| 2 | SRS27,a semisynthetic diterpenoid lactone,inhibits airway inflammation and hyper-responsiveness via NF-κB pathway in an allergic mouse asthma model显示文摘Andrographis paniculata contains two main diterpenoid constituents,andrographolide(AGP)and 14-deoxy-11,12-didehydroandrographolide(DDAG),which were found to exhibit antiasthma effects in a mouse asthma model.However,due to inadequacies of both compounds in terms of drug-likeness,DDAG analogues were semisynthesised to tackle these shortcomings.The objective of the study was to investigate the potential of DDAG analogues as new antiasthma agents.Among the analogues,(SRS27)was proven to inhibit cysteinyl leukotrienes(CysLT)and nitric oxide(NO)synthesis in mouse macrophages,like AGP.DDAG,on the other hand,failed to exhibit such activities.SRS27 is less cytotoxic than AGP,suggests that a simple chemical modification of DDAG produces a compound with CysLT and NO inhibitory activites similar to AGP while maintaining toxicity profile similar to DDAG.It is interesting to note that other analogues such as SRS28,SRS49,SRS76 and SRS83 with chemical modifications on the same carbon numbers 3 and 19 of DDAG were unable to show inhibition of CysLT and NO synthesis.Consequently,the potential anti-inflammatory effect of SRS27 was investigated in ovalbumin(OVA)-induced mouse asthma model.The compound was administered in a prophylactic manner and showed a substantial decrease in mouse asthma model parameters.SRS27 at 3mg·kg-1 significantly reduced OVA-induced total cell such as macrophages,eosinophils,lymphocytes and neutrophils,as well as inflammatory cytokines such as IL-4,IL-5,IL-13 and eotaxin in bronchoalveolar lavage BAL fluid.The compound also suppressed serum IgE production.In addition,SRS27 suppressed mucus hyper-secretion and expression of inflammatory mediators such as TNF-α,MCP-1,Muc5 ac,RANTES,IL-33 and iNOS.SRS27 is the first known DDAG derivative tested positive in mouse asthma model and as such SRS27 could serve as a prototype prophylactic agent. | Jonathan Chee Woei LIM Fera Yiqian GOH Sreenivasa Rao SAGINEEDU Audrey Chee Hui YONG Shiran Mohd SIDIK Nordin Haji LAJIS Wai-Shiu Fred WONG Johnson STANSLAS | 2015 | 中国药理学与毒理学杂志2015，29，S1： | 0 |
| 3 | Methyl gallate isolated from Mangifera pajang kernel induces proliferation inhibition and apoptosis in MCF-7 breast cancer cells via oxidative stress显示文摘Objective:To determine the lead bioactive compound in kernel extract of Mangifera pajang and its anti-cancer activity against human breast cancer cell lines with positive estrogen receptor(MCF-7).Methods:The methanolic extract of dried powder kernel of Mangifera pajang was exposed to column chromatography for isolation.The structural elucidation of the isolated compound was characterized using infrared,nuclear magnetic resonance,mass spectrometry.Furthermore,cytotoxicity,morphological changes,flow cytometry and cell cycle arrest analyses were performed to examine the mechanism of anti-proliferation and apoptosis induced by methyl gallate against MCF-7.Results:One compound was isolated from the methanolic extract of Mangifera pajang kernel and identified as methyl gallate.The flow cytometric results demonstrated induction of apoptosis in MCF-7 cells by three concentrations of methyl gallate.The cell cycle arrest showed a significant(P<0.05)decrease in cell progression at G2/M phase of MCF-7 after treatment with 100μM of methyl gallate.The cell percentage of early and late apoptosis was significant at 10 and 100μM of methyl gallate.Also,methyl gallate treatment induced up-regulation of reactive oxygen species levels in MCF-7 cells with a reduction in superoxide dismutase levels.Conclusions:These findings indicate that isolated methyl gallate from Mangifera pajang kernel extracts induces growth inhibition and apoptosis in MCF-7 cells via up-regulating oxidative stress pathway. | Ranneh Yazan Abu Bakar Mohd Fadzelly Rahim Azlen-Che Kassim Nur Kartinee Stanslas Johnson Teh Yuan-Han Fadel Abdulmannan Ellulu Mohammed S | 2022 | Asian Pacific Journal of Tropical Biomedicine2022，12，4： | 0 |
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