Sodium propionate exerts anticancer effect in mice bearing breast cancer cell xenograft by regulating JAK2/STAT3/ROS/p38 MAPK signaling
Acta Pharmacologica Sinica, Published online: 24 September 2020; doi:10.1038/s41401-020-00522-2Sodium propionate exerts anticancer effect in mice bearing breast cancer cell xenograft by regulating JAK2/STAT3/ROS/p38 MAPK signaling (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 24, 2020 Category: Drugs & Pharmacology Authors: Hyun-Soo Park Joo-Hui Han Jeong Won Park Do-Hyung Lee Keun-Woo Jang Miji Lee Kyung-Sun Heo Chang-Seon Myung Source Type: research

α-Galactosylceramide and its analog OCH differentially affect the pathogenesis of ISO-induced cardiac injury in mice
Acta Pharmacologica Sinica, Published online: 24 September 2020; doi:10.1038/s41401-020-00517-zα-Galactosylceramide and its analog OCH differentially affect the pathogenesis of ISO-induced cardiac injury in mice (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 24, 2020 Category: Drugs & Pharmacology Authors: Xin Chen Jie Liu Jie Liu Wen-jia Wang Wen-jing Lai Shu-hui Li Ya-fei Deng Jian-zhi Zhou Sheng-qian Yang Ying Liu Wei-nian Shou Da-yan Cao Xiao-hui Li Source Type: research

Caspase-11/4 and gasdermin D-mediated pyroptosis contributes to podocyte injury in mouse diabetic nephropathy
Acta Pharmacologica Sinica, Published online: 23 September 2020; doi:10.1038/s41401-020-00525-zCaspase-11/4 and gasdermin D-mediated pyroptosis contributes to podocyte injury in mouse diabetic nephropathy (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 23, 2020 Category: Drugs & Pharmacology Authors: Qian Cheng Jing Pan Zhuan-li Zhou Fan Yin Hong-yan Xie Pan-pan Chen Jing-yao Li Pei-qing Zheng Li Zhou Wei Zhang Jun Liu Li-min Lu Source Type: research

Targeted inhibition of calpain in mitochondria alleviates oxidative stress-induced myocardial injury
Acta Pharmacologica Sinica, Published online: 23 September 2020; doi:10.1038/s41401-020-00526-yTargeted inhibition of calpain in mitochondria alleviates oxidative stress-induced myocardial injury (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 23, 2020 Category: Drugs & Pharmacology Authors: Dong Zheng Ting Cao Lu-lu Zhang Guo-chang Fan Jun Qiu Tian-qing Peng Source Type: research

Pharmacological and cardiovascular perspectives on the treatment of COVID-19 with chloroquine derivatives
Acta Pharmacologica Sinica, Published online: 23 September 2020; doi:10.1038/s41401-020-00519-xPharmacological and cardiovascular perspectives on the treatment of COVID-19 with chloroquine derivatives (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 23, 2020 Category: Drugs & Pharmacology Authors: Xiao-lei Zhang Zhuo-ming Li Jian-tao Ye Jing Lu Lingyu Linda Ye Chun-xiang Zhang Pei-qing Liu Dayue D Duan Source Type: research

Berberine inhibits colorectal tumor growth by suppressing SHH secretion.
In conclusion, BBR promotes the degradation of SHH mRNA in colorectal cancer cells, interrupting the paracrine Hedgehog signaling pathway activity thus suppresses the colorectal cancer growth. This study reveals a novel molecular mechanism underlying the anticancer action of BBR. PMID: 32958873 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 21, 2020 Category: Drugs & Pharmacology Authors: Shen ZQ, Wang J, Tan WF, Huang TM Tags: Acta Pharmacol Sin Source Type: research

Berberine inhibits colorectal tumor growth by suppressing SHH secretion
Acta Pharmacologica Sinica, Published online: 21 September 2020; doi:10.1038/s41401-020-00514-2Berberine inhibits colorectal tumor growth by suppressing SHH secretion (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 21, 2020 Category: Drugs & Pharmacology Authors: Zhu-qing Shen Juan Wang Wen-fu Tan Tao-min Huang Source Type: research

Author Correction: Cobrotoxin could be an effective therapeutic for COVID-19.
Abstract An amendment to this paper has been published and can be accessed via a link at the top of the paper. PMID: 32948824 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 18, 2020 Category: Drugs & Pharmacology Authors: Lin F, Reid PF, Qin ZH Tags: Acta Pharmacol Sin Source Type: research

