Chinese Journal of Natural Medicines
·
2025
·
IF 4.9
Yongsheng Fang,Zhiyun Zhu,Chun Xie,Dazhen Xia,Huimin Zhao,Zihui Wang,Qian Lu,Caimei Zhang,Wenyong Xiong,Xiaodong Yang
Saponins associated with Panax notoginseng ( P. notoginseng ) demonstrate significant therapeutic efficacy across multiple diseases. However, certain high-yield saponins face limited clinical applications due to their reduced pharmacological efficacy. This study synthesized and evaluated 36 saponin-1,2,3-triazole derivatives of ginsenosides Rg1/Rb1 and notoginsenoside R1 for anti-adipogenesis activity in vitro . The research revealed that the ginsenosides Rg1-1,2,3-triazole derivative a17 demonstrates superior adipogenesis inhibitory effects. Structure-activity relationships (SARs) analysis indicates that incorporating an amidyl-substituted 1,2,3-triazole into the saponin side chain via Click reaction enhances anti-adipogenesis activity. Additionally, several other derivatives exhibit general adipogenesis inhibition. Compound a17 demonstrated enhanced potency compared to the parent ginsenoside Rg1. Mechanistic investigations revealed that a17 exhibits dose-dependent inhibition of adipogenesis in vitro , accompanied by decreased expression of preadipocytes. Peroxisome proliferator-activated receptor γ (PPARγ), fatty acid synthase (FAS), and fatty acid binding protein 4 (FABP4) adipogenesis regulators. These findings establish the ginsenoside Rg1-1,2,3-triazole derivative a17 as a promising adipocyte differentiation inhibitor and potential therapeutic agent for obesity and associated metabolic disorders. This research provides a foundation for developing effective therapeutic approaches for various metabolic syndromes.
研究领域:
药物化学
·
药理学
·
天然产物
·
生物有机化学
·
代谢性疾病研究
✓ 已验证
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2022
·
IF 6.51
Lu Yang,Tingwei Gu,Yang Xu,Yuda Liu,Yongping Zhang,Zhihong Jiang,Lihua Peng
Natural polysaccharides derived from medicinal plants , that are Dendrobium (DPS), Lycium barbarum (LBP), Ginseng (GPS), and Poria Cocos (PCP) were firstly combined with sodium alginate (SA) to construct microcapsules and improved the morphology, encapsulation efficiency, Biocompatibility and protective capability in drug loading. Diverse typical therapeutics, including VO 2 @ZIF67 nanoparticles , small molecule drugs salvianolic acid B (SaB)/ginsenoside (Rg1), probiotic Bacillus bifidus , and biomacromolecules SDF-1 were wrapped into 1.5 % GPS-0.5 % SA model microcapsules, respectively. Better mobility and formability were significantly observed, and showed 75 % survival rate of probiotics in simulated gastric juice and around 99 % encapsulation efficiency which is higher than single 2 % SA microcapsules. The microcapsules also obtained a delayed release and a higher cell index for SDF-1, which indicated better stability, biocompatibility and protective effect than single 2 % SA microcapsules. This study provides a strategy in developing plant derived polysaccharides as novel materials for the construction and improvement of traditional microcapsules.
