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OBJECTIVE： To study analgesic and anti-inflammatory effects of sophocarpine （SC） on inflammatory pain model mice and related COX-2/PGE2 signaling pathway. METHODS： （1）Analgesic experiment. Totally 50 mice were randomly divided into blank control group （normal saline）， positive control group （aspirin， 100 mg/kg） and SC high-dose， medium-dose and low-dose groups （40， 20， 10 mg/kg）， with 10 mice in each group. They were given relevant medicine once a day intragastrically for consecutive 5 d. 2 h after last medication， mice in each group was given glacial acetic acid solution intraperitoneal injection； writhing times of mice within 15 minutes were recorded. Other 50 mice were collected； they were grouped and given medicine as above. The response pain threshold （Tr） of mice was determined by intelligent hot plate instrument 15， 30， 60， 120 min after last administration. （2）Anti-inflammatory and mechanism experiment. Other 60 mice were randomly divided into blank control group （normal saline）， model control group （normal saline）， positive control group （aspirin， 100 mg/kg）， SC high-dose， medium-dose and low-dose groups （40， 20， 10 mg/kg）， with 10 mice in each group； they were given relevant medicine intragastrically， once a day， for consecutive 5 d. 60 min after last medication， except for blank control group， other groups were given 1％ carrageenan to induce inflammation. 1， 3， 5 h after inducing inflammation， the degree of paw swelling were determined in each group. Other 30 mice were randomly divided into blank control group （normal saline）， model control group （normal saline）， SC group （40 mg/kg）， with 10 mice in each group； they were given relevant medicine intragastrically once a day， for consecutive 5 d. 60 min after last medication， except for blank control group， other groups were given 1％ carrageenan to induce inflammation in other groups. 5 h later， the levels of SOD， MDA， GSH-Px and T-AOC in paw swelling tissue of mice were determined by biochemical method. The level of PGE2 in paw swelling tissue was determined by ELISA. The mRNA and protein expressions of COX-1 and COX-2 in paw swelling tissue of mice were detected by RT-PCR and Western blot method. RESULTS： In analgesic experiment， compared with blank control group， writhing times of mice were decreased significantly in administration groups （P＜0.05 or P＜0.01）， Tr were increased significantly 30， 60， 120 min after last medication （P＜0.05 or P＜0.01）. In anti-inflammatory and mechanism experiment， compared with blank control group， the degree of paw swelling were increased significantly in model control group 1， 3， 5 h after inducing inflammation （P＜0.01）； the levels of SOD， GSH-Px and T-AOC in paw swelling tissue were decreased significantly （P＜0.01）； the levels of MDA and PGE2 were increased significantly （P＜0.01）， and mRNA and protein expressions of COX-2 were increased significantly （P＜0.01）. Compared with model control group， the degree of paw swelling were decreased significantly in positive control group， SC high-dose and low-dose groups 3 and 5 h after inducing inflammation （P＜0.05 or P＜0.01）. The levels of SOD， GSH-Px and T-AOC in paw swelling tissue were increased significantly in SC group （P＜0.05 or P＜0.01）， while the levels of MDA and PGE2 were decreased significantly （P＜0.01） as well as mRNA and protein expressions of COX-2 were decreased significantly （P＜0.05）. There was no statistical significance in other indexes （P＞0.05）. CONCLUSIONS： SC possesses good anti-inflammatory and analgesic effects， and its mechanism may be related to anti-oxidative stress and inhibition of COX-2/PGE2 signaling pathway.
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Objective: To synthesize sophocarpine-cinnamic acid ester derivatives and evaluate the in vitro antitumor activities of the derivatives. Methods: Taking sophocarpine as the starting material, the target compounds were synthesized by oxidation, esterification, N-alkylation, reduction, condensation, hydrolysis, and salification. Their antitumor activities in vitro were evaluated for HeLa, HepG2 and A-549 by MTT assay. Results: Eleven sophocarpine-cinnamic acid ester derivatives were synthesized and the structures were characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay showed that some derivatives exhibited good antitumor activities. Compound 5g showed good antitumor activity against three human tumor cell lines, which was better than that of the positive control drug, cisplatin. Conclusion: Some derivatives showed promising antitumor activities and compound 5g was worth further studying.