Activation of GPR120 in podocytes ameliorates kidney fibrosis and inflammation in diabetic nephropathy.
Abstract Diabetic nephropathy (DN) is one of the most common causes of end-stage renal disease worldwide. ω3-Fatty acids (ω3FAs) were found to attenuate kidney inflammation, glomerulosclerosis, and albuminuria in experimental and clinical studies of DN. As G protein-coupled receptor 120 (GPR120) was firstly identified as the receptor of ω3FAs, we here investigated the function of GPR120 in DN. We first examined the renal biopsies of DN patients, and found that GPR120 expression was negatively correlated with the progression of DN. Immunofluorescence staining analysis revealed that GPR120 protein ...
Source: Acta Pharmacologica Sinica - September 18, 2020 Category: Drugs & Pharmacology Authors: Wei TT, Yang LT, Guo F, Tao SB, Cheng L, Huang RS, Ma L, Fu P Tags: Acta Pharmacol Sin Source Type: research

Activation of GPR120 in podocytes ameliorates kidney fibrosis and inflammation in diabetic nephropathy
Acta Pharmacologica Sinica, Published online: 18 September 2020; doi:10.1038/s41401-020-00520-4Activation of GPR120 in podocytes ameliorates kidney fibrosis and inflammation in diabetic nephropathy (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 18, 2020 Category: Drugs & Pharmacology Authors: Tian-tian Wei Le-tian Yang Fan Guo Si-bei Tao Lu Cheng Rong-shuang Huang Liang Ma Ping Fu Source Type: research

Author Correction: Cobrotoxin could be an effective therapeutic for COVID-19
Acta Pharmacologica Sinica, Published online: 18 September 2020; doi:10.1038/s41401-020-00533-zAuthor Correction: Cobrotoxin could be an effective therapeutic for COVID-19 (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 18, 2020 Category: Drugs & Pharmacology Authors: Fang Lin Paul F. Reid Zheng-hong Qin Source Type: research

Melittin ameliorates inflammation in mouse acute liver failure via inhibition of PKM2-mediated Warburg effect.
In this study we investigated the potential therapeutic effects of melittin, a major peptide component of bee venom both in mice model of ALF and in LPS-stimulated macrophages in vitro, and elucidated the underlying mechanisms. ALF was induced in mice by intraperitoneal injection of D-galactosamine/LPS. Then the mice were treated with melittin (2, 4, and 8 mg/kg, ip). We showed that melittin treatment markedly improved mortality, attenuated severe symptoms and signs, and alleviated hepatic inflammation in D-galactosamine/LPS-induced ALF mice with the optimal dose being 4 mg/kg. In addition, melittin within th...
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Fan XG, Pei SY, Zhou D, Zhou PC, Huang Y, Hu XW, Li T, Wang Y, Huang ZB, Li N Tags: Acta Pharmacol Sin Source Type: research

Emerging roles of class I PI3K inhibitors in modulating tumor microenvironment and immunity.
Abstract Immune system-mediated tumor killing has revolutionized anti-tumor therapies, providing long-term and durable responses in some patients. The phosphoinositide 3-kinase (PI3K) pathway controls multiple biological processes and is frequently dysregulated in malignancies. Enormous efforts have been made to develop inhibitors against class I PI3K. Notably, with the increasing understanding of PI3K, it has been widely accepted that PI3K inhibition not only restrains tumor progression, but also reshapes the immunosuppressive tumor microenvironment. In this review, we focus on the pivotal roles of class I PI3Ks ...
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Sun P, Meng LH Tags: Acta Pharmacol Sin Source Type: research

Catalpol counteracts the pathology in a mouse model of Duchenne muscular dystrophy by inhibiting the TGF- β1/TAK1 signaling pathway.
In conclusion, catalpol can restore skeletal muscle strength and alleviate skeletal muscle damage in aged mdx mice, thus may provide a novel therapy for DMD. Catalpol attenuates muscle fibrosis by inhibiting the TGF-β1/TAK1 signaling pathway. PMID: 32939036 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Xu DQ, Zhao L, Li SJ, Huang XF, Li CJ, Sun LX, Li XH, Zhang LY, Jiang ZZ Tags: Acta Pharmacol Sin Source Type: research