研究领域:
药学
·
材料科学
·
生物技术
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF NANOBIOTECHNOLOGY
·
2023
·Vol. 21
·期 1
·1-19
·
IF 10.2
Yuan Tiejun,Tan Minhong,Xu Yang,Xiao Qiyao,Wang Hui,Wu Chen,Li Fulun,Peng Lihua
Wound repair, along with skin appendage regeneration, is challenged by insufficient angiogenesis and neural regeneration. Therefore, promoting both proangiogenic and neuro-regenerative therapeutic effects is essential for effective wound repair. However, most therapeutic systems apply these strategies separately or ineffectively. This study investigates the performance of an all-in-one smart dressing (ASD) that integrates angiogenic functional materials and multiple biological factors within a light crosslinked hydrogel, forming a multi-functional dressing capable of facilitating simultaneous micro-vascularization and neural regeneration. The ASD uses a zeolite-imidazolate framework 67 with anchored vanadium oxide (VO 2 @ZIF-67) that allows for the on-demand release of Co 2+ with fluctuations in pH at the wound site to stimulate angiogenesis. It can simultaneously release CXCL12, ligustroflavone, and ginsenoside Rg1 in a sustained manner to enhance the recruitment of endogenous mesenchymal stem cells, inhibit senescence, and induce neural differentiation to achieve in situ nerve regeneration. The ASD can stimulate rapid angiogenesis and nerve regeneration within 17 days through multiple angiogenic and neuro-regenerative cues within one dressing. This study provides a proof-of-concept for integrating functional nanomaterials and multiple complementary drugs within a smart dressing for simultaneous angiogenesis and neural regeneration.
研究领域:
生物材料
·
组织工程
·
伤口愈合
·
纳米技术
✓ 已验证
产品关联
DOI
PubMed
高影响因子
BIOMEDICINE & PHARMACOTHERAPY
·
2022
·
IF 7.419
Hongqiang Lin,Caixia Wang,Hui Yu,Yunhe Liu,Luying Tan,Shanmei He,Zhuoqiao Li,Cuizhu Wang,Fang Wang,Pingya Li,Jinping Liu
Chronic obstructive pulmonary disease (COPD) is a prevalent respiratory disease. Aiming at assessing the effect of total saponins from American ginseng on COPD, both the chemical composition and anti-COPD activity of total saponins from wild-simulated American ginseng (TSW) and field-grown American ginseng (TSF) were investigated in this study. Firstly, a HPLC-ELSD chromatographic method was established to simultaneously determine the contents of 22 saponins in TSW and TSF. Secondly, CS-induced COPD mouse model was established to evaluate the activity of TSW and TSF. The results indicated that both TSW and TSF had the protective effect against COPD by alleviating oxidative stress and inflammatory response. TSW showed a stronger effect than TSF. Thirdly, an integrated approach involving metabolomics and network pharmacology was used to construct the "biomarker-reaction-enzyme-target" correlation network aiming at further exploring the observed effects. As the results, 15 biomarkers, 9 targets and 5 pathways were identified to play vital roles in the treatment of TSW and TSF on COPD. Fourthly, based on network pharmacology and the CS-stimulated A549 cell model, ginsenoside Rgl, Rc, oleanolic acid, notoginsenoside R1, Fe, silphioside B were certified to be the material basis for the stronger effect of TSW than TSF. Finally, the molecular docking were performed to visualize the binding modes. Our findings suggested that both TSW and TSF could effectively ameliorate the progression of COPD and might be used for the treatment of COPD.