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Matrine is pyrrolizidine alkaloid derived from Chinese materia medica such as Sophora flavescens and Sophora alopecuroides. It has a wide range of pharmacological effects and abundant resources. Sophocarpine is a D ring 13,14-position dehydrogenation analogue of matrine. Due to the high similarity in structure, sophocarpine also exhibits a wide range of pharmacological activities. However, the pharmacological activities of matrine and sophocarpine are not strong, so a great scale of structural modification were carried out. In this paper, the structural modification and derivative activity of matrine and sophoridine were reviewed according to the modification sites classification, and the future development trend was prospected.
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Sophorae Tonkinensis Radix et Rhizoma is known as the important drug for treating sore throat and is widely used in clinic. Because of the coexisting of its efficacy and poison, Sophorae Tonkinensis Radix et Rhizoma often leads to a series of safety problems in the clinical application process. In this study, we attempt to analyze the ultimate cause of the toxicity of Sophorae Tonkinensis Radix et Rhizoma by reviewing nearly 20 years of literature, discuss the substance of its efficacy/toxicity from the point of view of chemical composition, and put forward exploratory thinking on its clinical rational application.
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Sophocarpine is an alkaloid extracted from the dry roots and ground parts of Leguminous Sophora flavescens or S. alopecuroides. Sophocarpine has a wide range of sources, it is abundant in S. flavescens and S. alopecuroides, and it is easy to extract. Sophocarpine has a wide range of pharmacological effects, such as antitumor, anti-inflammatory and analgesia, antivirus, liver protection, cardiovascular protection and so on. In this paper, the pharmacological effects of sophocarpine were reviewed in order to provide references for the treatment of related diseases and new drug research and development.
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Aim To observe the ameliorating effects of sophocarpine on mice with neuropathic pain induced by spared nerve injury(SNI), and to explore the analgesic mechanism.Methods Sixty male ICR mice were randomly divided into six groups: sham-operated, neuropathic-pain model(SNI), SNI+Pregabalin(Pre) 10 mg·kg-1, SNI+SC 40 mg·kg-1, 20 mg·kg-1 and 10 mg·kg-1 group.Neuropathic-pain mouse models were established by SNI of the sciatic nerve.The paw withdrawal mechanical threshold(PWMT), paw withdrawal thermal latency(PWTL), and cold withdrawal times(CWT) were detected to assess the analgesic effects of sophocarpine on mice with neuropathic pain induced by spared nerve injury.The expressions levels of TLR4, p38 MAPK, IL-1β and TNF-α mRNA and protein in spinal cord tissue were detected by reverse transcription-polymerase chain reaction(RT-PCR) and Western blot methods.Results Compared with sham group, the SNI group′s PWMT decreased, PWTL was shorten, CWT increased, and the expression levels of p38 MAPK, TLR4, TNF-α and IL-1β mRNA and protein in spinal cord tissue were up-regulated.Compared with SNI model group, the sophocarpine 40 mg·kg-1 group′s PWMT increased, PWTL was lengthened, CWT decreased, and the expression levels of p38 MAPK, TLR4, TNF-α and IL-1β mRNA and protein in spinal cord tissue were down-regulated.Conclusion Sophocarpine has the analgesic effects on neuropathic pain induced by SNI, and its mechanism may be related to the down-regulation of TLR4, p38 MAPK, IL-1β and TNF-α expression levels.