HDAC6 is critical for ketamine-induced impairment of dendritic and spine growth in GABAergic projection neurons.
This study reveals a novel role of HDAC6 as a regulator for ketamine-induced deficits in the morphological development of MSNs and provides an innovative method for prevention and treatment with respect to ketamine clinical applications. PMID: 32939037 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Li X, Saiyin H, Zhou JH, Yu Q, Liang WM Tags: Acta Pharmacol Sin Source Type: research

Melittin ameliorates inflammation in mouse acute liver failure via inhibition of PKM2-mediated Warburg effect
Acta Pharmacologica Sinica, Published online: 16 September 2020; doi:10.1038/s41401-020-00516-0Melittin ameliorates inflammation in mouse acute liver failure via inhibition of PKM2-mediated Warburg effect (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Xue-gong Fan Si-ya Pei Dan Zhou Peng-cheng Zhou Yan Huang Xing-wang Hu Teng Li Yang Wang Ze-bing Huang Ning Li Source Type: research

Catalpol counteracts the pathology in a mouse model of Duchenne muscular dystrophy by inhibiting the TGF-β1/TAK1 signaling pathway
Acta Pharmacologica Sinica, Published online: 16 September 2020; doi:10.1038/s41401-020-00515-1Catalpol counteracts the pathology in a mouse model of Duchenne muscular dystrophy by inhibiting the TGF-β1/TAK1 signaling pathway (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Deng-qiu Xu Lei Zhao Si-jia Li Xiao-fei Huang Chun-jie Li Li-xin Sun Xi-hua Li Lu-yong Zhang Zhen-zhou Jiang Source Type: research

Emerging roles of class I PI3K inhibitors in modulating tumor microenvironment and immunity
Acta Pharmacologica Sinica, Published online: 16 September 2020; doi:10.1038/s41401-020-00500-8Emerging roles of class I PI3K inhibitors in modulating tumor microenvironment and immunity (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Pu Sun Ling-hua Meng Source Type: research

HDAC6 is critical for ketamine-induced impairment of dendritic and spine growth in GABAergic projection neurons
Acta Pharmacologica Sinica, Published online: 16 September 2020; doi:10.1038/s41401-020-00521-3HDAC6 is critical for ketamine-induced impairment of dendritic and spine growth in GABAergic projection neurons (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 16, 2020 Category: Drugs & Pharmacology Authors: Xuan Li Hexige Saiyin Jian-hua Zhou Qiong Yu Wei-min Liang Source Type: research

Quercetin prevents bone loss in hindlimb suspension mice via stanniocalcin 1-mediated inhibition of osteoclastogenesis.
In conclusion, Quer protects bones and prevents unloading-caused bone loss in mice through STC1-mediated inhibition of osteoclastogenesis. The findings suggest that Quer has the potential to prevent and treat off-load bone loss as an alternative supplement. PMID: 32934346 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 15, 2020 Category: Drugs & Pharmacology Authors: Niu YB, Yang YY, Xiao X, Sun Y, Zhou YM, Zhang YH, Dong D, Li CR, Wu XL, Li YH, Mei QB Tags: Acta Pharmacol Sin Source Type: research

Pyrazolone derivative C29 protects against HFD-induced obesity in mice via activation of AMPK in adipose tissue.
Abstract Beige adipocytes have been considered as a potential strategy in anti-obesity therapy because of its thermogenic capacity. AMP-activated protein kinase (AMPK) plays important roles in regulating adipose tissue function. C29 is a novel pyrazolone derivative with AMPK activity. In the current study, we investigated the role of C29 in the regulation of thermogenesis using differentiated adipocytes and diet-induced obese mice, and explored the mechanisms that might be involved in energy expenditure via adipocyte AMPK activation. We showed that treatment with C29 (2.5-10 μM) concentration-dependently...
Source: Acta Pharmacologica Sinica - September 15, 2020 Category: Drugs & Pharmacology Authors: Li BH, Zhang M, Duan YN, Shuai L, Jiang HW, Li J, Nan FJ, Li JY Tags: Acta Pharmacol Sin Source Type: research

