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Acta Pharmacologica Sinica

Yeon-Yong Kim, In-Gyu Je, Min Jong Kim, Byeong-Cheol Kang, Young-Ae Choi, Moon-Chang Baek, Byungheon Lee, Jin Kyeong Choi, Hae Ran Park, Tae-Yong Shin, Soyoung Lee, Seung-Bin Yoon, Sang-Rae Lee, Dongwoo Khang, Sang-Hyun Kim
Mast cells are important effector cells in immunoglobulin (Ig) E-mediated allergic reactions such as asthma, atopic dermatitis and rhinitis. Vanillic acid, a natural product, has shown anti-oxidant and anti-inflammatory activities. In the present study, we investigated the anti-allergic inflammatory effects of ortho-vanillic acid (2-hydroxy-3-methoxybenzoic acid, o-VA) that was a derivative of vanillic acid isolated from Amomum xanthioides. In mouse anaphylaxis models, oral administration of o-VA (2, 10, 50 mg/kg) dose-dependently attenuated ovalbumin-induced active systemic anaphylaxis and IgE-mediated cutaneous allergic reactions such as hypothermia, histamine release, IgE production and vasodilation; administration of o-VA also suppressed the mast cell degranulator compound 48/80-induced anaphylaxis...
November 28, 2016: Acta Pharmacologica Sinica
Da-Xuan Wang, Yu-Jiao Zou, Xi-Bin Zhuang, Shu-Xing Chen, Yong Lin, Wen-Lan Li, Jun-Jin Lin, Zhi-Qiang Lin
Sulforaphane is a common antioxidant selectively abundant in cruciferous plants, which exhibits effective anti-cancer actions in control of tumorigenesis or progression of various cancers. A recent study has shown that sulforaphane attenuates the EGFR signaling pathway in non-small cell lung cancer (NSCLC), suggesting its potential anti-metastatic effects. In this study we assessed the involvement of sulforaphane and miR-616-5p in epithelial-mesenchymal transition (EMT) and NSCLC metastasis. Sulforaphane suppressed the cell proliferation in human NSCLC cell lines H1299, 95C and 95D with IC50 values of 9...
November 28, 2016: Acta Pharmacologica Sinica
Kang-Feng Jiang, Gan Zhao, Gan-Zhen Deng, Hai-Chong Wu, Nan-Nan Yin, Xiu-Ying Chen, Chang-Wei Qiu, Xiu-Li Peng
Recent studies show that Polydatin (PD) extracted from the roots of Polygonum cuspidatum Sieb, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. In this study, we investigated the anti-inflammatory effects of PD on Staphylococcus aureus-induced mastitis in mice and elucidated the potential mechanisms. In mice with S aureus-induced mastitis, administration of PD (15, 30, 45 mg/kg, ip) or dexamethasone (Dex, 5 mg/kg, ip) significantly suppressed the infiltration of inflammatory cells, ameliorated the mammary structural damage, and inhibited the activity of myeloperoxidase, a biomarker of neutrophils accumulation...
November 28, 2016: Acta Pharmacologica Sinica
Shang Wang, Chao-Liang Long, Jun Chen, Wen-Yu Cui, Yan-Fang Zhang, Hao Zhang, Hai Wang
Both iptakalim (Ipt) and natakalim (Nat) activate the SUR2B/Kir6.1 channel, an ATP-sensitive potassium channel (KATP) subtype, with high selectivity. In this study we investigated the therapeutic effects of Ipt and Nat against isoproterenol-induced chronic heart failure (ISO-CHF) in rats, and demonstrated a new therapeutic approach to the treatment of CHF through activation of the SUR2B/Kir6.1 channel in endothelial cells. In ISO-CHF rats, oral administration of Nat (1, 3, 9 mg·kg(-1)·d(-1)) or Ipt (3 mg·kg(-1)·d(-1)) for 60 days significantly improved cardiac dysfunction, reversed cardiac remodeling, significantly attenuated the pathological increases in BNP levels, and improved endothelial dysfunction by adjusting the balance between endothelin and NO systems...
