Botanical Studies
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2016
·Vol. 57
·期 1
·1-11
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IF 1.159
Shi Qiang-Qiang,Dang Jun,Wen Huai-Xiu,Yuan Xiang,Tao Yan-Duo,Wang Qi-Lan
Background
Dracocephalum heterophyllum was a traditional Tibetan medicine possesses various pharmacological effects involved in anti-inflammatory, antibacterial activities. However, its anti-hepatitis, antioxidant activity and bioactive compounds have not been reported, the objective of this research work was to investigate the pharmacological activity and bioactive compounds of D. heterophyllum extracts. Results In the present study, the anti-hepatics and antioxidant activities of four D. heterophyllum extracts (i.e. petroleum ether extracts, ethyl acetate extracts, n -BuOH extracts, and water extracts) were conducted. The main chemical constituent of petroleum ether and ethyl acetate extracts were also isolated using chromatographic techniques and identified by NMR spectroscopic methods. The anti-hepatitis assay showed that the petroleum ether and ethyl acetate extracts of D. heterophyllum significantly prolonged the mean survival times and reduced the mortality of mouse hepatitis model induced by concanavalin A (ConA). The levels of alanine transaminase, aspartate transaminase in blood serum could be decreased obviously by ethyl acetate extracts compared with ConA group (P < 0.01). The histological analysis demonstrated that the ethyl acetate extracts could inhibit apoptosis and necrosis caused by ConA. In addition, the antioxidant activities of the four extracts of D. heterophyllum were measured by DPPH assay, ABTS assay, anti-lipidperoxidation assay, ferric reducing antioxidant power assay, ferrous metal ions chelating assay and determination of total phenolic contents. The results showed that the ethyl acetate extract had the highest antioxidant activities, followed by petroleum ether extract. Finally, nine mainly compounds were isolated from the Petroleum ether and ethyl acetate extracts, including four triterpenes: oleanolic acid ( 1 ), ursolic acid ( 2 ), pomolic acid ( 3 ), 2α- hydroxyl ursolic acid ( 4 ), three flavonoids: apigenin-7- O -rutinoside ( 5 ), luteolin ( 8 ), diosmetin ( 9 ) and two phenolic acids: rosmarinic acid ( 6 ), methyl rosmarinate ( 7 ). Conclusion The Ethyl acetate extract of D. heterophyllum had the highest anti-hepatitis and antioxidants activities, followed by petroleum ether extract. The bioactive substances may be triterpenes, flavonoids and phenolic acids, the ethyl acetate extracts of D. heterophyllum may be possible candidates in developing anti-hepatitis medicine.
研究领域:
药理学
·
植物学
·
药物化学
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DOI
PubMed
高影响因子
MEDICAL SCIENCE MONITOR
·
2018
·
IF 1.894
Hong Jiang,Chen Zhang,Wen He
Background Dracocephalum heterophyllum Benth flavonoid (DHBF) is a Tibetan and Uighur traditional medicine used to treat various disorders such as hypertension, lung heat, cough, and bronchitis; it has good antioxidant activity. Previous studies have shown that DHBF can reduce blood pressure in renovascular hypertensive rats, improve left ventricular systolic and diastolic function, and improve myocardial contractility. Therefore, we aimed to study the effect of DHBF on cardiomyocyte hypertrophy in cultured cells. Material/Methods Neonatal rat cardiomyocytes were cultured, and hypertrophy was induced by angiotensin II (Ang II), with or without varying concentrations of the DHBF extract. Cell Counting Kit-8 assay was used to assess cell viability, RT-qPCR was used to determine mRNA levels, confocal laser scanning microscopy was used to measure cell surface area and intracellular Ca 2+ concentrations ([Ca 2+ ] i ), and colorimetric assays were used to assess nitric oxide (NO) levels and nitric oxide synthase (NOS) activity. Results Ang II treatment of cardiomyocytes reduced cell viability to ~75% that of controls. Ang II treatment also increased cell surface area; increased mRNA expression of c-jun, atrial natriuretic peptide (ANP), brain natriuretic peptide (BNP), and β-myosin heavy chain (β-MHC); increased [Ca 2+ ] i ; and reduced NOS activity and NO production. DHBF treatment could reverse these effects in a concentration-dependent manner. Conclusions These results showed that DHBF can ameliorate cardiomyocyte hypertrophy induced by Ang II, as indicated by the downregulation of cardiac hypertrophy genes ( ANP , BNP , and β -MHC ) and reduction in cell surface area. The mechanism may be related to NO release and [Ca 2+ ] I regulation.
