摘要:
Brain disorders such as neurodegenerative diseases and neuropsychiatric diseases have become serious threatens to human health and quality of life. Oleanolic acid (OA) and ursolic acid (UA) are pentacyclic triterpenoid isomers widely distributed in various plant foods and Chinese herbal medicines. Accumulating evidence indicates that OA and UA exhibit neuroprotective effects on multiple brain disorders. Therefore, this paper reviews researches of OA and UA on neurodegenerative diseases, neuropsychiatric diseases and other brain disorders including ischemic stroke, epilepsy, etc, as well as the potential underlying molecular mechanisms. [GRAPHICS]
作者机构:
[Li, Li; Yuan, Zhiying; Huang, Shiyi; Huang, Chencun; Xu, Guangming; Zhao, Yuan] Hunan Univ Chinese Med, Coll Pharm, Changsha, Hunan, Peoples R China.;[Xu, Guangming] Hunan Univ Chinese Med, Coll Pharm, Changsha 410208, Hunan, Peoples R China.
通讯机构:
[Guangming Xu] C;College of Pharmacy, Hunan University of Chinese Medicine, Changsha, Hunan, China
关键词:
affinity ultrafiltration mass spectrometry (AUF-MS);Ligusticum chuanxiong;molecular docking;screening of active compounds;thrombin
摘要:
INTRODUCTION: Ligusticum chuanxiong ('chuanxiong') is a traditional Chinese medicine for promoting blood circulation and removing blood stasis, which is often used to treat thrombotic diseases. However, its potential anticoagulant active ingredients have been unexplored. OBJECTIVES: The study aims to establish an affinity ultrafiltration mass spectrometry (AUF-MS) method for rapid screening of anti-thrombin active components of chuanxiong and to verify it in vitro. METHOD: In this study, the chemical constituents of different parts of chuanxiong were determined. A method for rapid screening of anticoagulant active ingredients by AUF-MS was established using thrombin as an affinity receptor target. Subsequently, the anticoagulant effect of such ligands was verified by in vitro anticoagulation experiments such as chromogenic substrate method and in vitro coagulation assay. Then the possible interaction mechanism between these ligands and thrombin was further studied by molecular docking. RESULTS: Twenty-one components were detected from different parts of chuanxiong. And three potential anti-thrombin active components were screened: ferulic acid, chlorogenic acid, isochlorogenic acid A by AUF coupled with high-performance liquid chromatography-quadrupole-Orbitrap mass spectrometry (HPLC-Q-Orbitrap-MS(n) ). The in vitro activity experiments and molecular docking revealed that these potential ligands exhibited strong binding ability and inhibitory activities on thrombin. CONCLUSION: The present study revealed that chuanxiong is a traditional Chinese medicine with excellent anticoagulation effects. Meanwhile, the integrated strategy based on AUF-MS, in vitro experiments and molecular docking also provided a powerful tool for further exploration of active ingredients responsible for the anticoagulant activity in chuanxiong.
摘要:
Ampelopsis grossedentata is a valuable medicinal and edible plant, which is often used as a traditional tea by the Tujia people in China. A. grossedentata has numerous biological activities and is now widely used in the pharmaceutical and food industries. In this study, two new flavonoids (1-2) and seventeen known compounds (3-19) were isolated and identified from the dried stems and leaves of A. grossedentata. These isolated compounds were characterized by various spectroscopic data including mass spectrometry and nuclear magnetic resonance spectroscopy. All isolates were assessed for their alpha-glucosidase inhibitory, antioxidant, and hepatoprotective activities, and their structure-activity relationships were further discussed. The results indicated that compound 1 exhibited effective inhibitory activity against alpha-glucosidase, with an IC50 value of 0.21 mu M. In addition, compounds 1-2 demonstrated not only potent antioxidant activities but also superior hepatoprotective properties. The findings of this study could serve as a reference for the development of A. grossedentata-derived products or drugs aimed at realizing their antidiabetic, antioxidant, and hepatoprotective functions.
