journal
MENU ▼
Read by QxMD icon Read
search

Acta Pharmacologica Sinica

journal
https://www.readbyqxmd.com/read/28065935/two-birds-one-stone-dual-targeting-of-the-cancer-cell-surface-and-subcellular-mitochondria-by-the-galectin-3-binding-peptide-g3-c12
#1
Wei Sun, Lian Li, Qing-Qing Yang, Zhi-Rong Zhang, Yuan Huang
Active tumor-targeting approaches using specific ligands have drawn considerable attention over the years. However, a single ligand often fails to simultaneously target the cancer cell surface and subcellular organelles, which limits the maximum therapeutic efficacy of delivered drugs. We describe a polymeric delivery system modified with the G3-C12 peptide for sequential dual targeting. In this study, galectin-3-targeted G3-C12 peptide was conjugated onto the N-(2-hydroxypropyl) methacrylamide (HPMA) copolymer for the delivery of D(KLAKLAK)2 (KLA) peptide...
January 9, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28065934/brain-cannabinoid-receptor-2-expression-function-and-modulation
#2
REVIEW
De-Jie Chen, Ming Gao, Fen-Fei Gao, Quan-Xi Su, Jie Wu
Cannabis sativa (marijuana) is a fibrous flowering plant that produces an abundant variety of molecules, some with psychoactive effects. At least 4% of the world's adult population uses cannabis annually, making it one of the most frequently used illicit drugs in the world. The psychoactive effects of cannabis are mediated primarily through cannabinoid receptor (CBR) subtypes. The prevailing view is that CB1Rs are mainly expressed in the central neurons, whereas CB2Rs are predominantly expressed in peripheral immune cells...
January 9, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28042876/the-chk1-inhibitor-mk-8776-increases-the-radiosensitivity-of-human-triple-negative-breast-cancer-by-inhibiting-autophagy
#3
Zhi-Rui Zhou, Zhao-Zhi Yang, Shao-Jia Wang, Li Zhang, Ju-Rui Luo, Yan Feng, Xiao-Li Yu, Xing-Xing Chen, Xiao-Mao Guo
MK-8776 is a recently described inhibitor that is highly selective for checkpoint kinase 1 (Chk1), which can weaken the DNA repair capacity in cancer cells to achieve chemo-sensitization. A number of studies show that MK-8776 enhances the cytotoxicity of hydroxyurea and gemcitabine without increasing normal tissue toxicities. Thus far, there is no evidence that MK-8776 can be used as a radiotherapy sensitization agent. In this study, we investigated the effects of MK-8776 on the radiosensitivity of 3 human triple-negative breast cancer (TNBC) cell lines MDA-MB-231, BT-549 and CAL-51...
January 2, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28042875/the-pik3-mtor-dual-inhibitor-bez235-suppresses-proliferation-and-migration-and-reverses-multidrug-resistance-in-acute-myeloid-leukemia
#4
Lan Deng, Ling Jiang, Xiang-Hua Lin, Kuo-Fu Tseng, Yuan Liu, Xing Zhang, Rui-Hong Dong, Zhi-Gang Lu, Xiu-Ju Wang
Aberrant activation of the PI3K/Akt/mTOR pathway contributes to the proliferation of malignant cells, and may confer resistance to chemotherapy in various malignancies, including acute myeloid leukemia (AML). Chemoresistance is the major reason for relapse in AML. RAD001 (everolimus) has been used at d1 and d7 of an induction chemotherapy regimen for AML, which has acceptable toxicity and may improve conventional chemotherapeutic treatment. Dual inhibitors of PI3K and mTOR overcome some of the intrinsic disadvantages of rapamycin and its derivatives...
January 2, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28042874/in-vitro-assessment-of-the-glucose-lowering-effects-of-berberrubine-9-o-%C3%AE-d-glucuronide-an-active-metabolite-of-berberrubine
#5
Na Yang, Run-Bin Sun, Xing-Long Chen, Le Zhen, Chun Ge, Yu-Qing Zhao, Jun He, Jian-Liang Geng, Jia-Hua Guo, Xiao-Yi Yu, Fei Fei, Si-Qi Feng, Xuan-Xuan Zhu, Hong-Bo Wang, Feng-Hua Fu, Ji-Ye Aa, Guang-Ji Wang
Berberrubine (BRB) is the primary metabolite of berberine (BBR) that has shown a stronger glucose-lowering effect than BBR in vivo. On the other hand, BRB is quickly and extensively metabolized into berberrubine-9-O-β-D-glucuronide (BRBG) in rats after oral administration. In this study we compared the pharmacokinetic properties of BRB and BRBG in rats, and explored the mechanisms underlying their glucose-lowering activities. C57BL/6 mice with HFD-induced hyperglycemia were administered BRB (50 mg·kg(-1)·d(-1), ig) for 6 weeks, which caused greater reduction in the plasma glucose levels than those caused by BBR (120 mg·kg(-1)·d(-1)) or BRB (25 mg·kg(-1)·d(-1))...