Quercetin prevents bone loss in hindlimb suspension mice via stanniocalcin 1-mediated inhibition of osteoclastogenesis
Acta Pharmacologica Sinica, Published online: 15 September 2020; doi:10.1038/s41401-020-00509-zQuercetin prevents bone loss in hindlimb suspension mice via stanniocalcin 1-mediated inhibition of osteoclastogenesis (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 15, 2020 Category: Drugs & Pharmacology Authors: Yin-bo Niu Yuan-yuan Yang Xuan Xiao Yang Sun Yu-mei Zhou Yu-han Zhang Dong Dong Chen-rui Li Xiang-long Wu Yu-hua Li Qi-bing Mei Source Type: research

Pyrazolone derivative C29 protects against HFD-induced obesity in mice via activation of AMPK in adipose tissue
Acta Pharmacologica Sinica, Published online: 15 September 2020; doi:10.1038/s41401-020-00524-0Pyrazolone derivative C29 protects against HFD-induced obesity in mice via activation of AMPK in adipose tissue (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 15, 2020 Category: Drugs & Pharmacology Authors: Bo-han Li Mei Zhang Ya-nan Duan Lin Shuai Hao-wen Jiang Jia Li Fa-jun Nan Jing-ya Li Source Type: research

SAF-189s, a potent new-generation ROS1 inhibitor, is active against crizotinib-resistant ROS1 mutant-driven tumors.
Abstract The ROS1 fusion kinase is an attractive antitumor target. Though with significant clinical efficacy, the well-known first-generation ROS1 inhibitor (ROS1i) crizotinib inevitably developed acquired resistance due to secondary point mutations in the ROS1 kinase. Novel ROS1is effective against mutations conferring secondary crizotinib resistance, especially G2032R, are urgently needed. In the present study, we evaluated the antitumor efficacy of SAF-189s, the new-generation ROS1/ALK inhibitor, against ROS1 fusion wild-type and crizotinib-resistant mutants. We showed that SAF-189s potently inhibited ROS1 kina...
Source: Acta Pharmacologica Sinica - September 11, 2020 Category: Drugs & Pharmacology Authors: Xia ZJ, Ji YC, Sun DQ, Peng X, Gao YL, Fang YF, Zhao XD, Wang WB, Ding J, Geng MY, Ai J Tags: Acta Pharmacol Sin Source Type: research

SAF-189s, a potent new-generation ROS1 inhibitor, is active against crizotinib-resistant ROS1 mutant-driven tumors
Acta Pharmacologica Sinica, Published online: 11 September 2020; doi:10.1038/s41401-020-00513-3SAF-189s, a potent new-generation ROS1 inhibitor, is active against crizotinib-resistant ROS1 mutant-driven tumors (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 11, 2020 Category: Drugs & Pharmacology Authors: Zong-jun Xia Yin-chun Ji De-qiao Sun Xia Peng Ying-lei Gao Yan-fen Fang Xing-dong Zhao Wei-bo Wang Jian Ding Mei-yu Geng Jing Ai Source Type: research

Drp1-dependent mitochondrial fission in cardiovascular disease.
Abstract Mitochondria are highly dynamic organelles undergoing cycles of fusion and fission to modulate their morphology, distribution, and function, which are referred as 'mitochondrial dynamics'. Dynamin-related protein 1 (Drp1) is known as the major pro-fission protein whose activity is tightly regulated to clear the damaged mitochondria via mitophagy, ensuring a strict control over the intricate process of cellular and organ dynamics in heart. Various posttranslational modifications (PTMs) of Drp1 have been identified including phosphorylation, SUMOylation, palmitoylation, ubiquitination, S-nitrosylation, and ...
Source: Acta Pharmacologica Sinica - September 10, 2020 Category: Drugs & Pharmacology Authors: Jin JY, Wei XX, Zhi XL, Wang XH, Meng D Tags: Acta Pharmacol Sin Source Type: research

Drp1-dependent mitochondrial fission in cardiovascular disease
Acta Pharmacologica Sinica, Published online: 10 September 2020; doi:10.1038/s41401-020-00518-yDrp1-dependent mitochondrial fission in cardiovascular disease (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 10, 2020 Category: Drugs & Pharmacology Authors: Jia-yu Jin Xiang-xiang Wei Xiu-ling Zhi Xin-hong Wang Dan Meng Source Type: research

