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Acta Pharmacologica Sinica

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https://www.readbyqxmd.com/read/28713162/abt-263-induces-g1-g0-phase-arrest-apoptosis-and-autophagy-in-human-esophageal-cancer-cells-in-vitro
#1
Qing-Huan Lin, Fu-Chang Que, Chun-Ping Gu, De-Sheng Zhong, Dan Zhou, Yi Kong, Le Yu, Shu-Wen Liu
Both the anti- and pro-apoptotic members of the Bcl-2 family are regulated by a conserved Bcl-2 homology (BH3) domain. ABT-263 (Navitoclax), a novel BH3 mimetic and orally bioavailable Bcl-2 family inhibitor with high affinity for Bcl-xL, Bcl-2 and Bcl-w has entered clinical trials for cancer treatment. But the anticancer mechanisms of ABT-263 have not been fully elucidated. In this study we investigated the effects of ABT-263 on human esophageal cancer cells in vitro and to explore its anticancer mechanisms...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713161/functional-expression-of-the-ca-2-signaling-machinery-in-human-embryonic-stem-cells
#2
Ji-Jun Huang, Yi-Jie Wang, Min Zhang, Peng Zhang, He Liang, Hua-Jun Bai, Xiu-Jian Yu, Huang-Tian Yang
Emerging evidence suggests that Ca(2+) signals are important for the self-renewal and differentiation of human embryonic stem cells (hESCs). However, little is known about the physiological and pharmacological properties of the Ca(2+)-handling machinery in hESCs. In this study we used RT-PCR and Western blotting to analyze the expression profiles of genes encoding Ca(2+)-handling proteins; we also used confocal Ca(2+) imaging and pharmacological approaches to determine the contribution of the Ca(2+)-handling machinery to the regulation of Ca(2+) signaling in hESCs...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713160/pathogenic-roles-of-microvesicles-in-diabetic-retinopathy
#3
REVIEW
Wei Zhang, Song Chen, Ming-Lin Liu
Diabetic retinopathy (DR) is a common complication of diabetes and has been recognized as the leading cause of blindness in adults. Several interrelated molecular pathways are involved in the development of DR. Microvesicles (MVs) are cell membrane vesicles, which carry many biologic molecules, such as mRNAs, microRNAs, transcription factors, membrane lipids, membrane receptors, and other proteins. They may be involved in intercellular communication that can promote inflammation, angiogenesis, and coagulation...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713159/co-delivery-of-docetaxel-and-silibinin-using-ph-sensitive-micelles-improves-therapy-of-metastatic-breast-cancer
#4
Xin-Yue Dong, Tian-Qun Lang, Qi Yin, Peng-Cheng Zhang, Ya-Ping Li
Breast cancer is the most vicious killer for women, and tumor metastasis is one of the leading causes of breast cancer therapy failure. In this study, a new pH-sensitive polymer (polyethylene glycol-block-poly[(1,4-butanediol)-diacrylate-β-N,N-diisopropylethylenediamine], BDP) was synthesized. Based on BDP, docetaxel/silibinin co-delivery micelles (DSMs) was constructed. DSM had a well-defined spherical shape under the transmission electron microscope with average hydrodynamic diameter of 85.3±0.4 nm, and were stable in the bloodstream but could dissociate to release the chemotherapeutic agents in the low pH environment of the endo/lysosomes in the tumor cells...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713158/amyloid-beta-structure-biology-and-structure-based-therapeutic-development
#5
REVIEW
Guo-Fang Chen, Ting-Hai Xu, Yan Yan, Yu-Ren Zhou, Yi Jiang, Karsten Melcher, H Eric Xu
Amyloid beta peptide (Aβ) is produced through the proteolytic processing of a transmembrane protein, amyloid precursor protein (APP), by β- and γ-secretases. Aβ accumulation in the brain is proposed to be an early toxic event in the pathogenesis of Alzheimer's disease, which is the most common form of dementia associated with plaques and tangles in the brain. Currently, it is unclear what the physiological and pathological forms of Aβ are and by what mechanism Aβ causes dementia. Moreover, there are no efficient drugs to stop or reverse the progression of Alzheimer's disease...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713157/population-pharmacokinetics-of-moxifloxacin-and-its-concentration-qt-interval-relationship-modeling-in-chinese-healthy-volunteers
#6
Feng-Yan Xu, Ji-Han Huang, Ying-Chun He, Li-Yu Liang, Lu-Jin Li, Juan Yang, Fang Yin, Ling Xu, Qing-Shan Zheng, Kun Wang
