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Source: Acta Pharmacologica Sinica

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Total 122 results found since Jan 2013.

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 26, 2020 Category: Drugs & Pharmacology Authors: Luo ZW, Ovcjak A, Wong R, Yang BX, Feng ZP, Sun HS Tags: Acta Pharmacol Sin Source Type: research

Methylene blue ameliorates brain edema in rats with experimental ischemic stroke via inhibiting aquaporin 4 expression.
Abstract Brain edema is a common and serious complication of ischemic stroke with limited effective treatment. We previously reported that methylene blue (MB) attenuated ischemic brain edema in rats, but the underlying mechanisms remained unknown. Aquaporin 4 (AQP4) in astrocytes plays a key role in brain edema. We also found that extracellular signal-regulated kinase 1/2 (ERK1/2) activation was involved in the regulation of AQP4 expression in astrocytes. In the present study, we investigated whether AQP4 and ERK1/2 were involved in the protective effect of MB against cerebral edema. Rats were subjected to transie...
Source: Acta Pharmacologica Sinica - July 13, 2020 Category: Drugs & Pharmacology Authors: Shi ZF, Fang Q, Chen Y, Xu LX, Wu M, Jia M, Lu Y, Wang XX, Wang YJ, Yan X, Dong LP, Yuan F Tags: Acta Pharmacol Sin Source Type: research

Icariside II attenuates cerebral ischemia/reperfusion-induced blood-brain barrier dysfunction in rats via regulating the balance of MMP9/TIMP1.
Abstract Cerebral ischemia/reperfusion (I/R) results in harmful consequences during ischemic stroke, especially the disruption of the blood-brain barrier (BBB), which leads to severe hemorrhagic transformation through aggravation of edema and brain hemorrhage. Our previous study demonstrated that icariside II (ICS II), which is derived from Herba Epimedii, attenuates cerebral I/R injury by inhibiting the GSK-3β-mediated activation of autophagy both in vitro and in vivo. However, the effect of ICS II on the BBB remains unclear. Thus, in this study, we investigated the regulation of BBB integrity by ICS II after ce...
Source: Acta Pharmacologica Sinica - June 1, 2020 Category: Drugs & Pharmacology Authors: Liu MB, Wang W, Gao JM, Li F, Shi JS, Gong QH Tags: Acta Pharmacol Sin Source Type: research

Application of targeted therapy strategies with nanomedicine delivery for atherosclerosis.
Abstract Atherosclerosis (AS) is the main pathological cause of coronary heart disease (CHD). Current clinical interventions including statin drugs can effectively reduce acute myocardial infarction and stroke to some extent, but residual risk remains high. The current clinical treatment regimens are relatively effective for early atherosclerotic plaques and can even reverse their progression. However, the effectiveness of these treatments for advanced AS is not ideal, and advanced atherosclerotic plaques-the pathological basis of residual risk-can still cause a recurrence of acute cardiovascular and cerebrovascul...
Source: Acta Pharmacologica Sinica - May 25, 2020 Category: Drugs & Pharmacology Authors: Ou LC, Zhong S, Ou JS, Tian JW Tags: Acta Pharmacol Sin Source Type: research

Melatonin receptor agonist ramelteon attenuates mouse acute and chronic ischemic brain injury.
In this study we investigated whether ramelteon could attenuate cerebral ischemia in mice. Acute focal cerebral ischemia was induced in mice via middle cerebral artery occlusion (MCAO). We found oral administration of ramelteon (3.0 mg/kg) significantly attenuated ischemic injury even when it was given 4 h after the onset of ischemia. We showed that administration of ramelteon (3.0 mg/kg) displayed comparable protective efficacy and length of effective time window as administration of edaravone (10 mg/kg, i.p.), which was used in clinic to treat ischemic stroke. Chronic ischemic brain injury was induced in mice usi...
Source: Acta Pharmacologica Sinica - February 26, 2020 Category: Drugs & Pharmacology Authors: Wu XL, Lu SS, Liu MR, Tang WD, Chen JZ, Zheng YR, Ahsan A, Cao M, Jiang L, Hu WW, Wu JY, Chen Z, Zhang XN Tags: Acta Pharmacol Sin Source Type: research