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OBJECTIVE:To establish a method for the content determination of matrine,sophocarpine,emodin,rhein,chloro-genic acid,sarkosaponin a,aloe-emodin in Kuhuang injection.METHODS:UPLC-MS/MS was adopted. The determination was per-formed on Phenomenex Kenetix C18 column with mobile phase consisted of methanol-0.1% formic acid(gradient elution)at the flow rate of 0.5 mL/min. The column temperature was set at 20 ℃,and injector temperature was set at 10 ℃. The equilibrium time was 4 min and sample size was 5 μL. Ionization mode was electrospray ionization with spray voltage of 5500 V and -4500 V,at-omizing air pressure of 4.14×105 Pa,heater pressure of 4.48×105 Pa,curtain air of 1.72×105 Pa and ion source temperature of 600 ℃. The work mode was multiple reaction monitoring mode. RESULTS:The linear range were 1.25-80.0 ng/mL for matrine (r=0.9993),1.10-70.0 ng/mL for sophocarpine(r=0.9995),0.16-10.5 ng/mL for emodin(r=0.9993),2.61-168 ng/mL for rhe-in (r=0.9993),1.50-96.0 ng/mL for chlorogenic acid (r=0.9993),1.48-94.5 ng/mL for sarkosaponin a (r=0.9996) and 6.11-391 ng/mL for aloe-emodin(r=0.9991). The limits of quantification were 0.061,0.109,0.041,1.313,0.500,0.492,3.055 ng/mL,limits of detection were 0.025,0.054,0.016,0.656,0.150,0.148,1.528 ng/mL. RSDs of precision,stability and reproducibility tests were all no more than 3%. The recoveries of them were 95.45%-99.45%(RSD=1.43%,n=6),97.50%-101.00%(RSD=1.50%,n=6),95.67%-101.73%(RSD=2.85%,n=6),97.17%-100.57%(RSD=1.16%,n=6),95.19%-98.90%(RSD=1.71%, n=6),95.38%-103.85%(RSD=3.39%,n=6),95.50%-101.17%(RSD=1.20%,n=6),respectively. CONCLUSIONS:The method is simple,effective,accurate,reliable and suitable for simultaneous determination for 7 components in Kuhuang injection.
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AIM To establish a gas chromatography-flame ionization detector (GC-FID) method for the simultaneous content determination of four constituents in Kaihoujian Spray (a spray for management of oral and laryngopharyngeal inflammatory condition,containing Sophorae tonkinensis Radix et Rhizoma,Cicadae Periostracum,menthol,etc.).METHODS The analysis of mixure of Kaihoujian Spray and internal standard (dibutyl phthalate) solution was conducted on an HP-INNOWax column (30 m ×0.25 mm ×0.25 μm),both of the injector temperature and detector temperature were set at 260 ℃,the split ratio was 5 ∶ 1,and the flowing rate was 1.5 mL/min.RESULTS Menthol,matrine,sophocarpine and sophoridine showed good linear relationships within the ranges of 0.228 7-2.287 0 mg/mL (r =0.999 7),0.011 1-0.111 0 mg/mL (r =0.999 6),0.016 8-0.168 0 mg/mL (r =0.999 8) and 0.003 4-0.034 0 mg/mL (r =0.999 4),whose average recoveries (n =9) were 98.4％ (RSD=1.2％),95.9％ (RSD=1.8％),96.2％ (RSD=2.1％) and 97.1％ (RSD=1.7％),respectively.CONCLUSION This accurate,sensitive and simple method can be used for the quality control of Kaihoujian Spray.
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Objective To investigate the compatibility and room light' s influence on Kuhuang injection diluted by 5%glucose,10% glucose, and fructose for injection within 48 hours at room temperature. Methods Kuhuang injections( high or low dosage) were diluted by 3 solutions at room temperature and were divided into light-exposed group and light-screening group. Stability were then studied by changes of appearance, pH value, particulates, contents of matrine and sophocarpine in the solutions. Results The Kuhuang injection solution remained clear within 48 hours, showing no obvious turbidity, sedimentation or change of appearance ( deep yellow clear solution ) . The pH of the low concentration group with 10% glucose injection exposed to room light in creased significantly at 6 h,which was less stable than the light-screening group.The particulate content was acceptable according to regulation. The Kuhuang injection compatibility solution with fructose injection changed into weak acidic pH, and the particulate content did not meet regulation criteria in the high concentration group. The contents of matrine did not change, while the contents of sophocarpine decreased in each group.Sophocarpine seemed more stable in the light-screening group than in the light-exposed group. Conclusion The fructose injection was not suitable as the solvent for Kuhuang injection.The solutions are more stable if protected from light, and should be used as early as possible to reduce the degradation of some effective components.
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Objective To investigate the compatibility and room light' s influence on Kuhuang injection diluted by 5%glucose,10% glucose, and fructose for injection within 48 hours at room temperature. Methods Kuhuang injections( high or low dosage) were diluted by 3 solutions at room temperature and were divided into light-exposed group and light-screening group. Stability were then studied by changes of appearance, pH value, particulates, contents of matrine and sophocarpine in the solutions. Results The Kuhuang injection solution remained clear within 48 hours, showing no obvious turbidity, sedimentation or change of appearance ( deep yellow clear solution ) . The pH of the low concentration group with 10% glucose injection exposed to room light in creased significantly at 6 h,which was less stable than the light-screening group.The particulate content was acceptable according to regulation. The Kuhuang injection compatibility solution with fructose injection changed into weak acidic pH, and the particulate content did not meet regulation criteria in the high concentration group. The contents of matrine did not change, while the contents of sophocarpine decreased in each group.Sophocarpine seemed more stable in the light-screening group than in the light-exposed group. Conclusion The fructose injection was not suitable as the solvent for Kuhuang injection.The solutions are more stable if protected from light, and should be used as early as possible to reduce the degradation of some effective components.