November 28, 2016: Acta Pharmacologica Sinica
Nan Zheng, Lu Liu, Wei-Wei Liu, Fei Li, Toshihiko Hayashi, Shin-Ichi Tashiro, Satoshi Onodera, Takashi Ikejima
Reactive oxygen species (ROS) and reactive nitrogen species (RNS) play important roles in regulating cell survival and death. Silibinin is a natural polyphenolic flavonoid isolated from milk thistle with anti-tumor activities, but it was found to induce cytoprotective ROS/RNS in human breast cancer MCF-7 cells. Furthermore, treatment with silibinin down-regulates ERα expression in MCF-7 cells, and inducing both autophagy and apoptosis. In this study we explored the relationship between ER-associated pathways and RNS/ROS in MCF-7 cells...
November 21, 2016: Acta Pharmacologica Sinica
Wen-Yue Liu, Jing-Wei Zhang, Xue-Quan Yao, Chao Jiang, Ji-Chao He, Pin Ni, Jia-Li Liu, Qian-Ying Chen, Qing-Ran Li, Xiao-Jie Zang, Lan Yao, Ya-Zhong Liu, Mu-Lan Wang, Pei-Qiang Shen, Guang-Ji Wang, Fang Zhou
Shenmai injection (SMI) is a Chinese patent-protected injection, which was mainly made of Red Ginseng and Radix Ophiopogonis and widely used for treating coronary heart disease and tumors by boosting Qi and nourishing Yin. In this study we examined whether SMI could produce direct synergetic effects on the cytoxicity of adriamycin (ADR) and paclitaxel (PTX) in colorectal cancers in vivo and in vitro, and explored the underlying pharmacokinetic mechanisms. BALB/c nude mice with LoVo colon cancer xenografts were intraperitoneally injected with ADR (2 mg·kg(-1)·3d(-1)) or PTX (7...
November 21, 2016: Acta Pharmacologica Sinica
Yura Jang, Hye Jin Chung, Jung Wan Hong, Cheol-Won Yun, Hesson Chung
Paclitaxel is a most widely used anticancer drug with low oral bioavailability, thus it is currently administered via intravenous infusion. DHP107 is a lipid-based paclitaxel formulation that can be administered as an oral solution. In this study, we investigated the mechanism of paclitaxel absorption after oral administration of DHP107 in mice and rats by changing the dosing interval, and evaluated the influence of bile excretion. DHP107 was orally administered to mice at various dosing intervals (2, 4, 8, 12, 24 h) to examine how residual DHP107 affected paclitaxel absorption during subsequent administration...
November 21, 2016: Acta Pharmacologica Sinica
Hui Li, Xiao-Xiao Meng, Li Zhang, Bao-Jun Zhang, Xin-Yu Liu, Wen-Wei Fu, Hong-Sheng Tan, Yuan-Zhi Lao, Hong-Xi Xu
Oblongifolin C (OC) and guttiferone K (GUTK) are two anticancer compounds extracted from Garcinia yunnanensis Hu, but they act by different mechanisms. In this study we investigated whether a combination of OC and GUTK (1:1 molar ratio) could produce synergistic anticancer effects against human colorectal cancer cells in vitro. For comparison, we also examined the anticancer efficacy of ethanol extracts from G yunnanensis fruit, which contain OC and GUTK up to 5%. Compared to OC and GUTK alone, the combination of OC and GUTK as well as the ethanol extracts more potently inhibited the cancer cell growth with IC50 values of 3...
November 14, 2016: Acta Pharmacologica Sinica
Shi-Rong Zhang, Lu-Cheng Zhu, Yan-Ping Jiang, Jing Zhang, Ru-Jun Xu, Ya-Si Xu, Bing Xia, Sheng-Lin Ma
AIM: Few effective therapeutic options are currently available for the treatment of non-small cell lung cancer (NSCLC) with brain metastases (BM). Recent evidence shows that NSCLC patients with BMs respond well to afatinib, but little is known about the underlying mechanisms. In this study, we evaluated the efficacy of afatinib in treatment of BMs in mice and investigated whether afatinib could actively penetrate the brain-blood barrier and bind to its target. METHODS: NSCLC BM model was established in nude mice by intracerebral injection of PC-9...
