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Protective effects of S-propargyl-cysteine controlled release formulationon ischemic disease: hydrogen sulfide-mediated mechanism

Protective effects of S-propargyl-cysteine controlled releas...

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第二届世界天然药物和传统药物药理学学术会议

作者： Cheng-Rong HUANG Jun-Tao KAN Shu-Jun WANG Yi-Zhun ZHU Department of Pharmacology Fudan UniversityShanghai 201203China Department of PharmacologyShenyang Pharmaceutical UniversityShenyang 110016China

AIM S-propargyl-cysteine (SPRC), a structural analog of S-allylcysteine which is a major compound in garlic, has been proved to protect against myocardial ischemia through modulating *** order to produce more stable and sustaining H2S, we developed SPRC controlled release formulation [SPRC (RS)], thenelucidated the protective effects on ischemic disease and the involved mechanisms on apoptosis, oxidation and *** Heart failureandhind-limb ischemia model were induced by left coronary artery occlusion and femoral artery *** indexes were recorded to determine the cardiac *** staining was performed to determine the infarct *** level of H2S was detected by modified sulfide *** of enzyme and expression of protein were determined by colorimetry and Western *** and immunofluorescence were performed to discover the density of *** The cardioprotective effects of SPRC(RS) on HF rats were confirmed by significant reduction of infarct size and improvement of cardiac function, with better effects than normal *** (RS) modulated antioxidant defenses and protected against myocardial *** also promoted angiogenesis in ischemic heart and *** effects of SPRC(RS) were mediated by *** SPRC (RS) played a protective rote in ischemic *** important, it exerted better effects than normal SPRC in all respects, providing a new perspective on H2S-mediated drug therapy.

关键词： SPRC (RS) H2S oxidation apoptosis angiogenesis

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Neuroprotective effect of morroniside on focal cerebral ischemia in rats

Neuroprotective effect of morroniside on focal cerebral isch...

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第二届世界天然药物和传统药物药理学学术会议

作者： Wen WANG Hou-Xi AI Li ZHANG Xuanwu Hospital of Capital Medical University Key Laboratory for Neurodegenerative Diseases of Ministry of EducationBeijing 100053China

To examined whether morroniside could protect ischemia/reperfusion-induced brain injury by minimizing oxidative stress and *** was intragastrically administered to rats in doses of 30, 90 and 270 mg· kg-1 ·d-1, starting 3 h after the onset of middle cerebral artery *** behavioral test was performed by using the Zea-Longa scores, Prehensile Traction score and Ludmila Belayer *** were sacrificed 3 d after ischemia *** infarction volume of brain was assessed in the brain slices stained with 2, 3, 5-triphenyl tetrazolium *** tissues were also used for determination of malondialdehyde levels, glutathione levels and superoxide *** treatment with morroniside significantly improved Zea-Longa scores and Prehensile Traction score at the doses of 30, 90 and 270 mg·kg-1, increased Ludmila Belayer score and reduced the infarction volume at the doses of 90 and 270 rag· *** (30, 90 and 270 mg· kg-1) treatment significantly decreased the level of malondialdehyde in ischemic cortex *** 270 mgo kg-1 treatment significantly increased the content of glutathione,enhanced the activity of superoxide dismutase, but decreased the expression of caspase 3 protein in ischemic cortex *** findings demonstrated that morroniside could significantly protect the brain from damage induced by focal cerebral ischemia which might be related to morroniside antioxidant and anti-apoptotic properties in the brain.

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Anti-influenza viral and anti-inflammatory activities of theaflavin derivatives

Anti-influenza viral and anti-inflammatory activities of the...