研究领域:
药理学
·
呼吸病学
·
代谢组学
·
网络药理学
·
动物模型
✓ 已验证
DOI
PubMed
高影响因子
CHEMICAL ENGINEERING JOURNAL
·
2025
·
IF 13.2
Xietao Ye,Yeyang Sun,Lin Yang,Chen Chen,Shihao Li,Shuo Dong,Xiaoying Qin,Xiaoqi Li,Congyan Liu,Jiege Huo,Yuping Liu,Yan Chen
The low infiltration and insufficient tumor recognition of cytotoxic-T-lymphocytes (CTLs) are the two primary reasons for the low objective response rate of programmed death-1 protein (PD-1) inhibitors in treating microsatellite-stable colorectal-cancer (MSS-CRC). Ginsenoside Rg1 (Rg1) and atractylenolide-I (Att) can promote CTLs infiltration and recognition of CTLs by facilitating dendritic cells (DCs) maturation and upregulating tumor MHC-I expression, respectively, and the combination of two drugs is expected to improve the efficacy of PD-1 inhibitors. However, due to their poor water solubility and limited tumor targeting, the intratumoral delivery of both drugs faces challenges. Our previously reported a tumor-apoptotic-body-membrane (Ab) modified zeolitic-imidazolate-framework (ZIF) for co-delivering Rg1 and Att (Ab@Rg1/Att-ZIF). It could be transported by monocytes/macrophages into the deep tumor regions, however, partial formulations would be degraded by intracellular lysosomes. To overcome this, we innovatively incorporated inulin into Ab@Rg1/Att-ZIF, constructing an Ab/In@Rg1/Att-ZIF delivery system. By virtue of the Ab and inulin coating on its surface, the system could be specifically phagocytosed by monocytes/macrophages while maintaining stability in the lysosomal. Furthermore, after being transported to CRC tissues, inulin of the Ab/In@Rg1/Att-ZIF is enzymatically degraded by enzymes secreted by intratumoral bacteria, releasing Rg1 and Att to promote DCs maturation and upregulate tumor MHC-I expression, respectively. Ab/In@Rg1/Att-ZIF significantly inhibits tumor growth by enhancing CTLs infiltration and recognition, synergizing with PD-1 inhibitors to achieve a tumor suppression rate of ≈80 %, which is markedly higher than the combined efficacy of Ab@Rg1/Att-ZIF. This study provides new insights for the immunotherapy of MSS-CRC and the intratumoral co-delivery of drugs.
研究领域:
免疫治疗
·
纳米医学
·
药物递送
·
肿瘤学
·
肿瘤微环境
·
癌症免疫学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF ETHNOPHARMACOLOGY
·
2022
·
IF 5.195
Tingting Wang,Xiaoting Huang,Kefeng Zhai,Jialin Yu,Jiaxi Li,Hong Duan,Jinhong Liu,Zhuojian Lu,Jia Guo,Fei Li
Ethnopharmacological relevance Panax japonicus C. A. Meye (PJ) has unique effects on diseases by “qi” stagnation and blood stasis in ancient. Modern studies have shown that PJ can treat diabetic kidney disease (DKD) caused by deficiency and blood stasis. Aim of the study This study evaluated the potential effects of PJ on DKD, a microvascular complication, and investigated its possible mechanisms. Materials and methods In this study, the chemical constituents of PJ were analyzed by HPLC. In vivo studies, we constructed a diabetic mice model by HDF combined with STZ , then administered PJ to diabetic mice for 6 weeks. Blood lipid, BUN, 24h urine protein, and renal tissue HE staining were detected to comprehensively evaluate the protective effect of PJ on DKD. Metabolomics investigated the metabolic pathways influenced by PJ in the treatment of DKD. Moreover, the potential targets and signal pathways were investigated using network pharmacology . Finally, molecular docking predicts affinity of active compounds and core targets, and western blotting was used to detect core target expression levels. Results In vivo study, PJ can reduce hyperlipidemia , serum BUN, and 24-h urinary protein in diabetic mice, and protect the pathological changes in renal tissue. Metabolomics results showed that PJ had significant regulatory effect on unsaturated fatty acids , glycerophospholipid metabolism, and purine metabolism. Network pharmacology showed that MAPK1, MAPK8, Bcl-2, and Caspase 3 were the core targets in PJ against DKD. Molecular docking revealed that Bcl-2 and Caspase 3 have a strong affinity for Chikusetsusaponin Iva , Ginsenoside Rb1 , and Ginsenoside Rg1 . Moreover, when compared to the model group, the PJ group had higher levels of anti-apoptosis protein Bcl-2 and lower levels of pro-apoptosis protein Caspase 3. Conclusion PJ can reduce blood lipids, regulate the biosynthesis of unsaturated fatty acids and purine metabolism, thereby alleviating the renal injury of diabetic mice. Moreover, it can regulate the Bcl-2/caspase 3 apoptosis signaling pathway to prevent the apoptosis of renal cells and protect the renal function of diabetic mice.
