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Acta Pharmacologica Sinica

Dan-Dan Liu, Xia Yuan, Shi-Feng Chu, Chen Chen, Qian Ren, Piao Luo, Mei-Yu Lin, Sha-Sha Wang, Tian-Bi Zhu, Qi-di Ai, Ying-da Zang, Dong-Ming Zhang, Xin He, Zhi-Hua Huang, Hong-Shuo Sun, Zhong-Ping Feng, Nai-Hong Chen
Vascular dementia (VD) results from accumulated damage in the vascular system, which is characterized by progressive impairments in memory and cognition and is second only to Alzheimer's disease (AD) in prevalence among all types of dementia. In contrast to AD, there is no FDA-approved treatment for VD owing to its multiple etiologies. In this study, we investigated whether CZ-7, a new derivative of Claulansine F (Clau F) with verified neuroprotective activity in vitro, could ameliorate the cognitive impairment of rats with permanent occlusion of bilateral common carotid arteries (2VO) and its potential mechanisms of action...
October 31, 2018: Acta Pharmacologica Sinica
Jian Meng, Xiao-Yun Liu, Sheng Ma, Hua Zhang, Song-da Yu, Yi-Fan Zhang, Mei-Xia Chen, Xiao-Yu Zhu, Yi Liu, Ling Yi, Xiao-Liang Ding, Xiao-Yan Chen, Li-Yan Miao, Da-Fang Zhong
Pyrotinib is a novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor that is used to treat HER2-positive breast cancer. In this study we investigated the metabolism and disposition of pyrotinib in six healthy Chinese men after a single oral dose of 402 mg of [14 C]pyrotinib. At 240 h postdose, the mean cumulative excretion of the dose radioactivity was 92.6%, including 1.7% in urine and 90.9% in feces. In feces, oxidative metabolites were detected as major drug-related materials and the primary metabolic pathways were O-depicoline (M1), oxidation of pyrrolidine (M5), and oxidation of pyridine (M6-1, M6-2, M6-3, and M6-4)...
October 31, 2018: Acta Pharmacologica Sinica
Yun-Xiao Zhang, De-Zheng Peng, Qing-Feng Zhang, Biao Huang, Qiu-Chu Yang, Dong-Fang Tang, Min-Zhi Chen, Ming-Qiang Rong, Zhong-Hua Liu
Human genetic and pharmacological studies have demonstrated that voltage-gated sodium channels (VGSCs) are promising therapeutic targets for the treatment of pain. Spider venom contains many toxins that modulate the activity of VGSCs. To date, only 0.01% of such spider toxins has been explored, and thus there is a great potential for discovery of novel VGSC modulators as useful pharmacological tools or potential therapeutics. In the current study, we identified a novel peptide, µ-TRTX-Ca1a (Ca1a), in the venom of the tarantula Cyriopagopus albostriatus...
October 31, 2018: Acta Pharmacologica Sinica
Nai-Jun Miao, Hong-Yan Xie, Dan Xu, Jian-Yong Yin, Yan-Zhe Wang, Bao Wang, Fan Yin, Zhuan-Li Zhou, Qian Cheng, Pan-Pan Chen, Li Zhou, Hong Xue, Wei Zhang, Xiao-Xia Wang, Jun Liu, Li-Min Lu
Caspase-11 is a key upstream modulator for activation of inflammatory response under pathological conditions. In this study, we investigated the roles of caspase-11 in the maturation of interleukin-1β (IL-1β) and development of renal interstitial fibrosis in vivo and in vitro. Mice were subjected to unilateral ureteral obstruction (UUO). The mice were treated with either caspase-11 inhibitor wedelolactone (Wed, 30 mg/kg/day, ig) for 7 days or caspase-11 siRNA (10 nmol/20 g body weight per day, iv) for 14 days...
October 31, 2018: Acta Pharmacologica Sinica
Jian-Feng Liu, Jun-Xu Li
Drug addiction is a chronic, relapsing brain disorder. Multiple neural networks in the brain including the reward system (e.g., the mesocorticolimbic system), the anti-reward/stress system (e.g., the extended amygdala), and the central immune system, are involved in the development of drug addiction and relapse after withdrawal from drugs of abuse. Preclinical and clinical studies have demonstrated that it is promising to control drug addiction by pharmacologically targeting the addiction-related systems in the brain...