The lncRNA Malat1 functions as a ceRNA to contribute to berberine-mediated inhibition of HMGB1 by sponging miR-181c-5p in poststroke inflammation.
In this study, we explored the role of lncRNA metastasis-associated lung adenocarcinoma transcript 1 (Malat1) in the process of BBR-induced inhibition of HMGB1 in ischemic brain. Before the 60-min MCAO surgery, the mice were pretreated with BBR (50 mg· kg-1 per day, ig) for 14 days or ICV injected with specific lentiviral vector or shRNA. We showed that MCAO caused marked increase in the expression Malat1 and HMGB1 in the ipsilateral cortex, which was significantly attenuated by pretreatment with BBR. Knockdown of Malat1 attenuated the inflammatory injury after brain ischemia, whereas overexpression of Malat1 exacerba...
Source: Acta Pharmacologica Sinica - August 19, 2019 Category: Drugs & Pharmacology Authors: Cao DW, Liu MM, Duan R, Tao YF, Zhou JS, Fang WR, Zhu JR, Niu L, Sun JG Tags: Acta Pharmacol Sin Source Type: research

Influences of an NR1I2 polymorphism on heterogeneous antiplatelet reactivity responses to clopidogrel and clinical outcomes in acute ischemic stroke patients.
In this study we identified and evaluated the contributions of single nucleotide polymorphisms (SNPs) in NR1I2 and cytochrome P450 (CYP) 2C19 alleles to clopidogrel resistance (CR) and long-term clinical outcomes in acute ischemic stroke (IS) patients. A total of 634 patients with acute IS were recruited, who received antiplatelet medication (clopidogrel or aspirin) every day and completed a 1-year follow-up. The selected SNPs were genotyped, and platelet function was measured. Modified Rankin Scale (mRS) scores and main adverse cardiovascular and cerebrovascular events (MACCE) were noted to assess the prognosis. We showed...
Source: Acta Pharmacologica Sinica - November 28, 2018 Category: Drugs & Pharmacology Authors: Chen YB, Zhou ZY, Li GM, Xiao CX, Yu WB, Zhong SL, Cai YF, Jin J, Huang M Tags: Acta Pharmacol Sin Source Type: research

CID1067700, a late endosome GTPase Rab7 receptor antagonist, attenuates brain atrophy, improves neurologic deficits and inhibits reactive astrogliosis in rat ischemic stroke.
Abstract 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. We found that Rab7 was significantly elev...
Source: Acta Pharmacologica Sinica - October 12, 2018 Category: Drugs & Pharmacology Authors: Qin Y, He Y, Zhu YM, Li M, Ni Y, Liu J, Zhang HL Tags: Acta Pharmacol Sin Source Type: research

Berberine attenuates ischemia-reperfusion injury through inhibiting HMGB1 release and NF- κB nuclear translocation.
In this study, we explored the mechanisms underlying the neuroprotective action of berberine in mice subjected transient middle cerebral artery occlusion (tMCAO). Male mice were administered berberine (25, 50 mg/kg/d, intragastric; i.g.), glycyrrhizin (50 mg/kg/d, intraperitoneal), or berberine (50 mg/kg/d, i.g.) plus glycyrrhizin (50 mg/kg/d, intraperitoneal) for 14 consecutive days before tMCAO. The neurological deficit scores were evaluated at 24 h after tMCAO, and then the mice were killed to obtain the brain samples. We showed that pretreatment with berberine dose-dependently decreased the infarct size, neur...
Source: Acta Pharmacologica Sinica - September 28, 2018 Category: Drugs & Pharmacology Authors: Zhu JR, Lu HD, Guo C, Fang WR, Zhao HD, Zhou JS, Wang F, Zhao YL, Li YM, Zhang YD, Yang CQ, Sun JG Tags: Acta Pharmacol Sin Source Type: research

Increased risk for cerebral ischemic stroke in diabetes: genetically polymorphic CYP mediated production of neuroprotective EETs and sulfonylurea metabolism in relation with KATP channels.
PMID: 30254364 [PubMed - as supplied by publisher]
Source: Acta Pharmacologica Sinica - September 25, 2018 Category: Drugs & Pharmacology Authors: Yasar U, Babaoglu MO Tags: Acta Pharmacol Sin Source Type: research