November 14, 2016: Acta Pharmacologica Sinica
Ting Zhong, Li-Ying Zhang, Zeng-Yan Wang, Yue Wang, Feng-Mei Song, Ya-Hong Zhang, Jing-Hua Yu
AIM: Human enterovirus 71 (EV71) is the primary causative agent of recent large-scale outbreaks of hand, foot, and mouth disease (HFMD) in Asia. Currently, there are no drugs available for the prevention and treatment of HFMD. In this study, we compared the anti-EV71 activities of three natural compounds, Rheum emodin, Artemisinin and Astragaloside extracted from Chinese herbs Chinese rhubarb, Artemisia carvifolia and Astragalus, respectively, which have been traditionally used for the treatment and prevention of epidemic diseases...
November 14, 2016: Acta Pharmacologica Sinica
Shi-Rong Zhang, Ya-Si Xu, Er Jin, Lu-Cheng Zhu, Bing Xia, Xu-Feng Chen, Fan-Zhu Li, Sheng-Lin Ma
Most gefitinib-treated patients with non-small cell lung cancer (NSCLC) would eventually develop resistance. Lysimachia capillipes (LC) capilliposide extracts from LC Hemsl. show both in vitro and in vivo anti-cancer effects. In this study we investigated whether LC capilliposide in combination with gefitinib could overcome the resistance of NSCLC cells to gefitinib and identified the signaling pathways involved. Treatment with LC capilliposide alone inhibited the growth of a panel of NSCLC cell lines (PC-9, H460, H1975, H1299 and PC-9-GR) sensitive or resistant to gefitinib with IC50 values in the range of μg/mL...
November 14, 2016: Acta Pharmacologica Sinica
Sai Chang, Wen-Chen Ruan, Ya-Zhou Xu, Yun-Jie Wang, Jie Pang, Lu-Yong Zhang, Hong Liao, Tao Pang
Recent studies focus on promoting neurite outgrowth to remodel the central nervous network after brain injury. Currently, however, there are few drugs treating brain diseases in the clinic by enhancing neurite outgrowth. In this study, we established an NGF-induced PC12 differentiation model to screen novel compounds that have the potential to induce neuronal differentiation, and further characterized 4,10-Aromadendranediol (ARDD) isolated from the dried twigs of the Baccharis gaudichaudiana plant, which exhibited the capability of promoting neurite outgrowth in neuronal cells in vitro...
November 14, 2016: Acta Pharmacologica Sinica
Yong-Qin Zhou, Xiu-Fang Weng, Rui Dou, Xiao-Sheng Tan, Tian-Tian Zhang, Jin-Bo Fang, Xiong-Wen Wu
AIM: Hedyotis hedyotidea has been used in traditional Chinese medicine for the treatment of autoimmune diseases. However, the mechanisms underlying for the effect remain unknown. We previously showed that, among 11 compounds extracted from H hedyotidea, betulin produced the strongest suppressive effect on T cell activation. Here, we examined the hepatoprotective effects of betulin against acute autoimmune hepatitis in mice and the mechanisms underlying the effects. METHODS: Freshly isolated mouse splenocytes were stimulated with concanavalin A (Con A, 5 μg/mL) in the presence of betulin, the cell proliferation was assessed with CSFE-dilution assay...
October 31, 2016: Acta Pharmacologica Sinica
Ying Liu, Yang Qi, Zhi-Hui Bai, Chen-Xu Ni, Qi-Hui Ren, Wei-Heng Xu, Jing Xu, Hong-Gang Hu, Lei Qiu, Jian-Zhong Li, Zhi-Gao He, Jun-Ping Zhang
AIM: Matrine is an alkaloid extracted from a Chinese herb Sophora flavescens Ait, which has shown chemopreventive potential against various cancers. In this study, we evaluated the anticancer efficacy of a novel derivative of matrine, (6aS, 10S, 11aR, 11bR, 11cS)-10- methylamino-dodecahydro- 3a,7a-diaza-benzo (de) (MASM), against human hepatocellular carcinoma (HCC) cells and their corresponding sphere cells in vitro and in vivo. METHODS: Human HCC cell lines (Hep3B and Huh7) were treated with MASM...
