti-cancer activities. Pharmacological studies have shown that Curcumae Rhizoma suppresses cancer cell proliferation, invasion, and migration, triggering apoptosis and regulating cellular autophagy to achieve anticancer effects. Here, we summarized the research progress of Curcumae Rhizoma on anti-cancer effects from 2013 to 2022, aiming to explore the deeper molecular mechanisms of Curcumae Rhizoma’s active components in cancer treatment.
姜黄(Curcumae Rhizoma)是由黄姜黄(Curcuma phaeocaulis)、黄姜黄(Curcuma kwangsiensis)和文榆金姜黄(Curcuma wenyujin)的根茎衍生而来,中国称莪术。过去,姜黄提取物通过水煎或替代方法获得,具有显著的抗癌作用。然而,混合提取物中含有多种姜黄的复合成分,导致姜黄提取物的抗癌作用机制不明确。当代研究者分别提取了姜黄的化学成分,对其在抗癌领域的有效成分进行了实验验证。大量研究表明,姜黄提取物中的姜黄酚、germacone、β-榄香烯和姜黄素具有显著的抗癌作用。药理研究表明,姜黄可抑制癌细胞的增殖、侵袭和迁移,触发细胞凋亡,调节细胞自噬,达到抗癌作用。本文总结了2013 - 2022年姜黄抗癌作用的研究进展,旨在探讨姜黄有效成分治疗癌症的更深层次分子机制。
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引用次数: 0
Unveiling secrets of traditional Chinese medicine: Cutting-edge techniques in component analysis 揭开中药的秘密:成分分析的尖端技术
IF 4.7 4区 医学 Q1 CHEMISTRY, MEDICINAL Pub Date : 2025-07-01 DOI: 10.1016/j.chmed.2025.05.006
Tingting Zhou
Chemical component analysis is a critical challenge in Chinese herbal medicine research, involving the qualitative and quantitative identification of complex constituents in traditional Chinese medicine (TCM). However, traditional analytical methods are insufficient for efficient and comprehensive analysis of complex composition of TCM. Limitations exist in sample preparation, instrumental technology, data processing, and activity-related quality marker research. Recent advancements have significantly improved analytical precision, enabling more comprehensive profiling of TCM components. New pretreatment methods improve extraction efficiency and detection sensitivity, while novel instrumental technologies, such as mass spectrometry imaging, preserve spatial information lost in homogenization. AI enhances data interpretation, improving accuracy and efficiency. Online activity analysis links chemical composition with bioactivity, overcoming the limitations of purely chemical profiling and enabling a more comprehensive evaluation of TCM efficacy. This perspective provides an overview of the development trends in component analysis, aiming to advance the field and support TCM modernization.
化学成分分析是中药研究中的一个重要课题,涉及中药复杂成分的定性和定量鉴定。然而,传统的分析方法不足以对中药复杂成分进行高效、全面的分析。在样品制备、仪器技术、数据处理和与活动相关的质量标记研究方面存在局限性。最近的进展显著提高了分析精度,使中药成分的分析更加全面。新的预处理方法提高了提取效率和检测灵敏度,而新的仪器技术,如质谱成像,保留了均质化过程中丢失的空间信息。人工智能增强了数据解释,提高了准确性和效率。在线活性分析将化学成分与生物活性联系起来,克服了纯化学分析的局限性,使中药疗效的评估更加全面。这一视角概述了成分分析的发展趋势,旨在推动该领域的发展,支持中医药现代化。
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引用次数: 0
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Chinese Herbal Medicines
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