October 31, 2018: Acta Pharmacologica Sinica
Hai-Cheng Wang, Peng Wang, Yuan-Wei Chen, Yan Zhang
Fibronectin (FN) is a main component of extracellular matrix (ECM) in most adult tissues. Under pathological conditions, particularly inflammation, wound healing and tumors, an alternatively spliced exon extra domain A (EDA) is included in the FN protein (EDA+ FN), which facilitates cellular proliferation, motility, and aggressiveness in different lesions. In this study we investigated the effects of EDA+ FN on bone destruction in human radicular cysts and explored the possibility of editing FN gene or blocking the related paracrine signaling pathway to inhibit the osteoclastogenesis...
October 31, 2018: Acta Pharmacologica Sinica
Lei Chen, Zhi-Lai Yang, Juan Cheng, Ping-Ping Zhang, Le-Sha Zhang, Xue-Sheng Liu, Lie-Cheng Wang
Propofol is an intravenous anesthetic that can active γ-aminobutyric acid A (GABAA ) receptors and generate sedative-hypnotic effects. Propofol has been widely applied clinically to achieve sedation comparable to sleep in humans. The basal forebrain (BF) is a brain region that plays an important role in sleep-wake regulation. Previous studies suggest that propofol affects the sleep-wake circuit via the BF; however, the mechanism remains elusive. In the current study we investigated the effects of propofol on the inherent properties of cholinergic neurons and their ability to convert excitatory inputs into spikes in mouse BF slices using whole-cell patch clamp recordings...
October 26, 2018: Acta Pharmacologica Sinica
Fang Zhang, Yue Zhou, Xiao Yang, Ai-Zhen Xiong, Zheng-Tao Wang, Li Yang
Recently, hepatic sinusoidal obstruction syndrome (HSOS) caused by herbal preparations containing pyrrolizidine alkaloids (PAs), such as Gynura Rhizoma (Tusanqi), has gained global attention. However, the lack of a reliable and reproducible animal model has greatly hampered mechanistic studies. Therefore, we aimed to establish a reproducible HSOS mouse model and investigate the hepatotoxic mechanism. The model was established by intragastrical administration of Gynura Rhizoma extract, i.e., 1.0 g extract/kg per day (equal to 16...
October 26, 2018: Acta Pharmacologica Sinica
Li-Lan Sun, Tao-Yi Yang, Ning-Ning Wei, Wei Lu, Wen-Xuan Jiao, Qi-Qi Zhou, Yong-Zhen Miao, Qin Gao, Xin-Tong Wang, Qi Sun, KeWei Wang
The α7 nicotinic acetylcholine receptor (α7 nAChR) is a ligand-gated Ca2+ -permeable homopentameric ion channel implicated in cognition and neuropsychiatric disorders. Pharmacological enhancement of α7 nAChR function has been suggested for improvement of cognitive deficits. In the present study, we characterized a thiazolyl heterocyclic derivative, 6-(2-chloro-6-methylphenyl)-2-((3-fluoro-4-methylphenyl)amino)thiazolo[4,5-d]pyrimidin-7(6H)-one (JWX-A0108), as a novel type I α7 nAChR positive allosteric modulator (PAM), and evaluated its ability to reverse auditory gating and spatial working memory deficits in mice...
October 17, 2018: Acta Pharmacologica Sinica
Man Wu, Yuan-Zhi Lao, Hong-Sheng Tan, Guang Lu, Yi Ren, Zhao-Qing Zheng, Juan Yi, Wen-Wei Fu, Han-Ming Shen, Hong-Xi Xu
Lysosomes are the terminal organelles of the autophagic-endocytic pathway and play a key role in the degradation of autophagic contents. We previously reported that a natural compound oblongifolin C (OC) increased the number of autophagosomes and impaired the degradation of P62, most likely via suppression of lysosomal function and blockage of autophagosome-lysosome fusion. However, the precise mechanisms of how OC inhibits the lysosome-autophagy pathway remain unclear. In the present study, we investigated the effect of OC on transcription factor EB (TFEB), a master regulator of lysosomal biogenesis, lysosomal function and autophagy...