摘要:
Objective:To explore the pharmacodynamic mechanism of Ganfule(肝复乐)in treating hepatocellular carcinoma from a new perspective of the interactions between intestinal flora and inflammatory cytokines.Methods:Fifteen SPF Kunming mice were randomly assigned into three group...MORE Objective:To explore the pharmacodynamic mechanism of Ganfule(肝复乐)in treating hepatocellular carcinoma from a new perspective of the interactions between intestinal flora and inflammatory cytokines.Methods:Fifteen SPF Kunming mice were randomly assigned into three groups:a normal control group,a model control group,and a Ganfule(5.4 g/kg)group.The H22 tumor-bearing mouse model was established.The mice in the Ganfule(5.4 g/kg)group were intragastrically administered with the corresponding dose of drugs,once a day,while those in the model control group and the normal control group were administered with the same volume of normal saline.After 14 days of intervention,the mice were sacrificed and the serum,tumor tissue,and intestinal contents samples were collected.Hematoxylin-eosin(HE)staining was employed to observe tumor necrosis.The levels of four inflammatory cytokines in the serum were measured by enzyme-linked immunosorbent assay(ELISA).The 16S rDNA V3~V4 region of the intestinal flora was analyzed by high-throughput sequencing.Pearson correlation coefficient analysis was carried out to investigate the interactions between inflammatory cytokines in mouse serum and intestinal flora in vivo.Results:Compared with the normal control group,the model control group showed elevated serum levels of interleukin-10(IL-10),transforming growth factor(TGF-β),and tumor necrosis factor(TNF-α)(P<0.05 or P<0.01)and lowered level of interleukin-4(IL-4)(P<0.05).The diversity and abundance of intestinal flora in tumor-bearing mice decreased and the number of beneficial bacteria such as Proteobacteria and Verrucomicrobia reduced(P<0.05),compared with that of the normal control group.Compared with the model control group,Ganfule(5.4 g/kg)showed the tumor inhibition rate of 64.6%,caused serious tumor cell necrosis,lowered the levels of IL-10,TGF-β,and TNF-α(P<0.05 or P<0.01),and elevated the level of IL-4(P<0.05).In addition,Ganfule(5.4 g/kg)increased the diversity and abundance of intestinal flora,increased the beneficial bacteria such as Proteobacteria and Verrucomicrobia(P<0.05),and reduced the pathogenic bacteria such as Firmicutes(P<0.05)in tumor-bearing mice.The correlation analysis demonstrated a negative correlation between TGF-βand Akkermansia(P<0.01),a positive correlation between TNF-αand Staphylococcus(P<0.01),a positive correlation between IL-10 and Parabacteroides(P<0.01),and a positive correlation between IL-4 and Lactobacillus(P<0.01).Conclusion:Ganfule can regulate the structure of intestinal flora and change the abnormal expression of inflammatory cytokines.The strong correlations between differential intestinal bacteria and the four inflammatory cytokines suggest that Ganfule can curb liver cancer by regulating the inflammation-related intestinal-liver axis.FEWER
作者机构:
[Salman Zafar] Institute of Chemical Sciences, University of Peshawar;[Ping-An Liu] Hunan Academy of Chinese Medicine
摘要:
Rodgersia is a traditional Chinese medicine that contains a variety of chemical constituents, including flavonoids, terpenoids, phenylpropanoids,gallic acid derivatives, steroids, volatile oils, and tannins, with anti-inflammatory, antioxidant, antitumor, antibacterial, antivirus, hepatoprotective,and other properties. In this paper, the main chemical constituents and pharmacological effects of Rodgersia are summarized. On this basis,the quality markers of this genus were predicted based on chemical composition, traditional medicinal properties, traditional efficacy, and measurable components. This review provides the basis for in-depth research, utilization, and quality control of Rodgersia.
作者机构:
[Yin, Lu; Lei, Chang; Huang, Dan; Wan, Hongyan; Li, Shunxiang; Zhou, Wei; He, Ye] Hunan Univ Chinese Med, Sci & Technol Innovat Ctr, State Key Lab Chinese Med Powder & Med Innovat Hun, Changsha 410208, Peoples R China.;[Yin, Lu; Huang, Dan; Wan, Hongyan; Li, Shunxiang; He, Ye] Hunan Univ Chinese Med, Hunan Engn Technol Res Ctr Bioact Subst Discovery, Sch Pharm, Changsha 410208, Peoples R China.;[Huang, Dan; Li, Shunxiang] Hunan Prov Sino US Int Joint Res Ctr Therapeut Dru, Changsha 410208, Peoples R China.
通讯机构:
[Huang, D ; Li, SX] H;Hunan Univ Chinese Med, Sci & Technol Innovat Ctr, State Key Lab Chinese Med Powder & Med Innovat Hun, Changsha 410208, Peoples R China.;Hunan Univ Chinese Med, Hunan Engn Technol Res Ctr Bioact Subst Discovery, Sch Pharm, Changsha 410208, Peoples R China.;Hunan Prov Sino US Int Joint Res Ctr Therapeut Dru, Changsha 410208, Peoples R China.
作者机构:
湖南中医药大学药学院,湖南长沙 410208;中药成药性与制剂制备湖南省重点实验室,湖南长沙 410208;湖南中医药大学中医药超分子机理与数理特征化实验室,湖南长沙 410208;中药药性与药效国家中医药管理局重点实验室,湖南长沙 410208;[张伟龙; 李海英; 田丽; 潘雪; 肖美凤; 李文姣; 谯茹; 王玉钗; 张良琦] College of Pharmacy, Hunan University of Chinese Medicine, Changsha, 410208, China, Hunan Provincial Key Laboratory of Drug ability and Preparation Modification of Traditional Chinese Medicine, Changsha, 410208, China
通讯机构:
[Pan, X.; He, F.-Y.] C;College of Pharmacy, China
摘要:
Ginsenoside Rg1, a traditional Chinese medicine monomer, has been shown to have antidepressant effects. We previously found that Rg1 exerts antidepressant effects by improving the gap junction channels (GJCs) dysfunction; however, the downstream mechanisms through which Rg1 ameliorates GJC dysfunction remain unclear. Since hemichannels directly release glutamate, GJC dysfunction decreases the expression levels of glutamate transporters in astrocytes, and glutamatergic system dysfunction plays an essential role in the pathogenesis of depression. The glutamatergic system may be a potential downstream target of Rg1 that exerts antidepressant effects. Therefore, in this study, we aimed to determine the downstream mechanisms by which Rg1 ameliorated GJC dysfunction and exerted its antidepressant effects. Corticosterone (CORT) is used to mimic high glucocorticoid levels in patients with depression in vitro. Primary cortical astrocytes were isolated and phosphorylation of connexin43 (Cx43) as well as the functions of hemichannels, GJCs, and the glutamatergic system were evaluated after drug treatment. Rg1 pretreatment reversed the anomalous activation of Cx43 phosphorylation as well as the dysfunction of hemichannels, GJCs, and the glutamatergic system induced by CORT. These results suggest that Rg1 can ameliorate CORT-induced dysfunction of the glutamatergic system in astrocytes by potentially reducing Cx43 phosphorylation and inhibiting opening of hemichannels, thereby improving GJC dysfunction.