Moxifloxacin (MX) is an 8-methoxyquinolone antimicrobial drug, which is often used as a positive control in thorough QT (TQT) studies. In the present study we established the population pharmacokinetics model of MX and the relationship of MX concentrations with the QT and various corrected QT (QTc) intervals, and compared the results with other ethnicities. The MX data used for modeling were obtained from a published TQT interval prolongation study of antofloxacin with MX as the positive control. In this four-period crossover study, 24 adult Chinese healthy volunteers received either 200 or 400 mg of oral antofloxacin once daily, 400 mg of MX, or a placebo...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713156/discovery-of-a-novel-calcium-sensitive-fluorescent-probe-for-%C3%AE-ketoglutarate
#7
Lin-Lin Gan, Lin-Hai Chen, Fa-Jun Nan
α-Ketoglutarate (α-KG), a pivotal metabolite in energy metabolism, has been implicated in nonalcoholic fatty liver disease (NAFLD) and several cancers. It is recently proposed that plasma α-KG is a surrogate biomarker of NAFLD. Here, we report the development of a novel "turn-on" chemosensor for α-KG that contains a coumarin moiety as a fluorophore. Using benzothiazole-coumarin (BTC) as inspiration, we designed a probe for calcium ion recognition that possesses a unique fluorophore compared with previously reported probes for α-KG measurement...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28713155/hypoxia-induces-universal-but-differential-drug-resistance-and-impairs-anticancer-mechanisms-of-5-fluorouracil-in-hepatoma-cells
#8
Jing-Qiu Li, Xian Wu, Lu Gan, Xiang-Liang Yang, Ze-Hong Miao
Hepatocellular carcinoma (HCC) is one of the most refractory cancers. The mechanisms by which hypoxia further aggravates therapeutic responses of advanced HCC to anticancer drugs remain to be clarified. Here, we report that hypoxia (1% O2) caused 2.55-489.7-fold resistance to 6 anticancer drugs (sorafenib, 5-fluorouracil [5-FU], gemcitabine, cisplatin, adriamycin and 6-thioguanine) in 3 HCC cell lines (BEL-7402, HepG2 and SMMC-7721). Among the 6 drugs, sorafenib, the sole one approved for HCC therapy, inhibited proliferation with little influence from hypoxia and displayed the smallest variation among the 3 HCC cell lines tested...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649132/reassessment-of-subacute-mptp-treated-mice-as-animal-model-of-parkinson-s-disease
#9
Qiu-Shuang Zhang, Yang Heng, Zheng Mou, Ju-Yang Huang, Yu-He Yuan, Nai-Hong Chen
1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) mouse model remains the most commonly used animal model of Parkinson's disease (PD). There are three MPTP-treatment schemes: acute, subacute and chronic. Considering the advantages of the period and similarity to PD, the subacute model was often chosen to assess the validity of new candidates, but the changes caused by the subacute MPTP treatment and the appropriate positive control for this model remain to be further confirmed. The aim of this study was: 1 to estimate the value of the subacute MPTP mouse model in aspects of behavioral performance, biochemical changes and pathological abnormalities, and 2 to find effective positive drugs...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649131/blocking-the-utilization-of-glucose-induces-the-switch-from-senescence-to-apoptosis-in-pseudolaric-acid-b-treated-human-lung-cancer-cells-in-vitro
#10
Guo-Dong Yao, Jing Yang, Xiu-Xiu Li, Xiao-Yu Song, Toshihiko Hayashi, Shin-Ichi Tashiro, Satoshi Onodera, Shao-Jiang Song, Takashi Ikejima
Pseudolaric acid B (PAB), a diterpene acid isolated from the root bark of Pseudolarix kaempferi Gordon, exerts anti-tumor effects in several cancer cell lines. Our previous study showed that PAB mainly induced senescence via p53-p21 activation rather than apoptosis in suppression of the growth of human lung cancer A549 cells (p53 wild-type). In p53-null human lung cancer H1299 cells, however, PAB caused apoptosis without senescence. In this study we investigated what mechanism was responsible for the switch from senescence to apoptosis in PAB-treated human lung cancer cell lines...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649130/dopamine-d2-receptor-antagonist-sulpiride-enhances-dexamethasone-responses-in-the-treatment-of-drug-resistant-and-metastatic-breast-cancer
#11
Jian Li, Qing-Yu Yao, Jun-Sheng Xue, Li-Jie Wang, Yin Yuan, Xiu-Yun Tian, Hong Su, Si-Yuan Wang, Wen-Jun Chen, Wei Lu, Tian-Yan Zhou