研究领域:
心脏病学
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药理学
·
细胞生物学
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DOI
PubMed
高影响因子
JOURNAL OF MOLECULAR STRUCTURE
·
2025
·
IF 4.7
Chuang Liu,Ying Li,Yu Zhang,Shiyu Li,Jun Dang
The discovery of tyrosinase modulators from natural products has long been hampered by limitations in screening efficiency and accuracy. In this study, a novel online screening system for tyrosinase was constructed based on HPLC technology that enables high-throughput recognition of active constituents in complex matrices. Applying this HPLC-tyrosinase system to Dracocephalum heterophyllum ( D. heterophyllum ), three active peaks were precisely captured, which were subsequently isolated and structurally characterized as caffeic acid, verbascoside, and rosmarinic acid. Enzyme activity assays revealed that caffeic acid (IC 50 = 1.08 mM) and rosmarinic acid (IC 50 = 0.41 mM) markedly inhibited tyrosinase activity, whereas verbascoside exhibited activating properties (EC 50 = 0.24 mM). The action mechanisms and bioactivities of these compounds were further elucidated through density functional theory calculations, molecular docking analysis, and in vivo validation. Collectively, the online HPLC-tyrosinase activity screening system established in this work not only provides a theoretical basis for the high value-added development of D. heterophyllum , but also delivers a high-throughput, precision tool for discovering natural tyrosinase inhibitors, demonstrating robust application potential in the fields of cosmetic science, food preservation and pharmaceutical development.
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高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2022
·Vol. 23
·期 19
·11572
·
IF 6.208
Chengzhao Li,Jun Dang,Yue Lv,Yan Fang,Chengjun Ma,Qilan Wang,Gang Li
Dracocephalum heterophyllum(D. heterophyllum) is a traditional Chinese Tibetan medicine that has been used for the treatment of lymphitis, hepatitis, and bronchitis. However, only a few selected chemical components are currently obtained fromD. heterophyllum, which limits its further pharmacological applications. In this study, we have obtained samwinol fromD. heterophyllumby medium- and high-pressure liquid chromatography separation for the first time. Thereafter, we investigated the protective actions of samwinol against amyloid beta protein fragment 25–35 (Aβ25–35) induced neurotoxicity in cultured rat pheochromocytoma PC-12 cells and explored its underlying mechanisms of action. The results indicated that samwinol could increase cell viability and inhibit the production of reactive oxygen species (ROS) and mitochondria-derived ROS, as assessed by MTT assay, Giemsa staining, and flow cytometry assay. Through Western blot analysis, it was found that samwinol substantially inhibited the phosphorylation of ERK(1/2) and promoted the expression of HO-1 and Nrf2. The data obtained from molecular docking were also consistent with the above conclusions. All of these results showed that samwinol fromD. heterophyllumcan display significant anti-neuroinflammatory and antioxidant activities in vitro, which are associated with the suppression of ERK/AKT phosphorylation and the activation of the Nrf2/HO-1 signaling pathway. In the future, additional in-depth mechanism studies will be carried out to provide more evidence for the potential of samwinol in the treatment of Alzheimer’s disease.Keywords:D. heterophyllum;PC-12 Cells;Aβ25–35;neuroinflammatory;oxidative stress
研究领域:
药理学
·
神经科学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）