January 2, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28042873/a-mini-network-balance-model-for-evaluating-the-progression-of-cardiovascular-complications-in-goto-kakizaki-rats
#6
Hao Jiang, Yu-Hao Wang, Chun-Xiang Wei, Xue Zhang, Hao-Chen Liu, Xiao-Quan Liu
Cardiovascular complications represent a leading cause of mortality in patients with type 2 diabetes mellitus (T2DM). During such complicated progression, subtle variations in the cardiovascular risk (CVR)-related biomarkers have been used to identify cardiovascular disease at the incipient stage. In this study we attempt to integrally characterize the progression of cardiovascular complications and to assess the beneficial effects of metformin combined with salvianolic acid A (Sal A), in Goto-Kakizaki (GK) rats with spontaneous T2DM...
January 2, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28017962/sirt1-plays-a-neuroprotective-role-in-traumatic-brain-injury-in-rats-via-inhibiting-the-p38-mapk-pathway
#7
Hong Yang, Zheng-Tao Gu, Li Li, Mac Maegele, Bi-Ying Zhou, Feng Li, Ming Zhao, Ke-Sen Zhao
Traumatic brain injury (TBI) is a major cause of disability and death in patients who experience a traumatic injury. Mitochondrial dysfunction is one of the main factors contributing to secondary injury in TBI-associated brain damage. Evidence of compromised mitochondrial function after TBI has been, but the molecular mechanisms underlying the pathogenesis of TBI are not well understood. Silent information regulator family protein 1 (SIRT1), a member of the NAD(+)-dependent protein deacetylases, has been shown to exhibit neuroprotective activities in animal models of various pathologies, including ischemic brain injury, subarachnoid hemorrhage and several neurodegenerative diseases...
December 26, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28017961/ginsenoside-rb2-enhances-the-anti-inflammatory-effect-of-%C3%AF-3-fatty-acid-in-lps-stimulated-raw264-7-macrophages-by-upregulating-gpr120-expression
#8
Qi Huang, Ting Wang, He-Yao Wang
Recent studies confirm that chronic low-grade inflammation is closely associated with metabolic syndromes, and anti-inflammatory therapy is a potential approach for treating cardiovascular diseases and type 2 diabetes. Accumulating evidence suggests that GPR120 activation is a feasible solution to ameliorating chronic inflammation and improving glucose metabolism. In this study we investigated whether ginsenoside Rb2 (Rb2), which exhibited regulatory activities in glucose and lipid metabolism, affected GPR120 expression in lipopolysaccharide (LPS)-activated mouse macrophage RAW264...
December 26, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27941804/resveratrol-rescues-hyperglycemia-induced-endothelial-dysfunction-via-activation-of-akt
#9
Jin-Yi Li, Wei-Qiang Huang, Rong-Hui Tu, Guo-Qiang Zhong, Bei-Bei Luo, Yan He
Resveratrol (RSV), a phytoalexin, has shown to prevent endothelial dysfunction and reduce diabetic vascular complications and the risk of cardiovascular diseases. The aim of this study was to investigate the signaling mechanisms underlying the protecting effects of RSV against endothelial dysfunction during hyperglycemia in vitro and in vivo. Human umbilical vein endothelial cells (HUVECs) were treated with RSV, and then exposed to high glucose (HG, 30 mmol/L). Akt-Ser473 phosphorylation, eNOS-Ser1177 phosphorylation, and PTEN protein levels in the cells were detected using Western blot...