Recent evidence shows that dopamine D2-like receptor (D2DR) antagonists, such as trifluoperazine and thioridazine, are effective for cancer therapy and inhibition of cancer stem-like cells (CSCs). In this study, we investigated the anti-cancer effects of combination therapy of dexamethasone (DEX) and sulpiride (SUL), an atypical antipsychotic, against drug-resistant and metastatic breast cancers and further explored the underlying mechanisms. Oral administration of SUL (25, 100 mg·kg(-1)·d(-1)) alone did not inhibit the tumor growth in human breast cancer MCF-7/Adr xenograft model, but dose-dependently decreased the proportion of CSCs in vitro and in vivo...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649129/c33-s-a-novel-pde9a-inhibitor-protects-against-rat-cardiac-hypertrophy-through-upregulating-cgmp-signaling
#12
Pan-Xia Wang, Zhuo-Ming Li, Si-Dong Cai, Jing-Yan Li, Ping He, Yi Huang, Guo-Shuai Feng, Hai-Bin Luo, Shao-Rui Chen, Pei-Qing Liu
Phosphodiesterase-9A (PDE9A) expression is upregulated during cardiac hypertrophy and heart failure. Accumulating evidence suggests that PDE9A might be a promising therapeutic target for heart diseases. The present study sought to investigate the effects and underlying mechanisms of C33(S), a novel selective PDE9A inhibitor, on cardiac hypertrophy in vitro and in vivo. Treatment of neonatal rat cardiomyocytes (NRCMs) with PE (100 μmol/L) or ISO (1 μmol/L) induced cardiac hypertrophy characterized by significantly increased cell surface areas and increased expression of fetal genes (ANF and BNP)...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649128/lx2343-alleviates-cognitive-impairments-in-ad-model-rats-by-inhibiting-oxidative-stress-induced-neuronal-apoptosis-and-tauopathy
#13
Xiao-Dan Guo, Guang-Long Sun, Ting-Ting Zhou, Yi-Yang Wang, Xin Xu, Xiao-Fan Shi, Zhi-Yuan Zhu, Vatcharin Rukachaisirikul, Li-Hong Hu, Xu Shen
Alzheimer's disease (AD) is a progressive neurodegenerative disease leading to the irreversible loss of brain neurons and cognitive abilities, and the vicious interplay between oxidative stress (OS) and tauopathy is believed to be one of the major players in AD development. Here, we demonstrated the capability of the small molecule N-(1,3-benzodioxol-5-yl)-2-[5-chloro-2-methoxy(phenylsulfonyl)anilino]acetamide (LX2343) to ameliorate the cognitive dysfunction of AD model rats by inhibiting OS-induced neuronal apoptosis and tauopathy...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649127/the-novel-%C3%AE-glucan-ycp-improves-the-survival-rates-and-symptoms-in-septic-mice-by-regulating-myeloid-derived-suppressor-cells
#14
Dan Liu, Ming You, Guang-Feng Zhao, Xiu-Jun Li, Yu-Xian Song, Huan Dou, Wen-Bing Yao, Xiang-Dong Gao, Ya-Yi Hou
Sepsis is a life-threatening health condition that is initially characterized by uncontrolled inflammation, followed by the development of persistent immunosuppression. YCP is a novel α-glucan purified from the mycelium of the marine fungus Phoma herbarum YS4108, which has displayed strong antitumor activity via enhancing host immune responses. In this study, we investigated whether YCP could influence the development of sepsis in a mouse model. Caecal ligation and puncture (CLP)-induced sepsis was established in mice that were treated with YCP (20 mg/kg, ip or iv) 2 h before, 4 and 24 h after the CLP procedure, and then every other day...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28649126/cis-stilbene-glucoside-in-polygonum-multiflorum-induces-immunological-idiosyncratic-hepatotoxicity-in-lps-treated-rats-by-suppressing-ppar-%C3%AE
#15
Ya-Kun Meng, Chun-Yu Li, Rui-Yu Li, Lan-Zhi He, He-Rong Cui, Ping Yin, Cong-En Zhang, Peng-Yan Li, Xiu-Xiu Sang, Ya Wang, Ming Niu, Ya-Ming Zhang, Yu-Ming Guo, Rong Sun, Jia-Bo Wang, Zhao-Fang Bai, Xiao-He Xiao
The root of Polygonum multiflorum Thunb (PM) has been used in China to treat a variety of diseases, such as constipation, early graying of the hair and hyperlipemia. Recent evidence shows that PM causes idiosyncratic drug-induced liver injury (IDILI) in humans. In this study, we investigated the molecular basis of PM-induced liver injury in a rat model of IDILI based on a non-hepatotoxic dose of LPS. SD rats were orally administered 3 potentially hepatotoxic compounds of PM: cis-stilbene glucoside (cis-SG, 50 mg/kg), trans-SG (50 mg/kg) or emodin (5 mg/kg), followed by injection of LPS (2...