Feasibility study of 68Ga-labeled CAR  T cells for in vivo tracking using micro-positron emission tomography imaging.
In this study we used 68Ga, a commercially available short-lived positron emitter, to label CAR T cells for noninvasive cell tracking in vivo. CAR T cells could be tracked in vivo by 68Ga-PET imaging for at least 6 h. We showed a significant correlation between the distribution of 89Zr and 68Ga-labeled CAR T cells in the same tissues (lungs, liver, and spleen). The distribution and homing behavior of CAR T cells at the early period is highly correlated with the long-term fate of CAR T cells in vivo. And the effective absorbed dose of 68Ga-labeled CAR T cells is only one twenty-fourth of 89Zr-labeled CAR T ...
Source: Acta Pharmacologica Sinica - September 8, 2020 Category: Drugs & Pharmacology Authors: Wang XY, Wang Y, Wu Q, Liu JJ, Liu Y, Pan DH, Qi W, Wang LZ, Yan JJ, Xu YP, Wang GJ, Miao LY, Yu L, Yang M Tags: Acta Pharmacol Sin Source Type: research

Feasibility study of 68Ga-labeled CAR T cells for in vivo tracking using micro-positron emission tomography imaging
Acta Pharmacologica Sinica, Published online: 08 September 2020; doi:10.1038/s41401-020-00511-5Feasibility study of 68Ga-labeled CAR T cells for in vivo tracking using micro-positron emission tomography imaging (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 8, 2020 Category: Drugs & Pharmacology Authors: Xin-yu Wang Yan Wang Qiong Wu Jing-jing Liu Yu Liu Dong-hui Pan Wei Qi Li-zhen Wang Jun-jie Yan Yu-ping Xu Guang-ji Wang Li-yan Miao Lei Yu Min Yang Source Type: research

CP-25, a compound derived from paeoniflorin: research advance on its pharmacological actions and mechanisms in the treatment of inflammation and immune diseases.
Abstract Total glycoside of paeony (TGP) has been widely used to treat inflammation and immune diseases in China. Paeoniflorin (Pae) is the major active component of TGP. Although TGP has few adverse drug reactions, the slow onset and low bioavailability of Pae limit its clinical use. Enhanced efficacy without increased toxicity is pursued in developing new agents for inflammation and immune diseases. As a result, paeoniflorin-6'-O-benzene sulfonate (CP-25) derived from Pae, is developed in our group, and exhibits superior bioavailability and efficacy than Pae. Here we describe the development process and research...
Source: Acta Pharmacologica Sinica - September 3, 2020 Category: Drugs & Pharmacology Authors: Yang XZ, Wei W Tags: Acta Pharmacol Sin Source Type: research

CP-25, a compound derived from paeoniflorin: research advance on its pharmacological actions and mechanisms in the treatment of inflammation and immune diseases
Acta Pharmacologica Sinica, Published online: 03 September 2020; doi:10.1038/s41401-020-00510-6CP-25, a compound derived from paeoniflorin: research advance on its pharmacological actions and mechanisms in the treatment of inflammation and immune diseases (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - September 3, 2020 Category: Drugs & Pharmacology Authors: Xue-zhi Yang Wei Wei Source Type: research

Metformin and cancer immunity.
Abstract The immune system plays an essential and central role in tumor cell differentiation, proliferation, angiogenesis, apoptosis, invasion, and metastasis. Over the past decade, cancer therapy has rapidly evolved from traditional approaches, such as surgery, chemotherapy, and radiotherapy, to revolutionary new treatment options with immunotherapy. This new era of cancer treatment options has now been clinically tested and applied to many forms of human malignancies, often with quite dramatic results. As we develop more effective combinations of cancer treatment, several agents have been recently investigated, ...
Source: Acta Pharmacologica Sinica - August 31, 2020 Category: Drugs & Pharmacology Authors: Ma R, Yi B, Riker AI, Xi Y Tags: Acta Pharmacol Sin Source Type: research

DL0410 ameliorates cognitive disorder in SAMP8 mice by promoting mitochondrial dynamics and the NMDAR-CREB-BDNF pathway.
In this study, we investigated the therapeutic effect of DL0410 and its action mechanism in SAMP8 mice. DL0410 (1-10 mg·kg-1·d-1) was orally administered to 8-month-old SAMP mice (SAMP8) for 8 weeks. We showed that DL0410 administration effectively ameliorated the cognitive deficits in the Morris water maze test, novel object recognition test, and nest building test. We revealed that DL0410 dose-dependently increased the expression levels of the mitochondrial proteins (PGC-1α, Mitofusin 2, OPA1, and Drp1), and subsequently ameliorated the processes of mitochondrial biosynthesis, fusion, and fissi...
Source: Acta Pharmacologica Sinica - August 31, 2020 Category: Drugs & Pharmacology Authors: Lian WW, Zhou W, Zhang BY, Jia H, Xu LJ, Liu AL, Du GH Tags: Acta Pharmacol Sin Source Type: research