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12-N-m-Cyanobenzenesulfonyl matrinic butyl methyl ether is a potent anti-coxsackievirus B3(CVB3) agent bearing a novel structure skeleton. Taking this compound as a lead, totally 15 novel target compounds have been synthesized and evaluated for the anti-CVB3 activities using CPE method. Structureactivity relationship (SAR) demonstrated that the shorten-length of 11-side chain was not helpful for keeping the good anti-virus activity. Among the newly synthesized compounds, compound c1 displayed a good anti-CVB3 activity with the IC50 of 7.1 μmol·L-1 and SI of 35.5, similar to that of the lead. The SAR results provided useful information for further optimization of these compounds in the molecular structure.
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Objective: To investigate the possible protective effects of sophocarpine on mucosal injury and epithelial barrier disruption on dextran sulfate sodium (DSS)-induced acute colitis. Methods: Male BALB/c mice were randomly divided into three groups. The mice in normal group were given normal water, and those in model and sophocarpine-treated groups were given 2.5% DSS for 6 d to induce acute colitis. Sophocarpine (30 mg/kg) was ip administered once daily during the study period. Severity of colitis was evaluated by disease activity index (DAI), histological injury and inflammatory cytokine production including tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and monocyte chemoattractant protein-1 (MCP-1). The colonic barrier disruption was assessed by testing the expression of junctional adhesion molecule-1 (JAM-1), E-cadherin (E-CAD), and desmocollin-2 (DSC-2) in colon mucosa. Expression of HNF4α in colon mucosa was detected by immunohistochemistry staining and real-time RT-PCR, respectively. Results: Compared with normal group, DAI, colonic shortening, and histopathological injury in model group were elevated (P < 0.05), but reduced in sophocarpine-treated group (P < 0.05). Compared with model group, the mRNA expression of inflammatory cytokines (TNF-α, IL-1β, MCP-1) were obviously lower in sophocarpine-treated group (P < 0.05), while the cellular junction proteins (E-CAD, JAM-1, and DSC-2) were higher (P < 0.05). The expression of HNF4α at mRNA and protein levels was decreased significantly in model group, but increased apparently in sophocarpine-treated group. Conclusion: Sophocarpine can enhance the expression of HNF4α, promote the expression of colonic intrecellular junctions, thus, maintain the integrity of the colonic barrier and inhibit the colitis process. We suggest that sophocarpine could enhance the production of cellular junction proteins to protect the intestinal barrier fuction, at least partly, in HNF4α-dependent pathway.
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Objective To investigate the absorption behaviors of three kinds of sophora alkaloids(matrine, oxymatrine and sophocarpine)in Caco-2 cells and their metabolic rates in rat liver microsomes. Methods Caco-2 cell absorption model was used to analyze the absorption behaviors of three sophora alkaloids and rat liver microsomal model in vitro was used to investigate the metabolic rates of three sophora alkaloids. The contents of three kinds of sophora alkaloids were determined by HPLC-MS and the permeation rates and metabolic rates were calculated. The analytical conditions were as follows: chromatographic column: Agilent Zorbax SB-C18(3.0 mm×100 mm, 3.5 μm); mobile phase: acetonitrile/water(60:40, V/V)with isocratic elution; injection volume: 5 μL; flow rate: 0.8 mL/min; temperature of column: 30℃; and running time: 9 min. The selective ion monitoring(SIM)in positive ion mode was used in mass spectrometry, with drying gas temperature: 350℃; capillary voltage: 4 000 V; drying gas flow rate: 9.0 L/min; and fragmentor voltage: 90 eV. Results In the Caco-2 cell absorption model, matrine, oxymatrine and sophocarpine were separated with good linearity(r> 0.999 5)between 0.050 5-10.01 μmol/L, with the permeation rates being: matrine 1.251, oxymatrine 0.937 5, and sophocarpine 1.424. In rat liver microsomal model, matrine, oxymatrine and sophocarpine were separated with good linearity(r> 0.999 8)between 0.050 1-1.001 μmol/L, with the half-life period being: matrine 4.331 h,oxymatrine 1.084 h,and sophocarpine 2.478 h. The intra-day and inter-day precisions were 80%, and the extraction recovery rate was >88%. Conclusion The three kinds of sophora alkaloids can easily pass the Caco-2 cell absorption model, with active transport being the main way, and it is difficult for them to be metabolized in rat liver microsomes.