June 26, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552915/the-regioselective-glucuronidation-of-morphine-by-dimerized-human-ugt2b7-1a1-1a9-and-their-allelic-variants
#16
Zi-Zhao Yang, Li Li, Lu Wang, Ling-Min Yuan, Ming-Cheng Xu, Jing-Kai Gu, Hui-di Jiang, Lu-Shan Yu, Su Zeng
Uridine diphosphate-glucuronosyltransferase (UGT) 2B7 is expressed mostly in the human liver, lung and kidney and can transfer endogenous glucuronide group into its substrate and impact the pharmacological effects of several drugs such as estriol, AZT and morphine. UGT2B7 and its allelic variants can dimerize with the homologous enzymes UGT1A1 and UGT1A9, as well as their allelic variants, and then change their enzymatic activities in the process of substrate catalysis. The current study was designed to identify this mechanism using morphine as the substrate of UGT2B7...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552913/population-pharmacokinetic-analysis-of-tacrolimus-in-chinese-myasthenia-gravis-patients
#17
Yu-Si Chen, Zi-Qi Liu, Rong Chen, Lei Wang, Ling Huang, Xiao Zhu, Tian-Yan Zhou, Wei Lu, Ping Ma
The importance of tacrolimus in the treatment of myasthenia gravis (MG) as a substitute for corticosteroid-dependent immunosuppressive therapy is increasing. Thus far, however, no population pharmacokinetic (PopPK) analysis of tacrolimus in treating MG patients has been published. This article aimed to construct a PopPK model of tacrolimus for Chinese MG patients with the goal of improving its performance in MG treatment. A total of 253 trough concentration records were obtained from 83 Chinese MG patients...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552912/pterostilbene-suppresses-human-endometrial-cancer-cells-in-vitro-by-down-regulating-mir-663b
#18
Ya-Ling Wang, Yuan Shen, Jian-Ping Xu, Kun Han, Yan Zhou, Su Yang, Jun-Yi Yin, Da-Liu Min, Hai-Yan Hu
Resveratrol has long been known as an antioxidant and a chemopreventive agent. Similar to resveratrol, pterostilbene (PT) is also a phenolic compound extracted from the Vitis species. However, there are few studies on the antitumor effect of PT. Thus, we investigated the effects of PT on the endometrial cancer (EC) cells in vitro and the related molecular mechanisms. Treatment of EC cell lines HTB-111 and Ishikawa with PT (25-100 μmol/L) dose-dependently suppressed the cell viability and induced apoptosis...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552911/plumbagin-suppresses-chronic-periodontitis-in-rats-via-down-regulation-of-tnf-%C3%AE-il-1%C3%AE-and-il-6-expression
#19
Xin-Yi Zheng, Chuan-Yuan Mao, Han Qiao, Xi Zhang, Li Yu, Ting-Yu Wang, Eryi Lu
Chronic periodontitis (CP) is one of the most common oral diseases, which causes alveolar bone absorption and tooth loss in adults. In this study we aimed to investigate the potential of plumbagin (PL), a widely-investigated active compound extracted from the traditional Chinese herb Plumbago zeylanica L in treating CP. Human periodontal ligament stem cells (PDLSCs) were used for in vitro studies, whereas an animal model of CP was established in SD rats by ligation+Porphyromonas gingivalis (Pg) stimulation...
May 29, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28552908/xyloketal-b-alleviates-cerebral-infarction-and-neurologic-deficits-in-a-mouse-stroke-model-by-suppressing-the-ros-tlr4-nf-%C3%AE%C2%BAb-inflammatory-signaling-pathway
#20
Ni Pan, Liu-Yi Lu, Mei Li, Guo-Hao Wang, Fang-Yun Sun, Hong-Shuo Sun, Xue-Jun Wen, Jian-Ding Cheng, Jian-Wen Chen, Ji-Yan Pang, Jie Liu, Yong-Yuan Guan, Li-Yan Zhao, Wen-Liang Chen, Guan-Lei Wang
Xyloketal B (Xyl-B) is a novel marine compound isolated from mangrove fungus Xylaria sp. We previously demonstrated that pretreatment with Xyl-B exerted neuroprotective effects and attenuated hypoxic-ischemic brain injury in neonatal mice. In the present study we investigated the neuroprotective effects of pre- and post-treatment with Xyl-B in adult mice using a transient middle cerebral artery occlusion (tMCAO) model, and explored the underlying mechanisms. Adult male C57 mice were subjected to tMCAO surgery...
May 29, 2017: Acta Pharmacologica Sinica
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