Journal of Essential Oil Bearing Plants
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2022
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IF 1.971
Chunlian Li,Xiaobin Lin,Qiuyang Cai,Weicheng Zhang,Xianyi Wu,Zekai Tan,Lewen Yao,Shiyuan Huang,Yanghe Yuan,Lanyue Zhang
The perennial herb Alpinia oxyphylla Miq. (Zingiberaceae) is an important traditional medicinal plant in China. The present study evaluated the chemical composition of A. oxyphylla essential oil (AOEO) using GC-MS. The AOEO contained 55 compounds, including nootkatone (20.12%), valencene (12.26%), and ethyl-p-methoxycinnamate (5.00%). Previous studies have shown that AOEO possesses significant antioxidant and antibacterial activities. However, the anti-inflammatory effect of AOEO on tissue plasminogen activator (TPA)-induced ear edema is yet to be reported. In this study, TPA-induced ear edema was used to investigate the anti-inflammatory activity of AOEO. Hematoxylin and eosin staining of mouse tissue sections indicated that AOEO reduced the degree of edema, and immunohistochemistry experiments revealed that AOEO inhibited the expression of tumor necrosis factors, such as cyclooxygenase 2 (COX-2), interleukin-6 (IL-6), and nuclear factor-kappa B (NF-κB). A. oxyphylla is a commonly used traditional Chinese medicine with good biological activity. Analysis of the species potential geographical distribution and diversity indicated that the species can be rationally protected and exploited. Based on the chemical composition and biological activity of AOEO, further research and development should effectively promote the development of medicine, food, and cosmetics industries. The potential distribution of A. oxyphylla under current climatic conditions was predicted using DIVA-GIS and geographic information from herbarium specimens and other documents. The species predicted distribution spanned more than 12 provinces in China and was the most extensive in Hainan. Under current climatic conditions, A. oxyphylla is suitable for growing and expanding its population in the warm, humid regions of southern China.
研究领域:
植物学
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药理学
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生物化学
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DOI
高影响因子
Letters in Drug Design & Discovery
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2020
·Vol. 17
·期 4
·502-511
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IF 1.169
Song Mingxia,Liu Bing,Yu Shengwang,He Shihui,Liang Yuqiu,Li Sifan,Chen Qiuyan,Deng Xianqing
Background: Several series of hydrazone derivatives of pyrazole-4-carboxaldehydes (4- 11) were designed and synthesized to screen their inflammatory activity. Methods: The products were characterized by 1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo
xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Results and Conclusion: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF-α at the concentration of 10 μg/mL. Compounds 7b and 11c, two of the most potent
compounds, exhibited TNF-α inhibitory ability in a dose-dependent manner with IC50 values of 5.56 and 3.69 μM, respectively. In vivo, intraperitoneal administration with 7b and 11c markedly inhibited the ear edema at the doses of 20 and 50 mg/kg. Compound 11c, inhibited edema by 49.59
% at the dose of 20 mg/kg, was comparable to the reference drug dexamethasone at the same dose (with an inhibition of 50.49 %). To understand the binding pattern, molecular docking of representative 7b and 11c was performed, which demonstrated that both compounds have a forceful binding with
the TNF-α, and that the phenyl and hydrazide moieties of them play a significant role in binding with the target site.
研究领域:
药物化学
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炎症研究
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分子生物学
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DOI
高影响因子
POLYCYCLIC AROMATIC COMPOUNDS
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2021
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IF 3.744
Rui Yan,Xiaoliu Huang,Xianqing Deng,Mingxia Song
In this study, 18 pyrazole derivatives coupled with pyrazoline were synthesized and screened for their anti-inflammatory and antimicrobial activities. All the target compounds were synthesized smoothly and characterized using 1H NMR, 13C NMR, and HRMS. In vitro lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α model and in vivo xylene-induced ear-edema model were used to evaluate their anti-inflammatory activity. Antimicrobial activity against several Gram-positive strains and Gram-negative strains was evaluated using a serial dilution method. Pharmacological results indicated that most of the compounds markedly inhibited the expression of TNF-α at the concentration of 20 μg/mL. Compounds 9b showed 66.4% inhibition for the LPS-induced TNF-α release, which was superior than that of the positive control drug dexamethasone (DXMS). And compounds 4a, 4b, 5a, 5b, 6b, and 9b showed comparable inhibition activity to DXMS. In xylene-induced ear-edema model, compound 4a inhibited edema by 48.71%, which was more effective than DXMS (47.18%) in inhibiting xylene-induced ear edema. Compound 4b, 5a, 5b, 6b, and 9b showed inhibition of 36.82%, 27.65%, 45.87%, 31.78%, and 43.67%, respectively. Furthermore, compounds 4a, 5a, 5b, and 9b displayed broad-spectrum antimicrobial activity against several Gram-positive and Gram-negative bacterial. These compounds, 4a, 5a, 5b, and 9b, possess both anti-inflammatory and antimicrobial activities, thus are worth further investigation to enhance their antimicrobial activities for the development of new class of dual anti-inflammatory–antimicrobial agents.
研究领域:
药理学
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药物化学
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微生物学
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DOI
高影响因子
Letters in Drug Design & Discovery
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2019
·Vol. 16
·期 9
·1020-1030
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IF 0.953
Liang Zhaochang,Huang Yuping,Wang Shiben,Deng Xianqing
Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro
LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain.
Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 μg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition,
several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 μg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which
exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.
研究领域:
药理学
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药物化学
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传染病学
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炎症研究
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DOI
高影响因子
Revista Brasileira de Farmacognosia-Brazilian Journal of Pharmacognosy
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2019
·Vol. 29
·期 1
·46-53
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IF 1.754
Peng Wei,Han Ping,Yu Luyao,Chen Ying,Ye Bingzhu,Qin Luping,Xin Hailiang,Han Ting
The fruits of Xanthium strumarium L., Asteraceae, have been used for various diseases in Chinese folk medicine, including allergic rhinitis, tympanitis, arthritis, ozena etc. The current study was aimed to investigate the therapeutic effects of caffeoylquinic acids from fruits of X. strumarium on allergic rhinitis in animals. The toxicity test indicated that the caffeoylquinic acids have no obvious toxicity. By using HPLC assays combined with reference standards, ten caffeoylquinic acids were identified as the predominant constituents. Anti-allergic activities of the caffeoylquinic acids were evaluated using passive cutaneous anaphylaxis test and Schultz-Dale test; dimethylbenzene induced ear edema test was performed to evaluate its anti-inflammatory effect. Then, the allergic rhinitis model in rats was established to evaluate the therapeutic effects of the caffeoylquinic acids against allergic rhinitis with the following indexes: allergic rhinitis symptom scores, serum levels of pro-inflammatory cytokines, histopathological examination, and histamine release. Our study revealed that the caffeoylquinic acids showed obvious anti-allergic and anti-inflammatory properties, and its treatments were beneficial for ameliorating the nasal symptoms, decreasing pro-inflammatory cytokines, and inhibiting the releases of histamine. Collectively, the caffeoylquinic acids might be utilized as effective and safe disease therapeutic agents for allergic rhinitis.
研究领域:
药理学
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免疫学
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过敏
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植物化学
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产品关联
DOI
高影响因子
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