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第二届世界天然药物和传统药物药理学学术会议

作者： Mian ZU Wei-Ling ZHOU Ai-Lin LIU Guan-Hua DU Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical CollegeBeijing 100050China Institute of Materia MedicaChinese Academy of Medical Sciences & Peking Union Medical CollegeBeijing 100050China Beijing Key Laboratory of Drug Target and Screening Research Beijing 100050China

AIM The shortage of anti-viral drugs urge us to look for new lead compounds for developing new anti-influenza viral *** drug screening of influenza viral neuramindase (NA) inhibitors, theaflavin (TF) derivatives all displayed NA inhbition, In this paper, their in vitro anti-influenza viral activity and anti-inflammatory activity were *** The in vitro antiviral activities were evaluated by cytopathic effect (CPE) reduction assay, their action mechanisms were studied by NA activity assay, a haemagglutination (HA) inhibition assay and a real-time quantitative PCR (qPCR) assay for gene expression of HA, their anti-inflammatory activity were evaluated by cytokine secretion *** The experimental results showed that TF derivatives all exerted anti-influenza viral activities, their inhibitory effects on the NA of three distinct influenza virus strains, and they also displayed an inhibitory effect on *** addition, they decreased the expression level of the inflammatory cytokine IL-6 during viral *** We can concluded that TF derivatives are potential compounds with anti-influenza viral replication and anti-inflammatory properties, which will provide information for novel antiviral drug design and development.

关键词： antiviral anti-inflammatory influenza virus theaflavin derivatives

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Therapeutic effects of icarrin on amyloid-β burden in a mouse model of Alzheimer's disease

Therapeutic effects of icarrin on amyloid-β burden in a mou...

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第二届世界天然药物和传统药物药理学学术会议

作者： Lan ZHANG Jin CHU Ru-Yi ZHANG Ying XING Lin LI Department of Pharmacology Xuanwu Hospital of Capital Medical UniversityKey Laboratory for Neurodegenerative Diseases of Ministry of EducationBeijing 100053China

AIM To investigate the effect and pharmacological mechanism of icarrin (ICA), which is the main component extracted from a traditional Chinese epimedium herb, on Aβ production in AD-like APP transgenic *** PDAPPV717I transgenic (Tg) mice were randomly divided into model group and ICA treated (at doses 30 and 100 μmol· kg-1· d-1) *** was orally administered to Tg mice with an age range 4-10 *** burden of Aβ was measured by ELISA and *** amyloid senile plaques were detected by Congo red staining and Bielschowsky silver *** expression of APP and BACE-1 were measured by immunohistochemistry and Western *** co-expression of Aβ with amyloid fibers was detected by applying double labeled *** Orally administered ICA decreased the number of amyloid senile plaques in hippocampus of Tg *** immunohistochemical examination of brain sections stained with polyclonal anti-A3 antibody showed reduced Aβ burden,and Aβ levels were also decreased in the insoluble fractions of brain homogenates, as determined by *** expression of APP and BACE-1 in hippocampus was significantly decreased in ICA treated *** ICA could reduce the Aβ burden and plaque deposits in the hippocampus of APP transgenic mice through depressing the expression of APP and *** may have a promising application prospect in treatment of AD.

关键词： Alzheimer' s disease APPV717I transgenic mice β-amyloid icarrin

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New perspectives on current drug discovery from herbal medicines

New perspectives on current drug discovery from herbal medic...

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第二届世界天然药物和传统药物药理学学术会议

作者： Si-Yuan PAN Kam-Ming KO Shu-Feng ZHOU Si-Hua GAO Dik-Lung MA Shuo-Feng ZHANG Zhi-Ling YU Jian-Ning SUN Yi-Fan HAN Wang-Fun FONG Beijing University of Chinese Medicine BeijingChina Hong Kong University of Science & TechnologyHong KongChina University of South FloridaTampaFloridaUSA Hong Kong Baptist UniversityHong KongChina Hong Kong Polytechnic UniversityHong KongChina

The low success rate, despite a huge capital investment, has made the research and development of conventional drugs very *** the past few decades, researchers have focused on drug discovery from herbal medicines or botanical *** a long history of herbal usage for the clinical management of a variety of diseases in indigenous cultures, the success rate of developing a new drug from herbal medicinal preparations should, in theory, be higher than that from chemical *** the endeavor for drug discovery from herbal medicines is 'experience-driven', the search for a therapeutically useful synthetic drug, like 'looking for a needle in a haystack', is a daunting *** this article, we first illustrated various approaches of drug discovery from herbal *** examples of successful drug discovery were *** addition, problems in drug discovery from herbal medicines were described and possible solutions *** prospect of drug discovery from herbal medicines in the post-genomic era was made with the provision of future directions in this area of drug development.