Predicting functional outcome of ischemic stroke patients in Romania based on plasma CRP, sTNFR-1, D-Dimers, NGAL and NSE measured using a biochip array.
In this study we investigated the utility of a panel of 5 peripheral biomarkers of inflammatory status, neuronal destruction and secondary fibrinolysis in the acute phase of ischemia, and evaluated the impact of these biomarkers on functional outcome after ischemic stroke. The 5 biomarkers (plasma CRP, D-Dimers, sTNFR-1, NGAL and NSE) were measured using a biochip array technology. Eighty nine patients in Romania were divided into 2 subgroups using the modified Rankin Scale evaluated at 3 months after ischemic stroke; the possible impact of analyzed biomarkers on unfavorable functional outcome was tested by binomial logist...
Source: Acta Pharmacologica Sinica - June 21, 2018 Category: Drugs & Pharmacology Authors: Huţanu A, Iancu M, Bălaşa R, Maier S, Dobreanu M Tags: Acta Pharmacol Sin Source Type: research

A11, a novel diaryl acylhydrazone derivative, exerts neuroprotection against ischemic injury in vitro and in vivo.
Abstract There is an urgent need to develop effective therapies for ischemic stroke, but the complicated pathological processes after ischemia make doing so difficult. In the current study, we identified a novel diaryl acylhydrazone derivative, A11, which has multiple neuroprotective properties in ischemic stroke models. First, A11 was demonstrated to induce neuroprotection against ischemic injury in a dose-dependent manner (from 0.3 to 3 μM) in three in vitro experimental ischemic stroke models: oxygen glucose deprivation (OGD), hydrogen peroxide, and glutamate-stimulated neuronal cell injury models. Moreover,...
Source: Acta Pharmacologica Sinica - June 20, 2018 Category: Drugs & Pharmacology Authors: Feng HX, Li CP, Shu SJ, Liu H, Zhang HY Tags: Acta Pharmacol Sin Source Type: research

Positron emission tomography of type 2 cannabinoid receptors for detecting inflammation in the central nervous system.
Abstract Cannabinoid receptor CB2 (CB2R) is upregulated on activated microglia and astrocytes in the brain under inflammatory conditions and plays important roles in many neurological diseases, such as Alzheimer's disease, amyotrophic lateral sclerosis, and ischemic stroke. The advent of positron emission tomography (PET) using CB2R radiotracers has enabled the visualization of CB2R distribution in vivo in animal models of central nervous system inflammation, however translation to humans has been less successful. Several novel CB2R radiotracers have been developed and evaluated to quantify microglial activation. ...
Source: Acta Pharmacologica Sinica - June 19, 2018 Category: Drugs & Pharmacology Authors: Ni R, Mu L, Ametamey S Tags: Acta Pharmacol Sin Source Type: research

Naloxone attenuates ischemic brain injury in rats through suppressing the NIK/IKK α/NF-κB and neuronal apoptotic pathways.
Naloxone attenuates ischemic brain injury in rats through suppressing the NIK/IKKα/NF-κB and neuronal apoptotic pathways. Acta Pharmacol Sin. 2018 Jun 14;: Authors: Wang X, Sun ZJ, Wu JL, Quan WQ, Xiao WD, Chew H, Jiang CM, Li D Abstract Although naloxone has been documented to exert neuroprotection in animal model of cerebral ischemia, the mechanism is not well understood. In this present study we investigated whether naloxone affected the mitochondrial apoptotic pathway in ischemic brain injury of rats. SD rats were subjected to a permanent middle cerebral artery occlusion surgery, and received na...
Source: Acta Pharmacologica Sinica - June 14, 2018 Category: Drugs & Pharmacology Authors: Wang X, Sun ZJ, Wu JL, Quan WQ, Xiao WD, Chew H, Jiang CM, Li D Tags: Acta Pharmacol Sin Source Type: research

Leptin, cardiovascular diseases and type 2 diabetes mellitus.
Abstract Leptin, an adipokine that is implicated in the control of food intake via appetite suppression, may also stimulate oxidative stress, inflammation, thrombosis, arterial stiffness, angiogenesis and atherogenesis. These leptin-induced effects may predispose to the development of cardiovascular diseases. In the present review we discuss the evidence linking leptin levels with the presence, severity and/or prognosis of both coronary artery disease and non-cardiac vascular diseases such as stroke, carotid artery disease, peripheral artery disease (PAD) and abdominal aortic aneurysms (AAA) as well as with chroni...
Source: Acta Pharmacologica Sinica - June 7, 2018 Category: Drugs & Pharmacology Authors: Katsiki N, Mikhailidis DP, Banach M Tags: Acta Pharmacol Sin Source Type: research