研究领域:
药理学
·
代谢组学
·
糖尿病研究
·
分子生物学
·
病理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Advanced Science
·
2024
·
IF 14.3
Xietao Ye,Yuping Liu,Liangyin Wei,Yeyang Sun,Xiaoran Zhang,Hong Wang,Hong Guo,Xiaoying Qin,Xiaoqi Li,Ding Qu,Jiege Huo,Yan Chen
Microsatellite-stable colorectal cancer (MSS-CRC) exhibits resistance to programmed cell death protein-1 (PD-1) therapy. Improving the infiltration and tumor recognition of cytotoxic T-lymphocytes (CTLs) is a promising strategy, but it encounters huge challenges from drug delivery and mechanisms aspects. Here, a zeolitic imidazolate framework (ZIF) coated with apoptotic body membranes derived from MSS-CRC cells is engineered for the co-delivery of ginsenoside Rg1 (Rg1) and atractylenolide-I (Att) to MSS-CRC, named as Ab@Rg1/Att-ZIF. This system is selectively engulfed by Ly-6C + monocytes during blood circulation and utilizes a “hitchhiking” mechanism to migrate toward the core of MSS-CRC. Ab@Rg1/Att-ZIF undergoes rapid disassembly in the tumor, released Rg1 promotes the processing and transportation of tumor antigens in dendritic cells (DCs), enhancing their maturation. Meanwhile, Att enhances the activity of the 26S proteasome complex in tumor cells, leading to increased expression of major histocompatibility complex class-I (MHC-I). These coordinated actions enhance the infiltration and recognition of CTLs in the center of MSS-CRC, significantly improving the tumor inhibition of PD-1 treatment from ≈5% to ≈69%. This innovative design, involving inflammation-guided precise drug co-delivery and a rational combination, achieves synergistic engineering of the tumor microenvironment, providing a novel strategy for successful PD-1 treatment of MSS-CRC.
研究领域:
肿瘤学
·
药学
·
免疫治疗
·
纳米技术
·
癌症生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
LETTERS IN APPLIED MICROBIOLOGY
·
2021
·Vol. 73
·期 6
·779-792
·
IF 2.858
Yang R.,Yin D.,Yang D.,Liu X.,Zhou Q.,Pan Y.,Li J.,Li S.
This study aims to explore the potential mechanisms of Xinnaokang in atherosclerosis treatment. Firstly, the active components of Xinnaokang were analysed by HPLC, which contains ginsenoside Rg1, puerarin, tanshinone, notoginsenoside R1, ammonium glycyrrhizate and glycyrrhizin. Network pharmacology analysis showed there were 145 common targets of Xinnaokang, including the chemical stress, lipid metabolite, lipopolysaccharide, molecules of bacterial origin, nuclear receptor and fluid shear stress pathways. Then, the animal experiment showed that Xinnaokang reduced the body weight and blood lipid levels of atherosclerotic mice. Vascular plaque formation was increased in atherosclerotic mice, which was markedly reversed by Xinnaokang. In addition, Xinnaokang reduced CAV‐1 expression and increased ABCA1, SREBP‐1 and LXR expressions in the vasculature. Xinnaokang promoted SREBP‐2 and LDLR expressions in the liver but decreased IDOL and PCSK9 expressions, indicating that Xinnaokang regulated lipid transport‐related protein expression. Cecal microbiota diversity was reduced in atherosclerotic mice but increased after Xinnaokang treatment. Xinnaokang treatment also improved gut microbiota communities by enriching Actinobacteria, Bifidobacteriales and Bifidobacteriaceae abundances. Metabolic profile showed that Xinnaokang significantly reduced homogentisate, phenylacetylglycine, alanine and methionine expressions in the liver of atherosclerotic mice. Xinnaokang effectively alleviated atherosclerosis, and this effect might be linked with the altered features of the liver metabolite profiles and cecal microbiota.
研究领域:
药理学
·
心血管疾病
·
微生物学
·
代谢组学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）