关键词： drug discovery herbal medicine ecological ethics post-genomic era systems pharmacology database,artemisinin Fructus Schisandrae chinensis

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NMDA receptor regulation by Liu-Wei-Di-Huang Decoction accounts for its enhancement of LTP in SAMP8 hippocampal slices

NMDA receptor regulation by Liu-Wei-Di-Huang Decoction accou...

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第二届世界天然药物和传统药物药理学学术会议

作者： Yan HU ANG He-Ping ZHANG Zeng-Yao HU Gang LIU Sheng YANG Wen-Xia ZHOU Yong-Xiang ZHANG Beijing Institute of Pharmacology and Toxicology Beijing 100850China

AIM Previous pharmacological studies demonstrated that LW could ameliorate the decline of the learning and memory in senescence accelerated mouse/prone 8 (SAMP8), but the mechanism has not been well ***-containing serum (LWCS) was used in this study to elucidate the possible *** 6-month-old SAMP8 was used in this study to investigate the effect of LWCS on the induction of long-term potentiation (LTP).Primary cultured hippocampal neurons were used in this study to investigate the effects of LWCS on [Ca2 +] i, ICa and N-methyl-D-aspartate (NMDA)-evoked currents.[Ca2 +] i was imaged using Fluo-3 and whole-cell patch recordings were applied to study the ICa and NMDA-evoked *** We find that LWCS facilitates the induction of LTP in hippocampal slices of 6-month-old *** primary cultured hippocampal neurons, LWCS increases intracellular [Ca2 +] i, the ICa is suppressed by LWCS, and NMDA-evoked currents are *** These results indicate that LW improves the synaptic plasticity by inhibiting voltage-dependent calciumchannels and promoting the function of NMDA *** improvement might be one of the mechanisms contributing to cognitive improvement effect of LW.

关键词： Liu-Wei-Di-Huang Decoction long-term potentiation

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NHBA isolated from Gastrodia data exerts sedative and hypnotic effects

NHBA isolated from Gastrodia data exerts sedative and hypnot...

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第二届世界天然药物和传统药物药理学学术会议

作者： Ying ZHANG Min LI Jian-Jun ZHANG State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicoChinese Academy of Medical Sciences and Peking Union Medical CollegeBeijing 100050China

The rhizomes of Gastrodia data have been used for the treatment of insomnia in oriental countries.N6-(4-hydroxybenzyl) adenine riboside (NHBA) was originally isolated from *** the first time we report a detailed study on the effects and mechanisms of NHBA on its sedative and hypnotic ***, an endogenous sleep factor, regulates sleep-wake cycle via interacting with adenosine A1/A2A *** radioligand binding studies and cAMP accumulation assays, our results show that NHBA may be a functional ligand for the adenosine A1 and A2A *** significantly decreases spontaneous locomotor activity and potentiates the hypnotic effect of sodium pentobarbital in *** architecture analyses reveal that NHBA significantly decreases wakefulness time and increases NREM sleep ***, NHBA does not affect the amount of REM *** with the adenosine A1 receptor antagonist DPCPX or the A2A receptor antagonist SCH 58261 significantly reverses the increase in sleeping time induced by NHBA in sodium pentobarbital treated *** studies show that NHBA increases c-Fos expression in GABAergic neurons of the ventrolateral preoptic area (VLPO), which suggests that NHBA activates the sleep center in the anterior ***, these results indicate that NHBA produces significant sedative and hypnotic *** effects might be mediated by the activation of adenosine A1/A2A receptors and stimulation of the sleep center VLPO.

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Verticinone presents antinociceptive effect mediated by opioid systems

Verticinone presents antinociceptive effect mediated by opio...