10,11-dehydrocurvularin exerts antitumor effect against human breast cancer by suppressing STAT3 activation.
In this study we identified 10,11-dehydrocurvularin (DCV), a natural-product macrolide derived from marine fungus, as a selective STAT3 inhibitor. We showed that DCV (2-8 μM) dose-dependently inhibited the proliferation, migration and invasion of human breast cancer cell lines MDA-MB-231 and MDA-MB-468, and induced cell apoptosis. In the two breast cancer cell lines, DCV selectively inhibited the phosphorylation of STAT3 Tyr-705, but did not affect the upstream components JAK1 and JAK2, as well as dephosphorylation of STAT3. Furthermore, DCV treatment strongly inhibited IFN-γ-induced STAT3 phosphorylation but had ...
Source: Acta Pharmacologica Sinica - August 31, 2020 Category: Drugs & Pharmacology Authors: Zhao Q, Bi Y, Zhong J, Li X, Guo J, Liu YX, Pan LR, Tan Y, Deng ZS, Yu XJ Tags: Acta Pharmacol Sin Source Type: research

DL0410 ameliorates cognitive disorder in SAMP8 mice by promoting mitochondrial dynamics and the NMDAR-CREB-BDNF pathway
Acta Pharmacologica Sinica, Published online: 31 August 2020; doi:10.1038/s41401-020-00506-2DL0410 ameliorates cognitive disorder in SAMP8 mice by promoting mitochondrial dynamics and the NMDAR-CREB-BDNF pathway (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 31, 2020 Category: Drugs & Pharmacology Authors: Wen-wen Lian Wei Zhou Bao-yue Zhang Hao Jia Lv-jie Xu Ai-lin Liu Guan-hua Du Source Type: research

10,11-dehydrocurvularin exerts antitumor effect against human breast cancer by suppressing STAT3 activation
Acta Pharmacologica Sinica, Published online: 31 August 2020; doi:10.1038/s41401-020-0499-y10,11-dehydrocurvularin exerts antitumor effect against human breast cancer by suppressing STAT3 activation (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 31, 2020 Category: Drugs & Pharmacology Authors: Qun Zhao Yun Bi Jing Zhong Xiang Li Jian Guo Ying-xiang Liu Long-rui Pan Yan Tan Zhang-shuang Deng Xian-jun Yu Source Type: research

Metformin and cancer immunity
Acta Pharmacologica Sinica, Published online: 31 August 2020; doi:10.1038/s41401-020-00508-0Metformin and cancer immunity (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 31, 2020 Category: Drugs & Pharmacology Authors: Ruixia Ma Bin Yi Adam I. Riker Yaguang Xi Source Type: research

Sulfation predominates the pharmacokinetics, metabolism, and excretion of forsythin in humans: major enzymes and transporters identified.
Abstract Forsythin extracted from Forsythiae Fructus is widely used to treat fever caused by the common cold or influenza in China, Japan and Korea. The present study aimed to analyze the pharmacokinetics, metabolism and excretion routes of forsythin in humans and determine the major enzymes and transporters involved in these processes. After a single oral administration, forsythin underwent extensive metabolism via hydrolysis and further sulfation. In total, 3 of the 13 metabolites were confirmed by comparison to reference substances, i.e., aglycone M1, M1 sulfate (M2), and M1 glucuronide (M7). Hydrolysis was the...
Source: Acta Pharmacologica Sinica - August 28, 2020 Category: Drugs & Pharmacology Authors: Pan LL, Yang Y, Hui M, Wang S, Li CY, Zhang H, Ding YH, Fu L, Diao XX, Zhong DF Tags: Acta Pharmacol Sin Source Type: research