October 17, 2018: Acta Pharmacologica Sinica
Dai Lu, Sri Sujana Immadi, Zhixing Wu, Debra A Kendall
The cannabinoid type-1 (CB1 ) receptor, a G-protein-coupled receptor, is an attractive target for drug discovery due to its involvement in many physiological processes. Historically, drug discovery efforts targeting the CB1 receptor have focused on the development of orthosteric ligands that interact with the active site to which endogenous cannabinoids bind. Research performed over the last several decades has revealed substantial difficulties in translating CB1 orthosteric ligands into druggable candidates...
October 17, 2018: Acta Pharmacologica Sinica
Joo-Hyun Lee, Yeong-Jin Choo, Yong-Hun Lee, Jin-Ho Rhim, Soo-Han Lee, Byung-Moon Choi, Sung-Tae Oh, Kyu-Taek Choi, Gyu-Jeong Noh
In order to maintain stable blood pressure and heart rate during surgery, anesthesiologists need to administer the appropriate amount of fluid with appropriate fluid type to the patient, then quantifying how fluid is distributed and eliminated from the body is useful for establishing a fluid administration strategy. In this study we characterized the volume kinetics of Ringer's lactate solution in patients undergoing open gastrectomy. When propofol and remifentanil reached a pseudosteady state at the target concentration and blood pressure was stabilized following surgical stimulation, enrolled patients were administered 1000 mL of Ringer's lactate solution for 20 min, followed by continuous infusion at a rate of 6 mL/kg/h until the time of the last blood collection for volume kinetic analysis...
October 16, 2018: Acta Pharmacologica Sinica
Olajide E Olaleye, Wei Niu, Fei-Fei Du, Feng-Qing Wang, Fang Xu, Salisa Pintusophon, Jun-Lan Lu, Jun-Ling Yang, Chuan Li
ShenMai, an intravenous injection prepared from steamed Panax ginseng roots (Hongshen) and Ophiopogon japonicus roots (Maidong), is used as an add-on therapy for coronary artery disease and cancer; saponins are its bioactive constituents. Since many saponins inhibit human organic anion-transporting polypeptides (OATP)1B, this investigation determined the inhibition potencies of circulating ShenMai saponins on the transporters and the joint potential of these compounds for ShenMai-drug interaction. Circulating saponins and their pharmacokinetics were characterized in rats receiving a 30-min infusion of ShenMai at 10 mL/kg...
October 16, 2018: Acta Pharmacologica Sinica
Wei Tang, Ren Guo, Shi-Jun Shen, Yang Zheng, Yu-Ting Lu, Meng-Meng Jiang, Xue Cui, Ci-Zhong Jiang, Xin Xie
Human liver or hepatocyte transplantation is limited by a severe shortage of donor organs. Direct reprogramming of other adult cells into hepatic cells may offer a solution to this problem. In a previous study, we have generated hepatocyte-like cells from mouse fibroblasts using only one transcription factor (TF) plus a chemical cocktail. Here, we show that human urine-derived epithelial-like cells (hUCs) can also be transdifferentiated into human hepatocyte-like cells (hiHeps) using one TF (Foxa3, Hnf1α, or Hnf4α) plus the same chemical cocktail CRVPTD (C, CHIR99021; R, RepSox; V, VPA; P, Parnate; T, TTNPB; and D, Dznep)...
October 12, 2018: Acta Pharmacologica Sinica
Xiao-Hong Deng, Jing-Jing Liu, Xian-Jun Sun, Jing-Cheng Dong, Jian-Hua Huang
The traditional Chinese medicine "Fuzi" (Aconiti Lateralis Radix Praeparata) and its three representative alkaloids, aconitine (AC), benzoylaconine (BAC), and aconine, have been shown to increase mitochondrial mass. Whether Fuzi has effect on mitochondrial biogenesis and the underlying mechanisms remain unclear. In the present study, we focused on the effect of BAC on mitochondrial biogenesis and the underlying mechanisms. We demonstrated that Fuzi extract and its three components AC, BAC, and aconine at a concentration of 50 μM significantly increased mitochondrial mass in HepG2 cells...