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第二届世界天然药物和传统药物药理学学术会议

作者： Hao LI Zhe-Kai MAO Xu-Lin XU Qing LU Lian-Jun GUO German Class 2008 of Clinical Medicine Huazhong University of Science and TechnologyWuhan 430030China Department of PharmacologyTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China

AIM This study was designed to assess the antinociceptive effect of verticinone and to evaluate the involvement of opioid receptors *** In vivo nociceptive response was induced by hot-plate test and the hind paw withdrawal latencies (HWLS) of mice during thermal stimulation were measured before and repeated at 10, 15, 30, 45 and 60 min after verticinone(0.5 mg·kg-1, icy.) *** vitro guinea pig ileum(GPI) bioassay is relatively selective for mu opioid receptor and is used for define the action of mu *** inhibitory effect of verticinone on electric stimulus-induced contration of myenterio plexuslongitudinal muscle strip (MPLM) from GPI was *** Verticinone(0.5 mg·kg-1, icv.) presented anticociceptive effect in hot-plate test in mice and the effect was completely prevented by naloxone, the non-selective antagonist at mu, delta, and kappa opioid *** vitro study in the MPLM from GPI verticinoe showed weak inhibition on the electric stimulus-induced contraction, and the effect could not be reversed by naloxone, while morphine inhibited electric stimulus-induced contraction of MPLE from GPI and the effect can be reversed by *** The antinociceptive effect of verticinone probably is related to its activation of delta or kappa opioid receptor, but not mu-opioid receptor.

关键词： verticinone opioid ileum

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Association between the pharmacology and herbal quality in Chinese medicine

Association between the pharmacology and herbal quality in C...

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第二届世界天然药物和传统药物药理学学术会议

作者： Yi-Tao WANG Simon Ming Yuen LEE Xiu-Ping CHEN Mei-Wan CHEN Jin-Jian LU State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical SciencesUniversity of MacauMacaoChina

Focusing on the critical academic areas that restricting the quality of Chinese medicine, the project has carried out systematic study on the association between the pharmacology and herbal quality in Chinese medicine aiming at dissecting their relationships based on modem scientific *** and formulas under the three classical categories, Huoxue, Fuzheng and Qingre, were chosen for investigation of their pharmacological properties with latest ideas and novel technologies in the *** project performed systematic investigations of the beneficial effects of Chinese medicine such as anti-cancer, cardio-and cerobrovascular protection, anti-virus activities and the associated quality evaluation on more than ten representative regional Chinese herbs, including Panax notoginseng, Salvia miltiorrhiza, Angelica sinensis, Ganoderma lucidum, Coptis chinensis Franch, Radix Puerariae and so *** than thirty pharmacological assays have been established and several thousands herb samples have been systematically ***, more than 10 major active ingredients have been identified from Chinese *** pharmacological efficacy of the Chinese herbs in the three main classical categories and their potential mechanisms of actions have been *** addition, the association of drug safety and drug delivery systems on systematic quality evaluation has also been *** project provides new insight into mechanism of action of Chinese medicine and rationales for further development of clinical use of Chinese medicine.

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A new compound TCD inhibits the growth and migration of cancer cells and its molecular mechanisms of action in vitro and in vivo

A new compound TCD inhibits the growth and migration of canc...

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第二届世界天然药物和传统药物药理学学术会议

作者： Guo-Ying ZHANG Jian-Wen YAO Kun LIU Lin-Lin CHEN Xin LIU Fu-Jia SUN De-Xin JI Hua-Rong ZHANG Laboratory of Molecular Pharmacology School of PharmacyYantai UniversityYantai 264005China

Our previous results indicated that theanine and courmarin have some anticancer activities although the activities are not very *** order to enhance the anticancer activity of theanine and develop new anticancer agents, we synthesized new compounds,theanine-courmarin-derivatives (TCD) with theanine and *** results have shown that TCD has much stronger activity than either theanine or courmarin on reduction of the viability and migration as well as tumor growth in the tumor-bearing *** results indicated that TCD strongly reduced a serial of protein expressions and/or phosphorylation related to the growth and migration as well as metastasis of the cancer *** enhanced the expressions of Bax, caspase 3, PARP-I, p53 and p21 proteins and decreased the expressions and/or phosphorylation of Bcl-2, vascular endothelial growth factor receptor (VEGFR), cyclin D, AKT, and NF-κ*** further confirmed that inhibition of the signaling pathway of VEGFR-PI3K/Akt-NF-κB is the important molecular mechanism of action of TCD against the cancer cell growth and *** results suggest that TCD may have the wide therapeutic and/or adjuvant therapeutic application in the treatment cancer.

关键词： theanine-courmarin-derivatives cancer growth and migration suppression vascular endothelial growth factor receptor PI3K/Akt-NF-κB pathway

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