Pyrroloquinoline quinone promotes mitochondrial biogenesis in rotenone-induced Parkinson's disease model via AMPK activation.
Abstract Mitochondrial dysfunction is considered to be one of the important pathogenesis in Parkinson's disease (PD). We previously showed that pyrroloquinoline quinone (PQQ) could protect SH-SY5Y cells and dopaminergic neurons from cytotoxicity and prevent mitochondrial dysfunction in rotenone-induced PD models. In the present study we investigated the mechanisms underlying the protective effects of PQQ in a mouse PD model, which was established by intraperitoneal injection of rotenone (3 mg·kg-1·d-1, ip) for 3 weeks. Meanwhile the mice were treated with PQQ (0.8, 4, 20 mg·kg-1&...
Source: Acta Pharmacologica Sinica - August 28, 2020 Category: Drugs & Pharmacology Authors: Cheng Q, Chen J, Guo H, Lu JL, Zhou J, Guo XY, Shi Y, Zhang Y, Yu S, Zhang Q, Ding F Tags: Acta Pharmacol Sin Source Type: research

Pyrroloquinoline quinone promotes mitochondrial biogenesis in rotenone-induced Parkinson’s disease model via AMPK activation
Acta Pharmacologica Sinica, Published online: 28 August 2020; doi:10.1038/s41401-020-0487-2Pyrroloquinoline quinone promotes mitochondrial biogenesis in rotenone-induced Parkinson’s disease model via AMPK activation (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 28, 2020 Category: Drugs & Pharmacology Authors: Qiong Cheng Juan Chen Hui Guo Jin-li Lu Jing Zhou Xin-yu Guo Yue Shi Yu Zhang Shu Yu Qi Zhang Fei Ding Source Type: research

Sulfation predominates the pharmacokinetics, metabolism, and excretion of forsythin in humans: major enzymes and transporters identified
Acta Pharmacologica Sinica, Published online: 28 August 2020; doi:10.1038/s41401-020-0481-8Sulfation predominates the pharmacokinetics, metabolism, and excretion of forsythin in humans: major enzymes and transporters identified (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 28, 2020 Category: Drugs & Pharmacology Authors: Lu-lu Pan Yong Yang Min Hui Shuo Wang Cui-yun Li Hong Zhang Yan-hua Ding Li Fu Xing-xing Diao Da-fang Zhong Source Type: research

ABT-199 inhibits Hedgehog pathway by acting as a competitive inhibitor of oxysterol, rather as a BH3 mimetic.
In this study, we identify that FDA approved drug ABT-199 significantly and selectively inhibits the Hh pathway. Mechanistically, ABT-199 acts as a competitive inhibitor of oxysterol by potentially targeting the cysteine rich domain (CRD) of Smo, rather as a BH3 mimetic. ABT-199 obviously inhibits the growth of Hh-driven tumors and possesses capacity of combating the primary and acquired resistance to Smo inhibitors caused by Smo mutations. Our data reposition ABT-199 as a Smo inhibitor for treating Hh-driven tumors, especially for those bearing Smo mutations and resistant to current Smo inhibitors. Meanwhile, our findings...
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Wang J, Zhang Y, Huang WJ, Yang J, Tang WG, Huang TM, Tan WF Tags: Acta Pharmacol Sin Source Type: research

Deficiency of β-arrestin2 exacerbates inflammatory arthritis by facilitating plasma cell formation.
In this study we tried to elucidate the molecular mechanisms underlying β-arr2 depletion-induced exacerbation of CAIA. CAIA was induced in β-arr2-/- and wild-type (WT) mice by injection of collagen antibodies and LPS. The mice were sacrificed on d 13 after the injection, spleen, thymus and left ankle joints were collected for analysis. Arthritis index (AI) was evaluated every day or every 2 days. We showed that β-arr2-/- mice with CAIA had a further increase in the percentage of plasma cells in spleen as compared with WT mice with CAIA, which was in accordance with elevated serum IgG1 and IgG2A expressi...
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Zhou WJ, Wang DD, Tao J, Tai Y, Zhou ZW, Wang Z, Guo PP, Sun WY, Chen JY, Wu HX, Yan SX, Zhang LL, Wang QT, Wei W Tags: Acta Pharmacol Sin Source Type: research