October 12, 2018: Acta Pharmacologica Sinica
Wen-Bo Zhou, Xin-Xin Zhang, Yun Cai, Wu Sun, Hao Li
Tamoxifen (TMX) is an antiestrogen drug that is used in the treatment and prevention of all stages of estrogen-dependent breast cancer. Adverse effects of TMX include hepatotoxicity. In this study, we investigated the therapeutic effects of osthole, isolated from medicinal plants especially Fructus Cnidii, on TMX-induced acute liver injury in mice. Mice were injected with osthole (100 mg/kg, ip) or vehicle, followed by TMX (90 mg/kg, ip) 24 h later. We showed that a single injection of TMX-induced liver injury and oxidative stress...
October 12, 2018: Acta Pharmacologica Sinica
Yuan Qin, Yang He, Yong-Ming Zhu, Min Li, Yong Ni, Jin Liu, Hui-Ling Zhang
Increasing evidence suggests that Ras-related in brain 7 (Rab7), an endosome-localized small GTPase contributes to cerebral ischemic brain injury. In the present study, we investigated the role of Rab7 in ischemic stroke-induced formation of astrogliosis and glial scar. Rats were subjected to transient middle cerebral artery occlusion (tMCAO); the rats were injected with the Rab7 receptor antagonist CID1067700 (CID). Primary astrocytes were subjected to an oxygen and glucose deprivation and reoxygenation (OGD/Re) procedure; CID was added to the cell culture media...
October 12, 2018: Acta Pharmacologica Sinica
Shi-Long Jiang, Yi-di Guan, Xi-Sha Chen, Peng Ge, Xin-Luan Wang, Yuan-Zhi Lao, Song-Shu Xiao, Yi Zhang, Jin-Ming Yang, Xiao-Jun Xu, Dong-Sheng Cao, Yan Cheng
Autophagy, a form of cellular self-digestion by lysosome, is associated with various disease processes including cancers, and modulating autophagy has shown promise in the treatment of various malignancies. A number of natural products display strong antitumor activity, yet their mechanisms of action remain unclear. To gain a better understanding of how traditional Chinese medicine agents exert antitumor effects, we screened 480 natural compounds for their effects on autophagy using a high content screening assay detecting GFP-LC3 puncta in HeLa cells...
October 12, 2018: Acta Pharmacologica Sinica
Shu-Jun Chen, Yao Xu, Ye-Mei Liang, Ying Cao, Jin-Yan Lv, Jian-Xin Pang, Ping-Zheng Zhou
Hyperpolarization-activated cyclic nucleotide-gated (HCN) channels play a critical role in controlling pacemaker activity in both heart and nervous system. Developing HCN channel inhibitors has been proposed to be an important strategy for the treatment of pain, heart failure, arrhythmias, and epilepsy. One HCN channel inhibitor, ivabradine, has been clinically approved for the treatment of angina pectoris and heart failure. In this study, we designed and synthesized eight alkanol amine derivatives, and assessed their effects on HCN channels expressed in COS7 cells using a whole-cell patch clamp method...
October 12, 2018: Acta Pharmacologica Sinica
Xian-Bo Huang, Chun-Mei Yang, Qing-Mei Han, Xiu-Jin Ye, Wen Lei, Wen-Bin Qian
Although the treatment of adult T-cell acute lymphoblastic leukemia (T-ALL) has been significantly improved, the heterogeneous genetic landscape of the disease often causes relapse. Aberrant activation of mammalian target of rapamycin (mTOR) pathway in T-ALL is responsible for treatment failure and relapse, suggesting that mTOR inhibition may represents a new therapeutic strategy. In this study, we investigated whether the mTOR complex 1 (mTORC1) inhibitor everolimus could be used as a therapeutic agent against human T-ALL...
October 8, 2018: Acta Pharmacologica Sinica
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