October 24, 2016: Acta Pharmacologica Sinica
Qiang Meng, Xing-Ping Duan, Chang-Yuan Wang, Zhi-Hao Liu, Peng-Yuan Sun, Xiao-Kui Huo, Hui-Jun Sun, Jin-Yong Peng, Ke-Xin Liu
AIM: Alisol B 23-acetate (AB23A) is a natural triterpenoid isolated from the traditional Chinese medicine rhizoma alismatis, which exhibits a number of pharmacological activities, including anti-hepatitis virus, anti-cancer and antibacterial effects. In this study we examined whether AB23A protected against non-alcoholic steatohepatitis (NASH) in mice, and the mechanisms underlying the protective effects. METHODS: NASH was induced in mice fed a methionine and choline-deficient (MCD) diet for 4 weeks...
October 24, 2016: Acta Pharmacologica Sinica
Qing Li, Ting-Ting Tang, Feng Jiang, Rong Zhang, Miao Chen, Jun Yin, Yu-Qian Bao, Xiang Cheng, Cheng Hu, Wei-Ping Jia
AIM: KCNQ1 channel is a member of the voltage-gated potassium channel KQT-like subfamily. The KCNQ1 gene has recently been identified as a susceptibility locus for type 2 diabetes mellitus (T2DM). In the present study, we examined the effects of KCNQ1 variants on the therapeutic response to modified-release gliclazide (gliclazide MR) treatment in Chinese patients newly diagnosed with T2DM. METHODS: A total of 100 newly diagnosed T2DM patients without a history of any anti-diabetic medications were treated with gliclazide MR for 16 weeks, but 91 patients completed the entire study...
October 3, 2016: Acta Pharmacologica Sinica
Cong Li, Xiao-Dan Guo, Min Lei, Jia-Yi Wu, Jia-Zhen Jin, Xiao-Fan Shi, Zhi-Yuan Zhu, Vatcharin Rukachaisirikul, Li-Hong Hu, Tie-Qiao Wen, Xu Shen
AIM: Considering the complicated pathogenesis of Alzheimer's disease (AD), multi-targets have become a focus in the discovery of drugs for treatment of this disease. In the current work, we established a multi-target strategy for discovering active reagents capable of suppressing both Aβ level and Tau hyperphosphorylation from natural products, and found that the ethanol extract of Thamnolia vermicularis (THA) was able to improve learning ability in APP/PS1 transgenic mice by inhibiting both Aβ levels and Tau hyperphosphorylation...
October 3, 2016: Acta Pharmacologica Sinica
Cheng-Gang Li, Meng-Fan Pu, Chun-Zhu Li, Man Gao, Ming-Xia Liu, Cun-Zhi Yu, Hong Yan, Chun Peng, Yang Zhao, Yu Li, Ze-Long Ma, Xin-Ming Qi, Yi-Zheng Wang, Ling-Ling Miao, Jin Ren
AIM: Previous studies have shown that microRNA-1304 (miR-1304) is dysregulated in certain types of cancers, including non-small cell lung cancer (NSCLC), and might be involved in tumor survival and/or growth. In this study we investigated the direct target of miR-1304 and its function in NSCLC in vitro. METHODS: Human lung adenocarcinoma cell lines (A549 and NCI-H1975) were studied. The cell proliferation and survival were investigated via cell counting, MTT and colony-formation assays...
September 19, 2016: Acta Pharmacologica Sinica
Li-Yun Yang, Xiao-Fang Liu, Yang Yang, Lin-Lin Yang, Kai-Wen Liu, Yu-Bo Tang, Min Zhang, Min-Jia Tan, Shan-Mei Cheng, Ye-Chun Xu, Huai-Yu Yang, Zhi-Jie Liu, Gao-Jie Song, Wei Huang
AIM: CD97 belongs to the adhesion GPCR family characterized by a long ECD linked to the 7TM via a GPCR proteolytic site (GPS) and plays important roles in modulating cell migration and invasion. CD97 (EGF1-5) is a splicing variant of CD97 that recognizes a specific ligand chondroitin sulfate on cell membranes and the extracellular matrix. The aim of this study was to elucidate the extracellular molecular basis of the CD97 EGF1-5 isoform in protein expression, auto-proteolysis and cell adhesion, including epidermal growth factor (EGF)-like domain, GPCR autoproteolysis-inducing (GAIN) domain, as well as GPS mutagenesis and N-glycosylation...
September 19, 2016: Acta Pharmacologica Sinica
Sai-Fei Lei, De-Hua Yang, Ming-Wei Wang
No abstract text is available yet for this article.
December 2016: Acta Pharmacologica Sinica
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