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Objective To determine the content of sophocarpine, matrine, oxysophocarpine, sophoridine, oxymatrine in Sophora Flavescentis Radix from different areas. Methods Agilent ZORBAX NH2 column (4.6 mm×150 mm, 5 μm) was used with mobile phase of acetonitrile-ethanol-3% phosphate (84∶10∶6), at a flow rate of 1 mL/min. The wavelength of detection was 210 nm. Results The linear range of sophocarpine, matrine, oxysophocarpine, sophoridine and oxymatrine were 0.022 88-0.114 4 μg (r=0.999 7), 0.083 2-0.416 0 μg (r=0.999 7), 0.376 2-1.836 0 μg (r=0.999 8), 0.104 4-0.522 μg (r=0.999 2), 0.491 2-2.456 μg (r=0.999 9), respectively. The average recovery were 101.63% (RSD=2.08%), 98.29%(RSD=1.87%), 101.89% (RSD=1.97%), 99.87% (RSD=2.06%), 102.66% (RSD=1.34%), respectively. Conclusion The method is simple, rapid and accurate, and suitable for the quality control of Sophorae Flavescentis Radix.
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Objective To investigate the neuroprotective effect of sophocarpine against transient focal cerebral ischemia via down-regulation of the acid-sensing ion channel 1(ASICl) in rats.Methods Twenty-five SD rats were randomly allocated into sham operation,cerebral ischemia/reperfusion,and 5,10,and 20 mg/kg sophocarpine pretreatment groups (n=5 in each group).A rat focal ischemia model was induced by the intraluminal suture method.Five,10 and 20 mg/kg sophocarpine were injected intraperitoneally for pretreatrnent.2,3,5-triphenyltetrazolium chloride staining was used to detect cerebral infarct volume.TUNEL staining was used to detect apoptosis.Immunohistochemistry and Western blot were used to detect the expression of ASIC1 and ASIC2.Results The infarct volume after ischemia-reperfusion was(181.21±9.21)mm3,while the 5,10,and 20 mg/kg sophocarpine pretreatment groups were(150.12±6.19),(52.31±4.20),and(32.18±3.82)mm3,respectively;the neurological function scores in the cerebral ischemia/reperfusion group was(3.62±0.36),while the 5,10,and 20 mg/kg sophocarpine pretreatment grows were(3.15±0.36),(1.92±0.18),and(1.85±0.21),respectively;The surviving neurons only accounted for(31.2±2.8)% of the total cell number in the cerebral ischemia-reperfusion group,while they accounted for(51.2±3.7)%,(76.5±2.1)%,and(77.1±4.1)% in the 5,10,and 20 mg/kg sophocarpine pretreatnmat groups.Compared with the cerebral ischemia/reperfusion group,the cerebral infarct volume was decreased significantly in the sophocarpine pretreatrnent groups(all P<0.01),the neurological function scores were decreased significantly(all P<0.01),and the number of apoptotic cells was decreased significantly (all P<0.01).Immunohistochemistry showed that the number of ASIC-1 positive cells in the sham operation,cerebral ischemia-reperfusion,and 5,10,and 20 mg/kg sophocarpine pretreatment groups were(162.5±8.3),(165.1±5.3),(138.3±7.2),(82.1±6.3),and(69.2±5.5)/mm respectively;Western blot showed that the ASIC1 protein expression was decreased sigaificantly in the 10 and 20 mg/ky sophocarpine pretreatment groups (P<0.01),while there WaS no significant difference in the ASIC2 protein expression.Condusions Sophocarpine may play a neuroprotective role for cerebral ischemia-reperfusion injury in rats via down-regulating the expression of ASIC1 protein.