Drug development in targeting ion channels for brain edema.
Abstract Cerebral edema is a pathological hallmark of various central nervous system (CNS) insults, including traumatic brain injury (TBI) and excitotoxic injury such as stroke. Due to the rigidity of the skull, edema-induced increase of intracranial fluid significantly complicates severe CNS injuries by raising intracranial pressure and compromising perfusion. Mortality due to cerebral edema is high. With mortality rates up to 80% in severe cases of stroke, it is the leading cause of death within the first week. Similarly, cerebral edema is devastating for patients of TBI, accounting for up to 50% mortality. Curr...
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Luo ZW, Ovcjak A, Wong R, Yang BX, Feng ZP, Sun HS Tags: Acta Pharmacol Sin Source Type: research

Ruscogenin attenuates particulate matter-induced acute lung injury in mice via protecting pulmonary endothelial barrier and inhibiting TLR4 signaling pathway.
In conclusion, RUS effectively alleviates PM-induced ALI probably by inhibition of vascular leakage and TLR4/MyD88 signaling. TLR4 might be crucial for PM to initiate pulmonary lesion and for RUS to exert efficacy against PM-induced lung injury. PMID: 32855531 [PubMed - as supplied by publisher] (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Wang YW, Wu YH, Zhang JZ, Tang JH, Fan RP, Li F, Yu BY, Kou JP, Zhang YY Tags: Acta Pharmacol Sin Source Type: research

Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma.
Abstract Diffuse large B-cell lymphoma (DLBCL) is the most widespread type of non-Hodgkin lymphoma (NHL). As the most aggressive form of the DLBCL, the activated B-cell-like (ABC) subtype is often resistant to standard chemotherapies. Bruton's tyrosine kinase (BTK) inhibitor ibrutinib provides a potential therapeutic approach for the DLBCL but fails to improve the outcome in the phase III trial. In the current study, we investigated the molecular mechanisms underlying ibrutinib resistance and explored new combination therapy with ibrutinib. We generated an ibrutinib-resistant ABC-DLBCL cell line (OCI-ly10-IR) thro...
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Zhang XT, Hu XB, Wang HL, Kan WJ, Xu L, Wang ZJ, Xiang YQ, Wu WB, Feng B, Li JN, Gao AH, Dong TC, Xia CM, Zhou YB, Li J Tags: Acta Pharmacol Sin Source Type: research

ABT-199 inhibits Hedgehog pathway by acting as a competitive inhibitor of oxysterol, rather as a BH3 mimetic
Acta Pharmacologica Sinica, Published online: 27 August 2020; doi:10.1038/s41401-020-00504-4ABT-199 inhibits Hedgehog pathway by acting as a competitive inhibitor of oxysterol, rather as a BH3 mimetic (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Juan Wang Yu Zhang Wen-jing Huang Jun Yang Wei-guo Tang Tao-min Huang Wen-fu Tan Source Type: research

Drug development in targeting ion channels for brain edema
Acta Pharmacologica Sinica, Published online: 27 August 2020; doi:10.1038/s41401-020-00503-5Drug development in targeting ion channels for brain edema (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Zheng-wei Luo Andrea Ovcjak Raymond Wong Bao-xue Yang Zhong-ping Feng Hong-shuo Sun Source Type: research

Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma
Acta Pharmacologica Sinica, Published online: 27 August 2020; doi:10.1038/s41401-020-00505-3Activation of unfolded protein response overcomes Ibrutinib resistance in diffuse large B-cell lymphoma (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Xiao-tuan Zhang Xiao-bei Hu Han-lin Wang Wei-juan Kan Lei Xu Zhi-jia Wang Yu-qi Xiang Wen-biao Wu Bo Feng Jia-nan Li An-hui Gao Tian-cheng Dong Chun-mei Xia Yu-bo Zhou Jia Li Source Type: research

Ruscogenin attenuates particulate matter-induced acute lung injury in mice via protecting pulmonary endothelial barrier and inhibiting TLR4 signaling pathway
Acta Pharmacologica Sinica, Published online: 27 August 2020; doi:10.1038/s41401-020-00502-6Ruscogenin attenuates particulate matter-induced acute lung injury in mice via protecting pulmonary endothelial barrier and inhibiting TLR4 signaling pathway (Source: Acta Pharmacologica Sinica)
Source: Acta Pharmacologica Sinica - August 27, 2020 Category: Drugs & Pharmacology Authors: Yu-wei Wang Yun-hao Wu Jia-zhi Zhang Jia-hui Tang Rui-ping Fan Fang Li Bo-yang Yu Jun-ping Kou Yuan-yuan Zhang Source Type: research