December 12, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27917873/dose-biomarker-response-modeling-of-the-anticancer-effect-of-ethaselen-in-a-human-non-small-cell-lung-cancer-xenograft-mouse-model
#10
Suo-Fu Ye, Jian Li, Shuang-Min Ji, Hui-Hui Zeng, Wei Lu
Thioredoxin reductase (TrxR) is a component of several redox-sensitive signaling cascades that mediate important biological processes such as cell survival, maturation, growth, migration and inhibition of apoptosis. The expression levels of TrxR1 in some human carcinoma cell lines are nearly 10 times higher than those in normal cells. Ethaselen is a novel antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR. In this study we explored the relationship between the ethaselen dose and TrxR activity level and the relationship between TrxR degradation and tumor apoptosis in a human lung carcinoma A549 xenograft model...
December 5, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27917872/advances-in-the-study-of-berberine-and-its-derivatives-a-focus-on-anti-inflammatory-and-anti-tumor-effects-in-the-digestive-system
#11
REVIEW
Kun Zou, Zhao Li, Yong Zhang, Hao-Yue Zhang, Bo Li, Wei-Liang Zhu, Ji-Ye Shi, Qi Jia, Yi-Ming Li
It has been widely recognized that inflammation, particularly chronic inflammation, can increase the risk of cancer and that the simultaneous treatment of inflammation and cancer may produce excellent therapeutic effects. Berberine, an alkaloid isolated from Rhizoma coptidis, has broad applications, particularly as an antibacterial agent in the clinic with a long history. Over the past decade, many reports have demonstrated that this natural product and its derivatives have high activity against both cancer and inflammation...
December 5, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27917871/delivery-of-acetylthevetin-b-an-antitumor-cardiac-glycoside-using-polymeric-micelles-for-enhanced-therapeutic-efficacy-against-lung-cancer-cells
#12
Jing-Jing Zhu, Xin-Xin Zhang, Yun-Qiu Miao, Shu-Fang He, Dan-Mei Tian, Xin-Sheng Yao, Jin-Shan Tang, Yong Gan
Acetylthevetin B (ATB), a cardiac glycoside from the seed of Thevetia peruviana (Pers) K Schum (yellow oleander), exhibits not only antitumor activity but also potential cardiac toxicity. In the present study, we attempted to enhance its antitumor action and decrease its adverse effects via chitosan-Pluronic P123 (CP) micelle encapsulation. Two ATB-loaded CP micelles (ATB-CP1, ATB-CP2) were prepared using an emulsion/solvent evaporation technique. They were spherical in shape with a particle size of 40-50 nm, showed a neutral zeta potential, and had acceptable encapsulation efficiency (>90%)...
December 5, 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27890917/sulforaphane-suppresses-emt-and-metastasis-in-human-lung-cancer-through-mir-616-5p-mediated-gsk3%C3%AE-%C3%AE-catenin-signaling-pathways
#13
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
https://www.readbyqxmd.com/read/27890916/polydatin-ameliorates-staphylococcus-aureus-induced-mastitis-in-mice-via-inhibiting-tlr2-mediated-activation-of-the-p38-mapk-nf-%C3%AE%C2%BAb-pathway
#14
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
https://www.readbyqxmd.com/read/27867187/crosstalk-of-ros-rns-and-autophagy-in-silibinin-induced-apoptosis-of-mcf-7-human-breast-cancer-cells-in-vitro
#15
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
https://www.readbyqxmd.com/read/27867186/shenmai-injection-enhances-the-cytotoxicity-of-chemotherapeutic-drugs-against-colorectal-cancers-via-improving-their-subcellular-distribution
#16
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
https://www.readbyqxmd.com/read/27840412/oblongifolin-c-and-guttiferone-k-extracted-from-garcinia-yunnanensis-fruit-synergistically-induce-apoptosis-in-human-colorectal-cancer-cells-in-vitro
#17
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
https://www.readbyqxmd.com/read/27840411/efficacy-of-afatinib-an-irreversible-erbb-family-blocker-in-the-treatment-of-intracerebral-metastases-of-non-small-cell-lung-cancer-in-mice
#18
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
https://www.readbyqxmd.com/read/27840410/rheum-emodin-inhibits-enterovirus-71-viral-replication-and-affects-the-host-cell-cycle-environment
#19
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
https://www.readbyqxmd.com/read/27796295/betulin-from-hedyotis-hedyotidea-ameliorates-concanavalin-a-induced-and-t-cell-mediated-autoimmune-hepatitis-in-mice
#20
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
journal
journal
35064
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"