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Objective To observe the in vitro anti-Coxsackievirus B3m (CVB3m) effect of sophocarpine(SC) extracted from Sophora flavescens, a traditional Chinese herb. Methods HeLa cells were cultured and the micro-dose cytopathic effect (CPE) assays were applied to detect the toxicity of SC. CPE-inhibitory assays were used to observe the in vitro anti-CVB3m effect of SC. MTT and crystal assays were introduced to examine the anti-CVB3m effect of SC. HeLa cells were infected with CVB3m and added with SC in different concentrations 15 h later.The viability and number of survival of HeLa cells were determined by MTT and crystal violet assays, respectively. Results No toxicity was found on HeLa cells by SC with concentrations 100 ?g/mL, SC could accelerate and aggravate the CPE. SC could protect the CVB3m-infected HeLa cells with concentrations from 1.56 to 25 ?g/mL, and the viability and cell number measured by MTT and crystal violet assay in the SC-handled cells were higher and bigger than those in the virus infected ones. However, the inhibitory effect of virus was exacerbated with higher concentrations (50 and 100 ?g/mL), and the cell number and viability of the SC-handled cells were smaller and lower than those of the infected ones. Conclusion SC with a proper concentration has the in vitro anti-CVB3m effect and may protect HeLa cells from CVB3m infection.
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AIM: To establish an HPLC method for determining sophocarpine,sophoridine and oxymatrine in Sophora flavescens Ait,so as to investigate their contents in different years and different parts. METHODS: An Elite Hypersil NH2 column(250 mm ? 4. 6 mm,5 ?m) was used with the mobile phase being acetonitrile-absolute alcohol-3% phosphoric acid solution(82 ∶ 10 ∶ 8),flow rate being 1 mL/min,determinating wavelength being 220 nm,the column temperature being 26 ℃,The injection volume was 5 ?L. RESULTS: The calibration curves of sophocarpine,sophoridine and oxymatrine were in good linearity over the ranges of 0. 004 99 - 0. 149 7 ?g(r = 0. 999 9),0. 025 08 - 0. 752 25 ?g(r = 0. 999 9),0. 075 38 - 2. 261 25 ?g(r = 0. 999 9); and the average recovery of sophocarpine,sophoridine and oxymatrine was 99. 91% ,99. 26% ,100. 27% with RSD of 1. 11% , 0. 82% ,2. 18% respectively. CONCLUSION: The HPLC method shows a good separation,reproducibility and accuracy,there are obvious differences in the contents of three alkaloids in different years and different parts of Sophora flavescens Ait. The results provide important data for quality evaluation and utilization of Sophora flavescens materials.
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AIM: To study the effect of the four alkaloids of Sophora Alopecuroides On cycloxygenase(COX) activities in vitro. METHODS: The effect of matrine, oxymatrine sophocarpine and sophoridine on COX2 and COX1 activity were evaluated by the content of Prostaglandin E_2(PGE_2) and 6-Keto-PGF_~1a , respectively. The PGE_2 came from exogenous AA in cultured mouse peritoneal macrophage supernatants induced by lipopolysaccharide(LPS) 1 ug?mL~-1 was measured with radioimmunoassay(RIA) method using ~ 3H-labelled PGE_2. The 6-Keto-PGF_~1a from exogenous AA in cultured mouse peritoneal macrophage supernatants induced by calcium ionophore A23187 1 ?mol?L~-1 was measured with RIA method using~125 I-labelled 6-Keto-PGF_~1a . RESULTS: The COX2 activities were markedly inhibited in a dose dependent manner by oxymatrine, sophocarpine and sophoridine, Respectively. Excluding the sophoridine, all the other three alkaloids of Sophora Alopecuroids obviously suppressed the activities of COX1, respectively. CONCLUSION: The in vitro results show that oxymatrine, sophocarpine and sophoridine may have the significant specific inhibitory action for COX2, in contrase, matrine may be COX1 selective inhibitor.
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Sophocarpine ( SC ) , an alkaloid extracted from sophora alope -curoides L. , was found to have a rapid and significant hypotensive action both in anesthetized dogs and in conscious renal hypertensive rats. On superior cervical ganglia and nictitating membrane preparation ,SC 15mg, administered via lingual artery, briefly relaxes the rigid contraction of nictitating membrane caused by continuous stimulation of sympathetic preganglionic fibers. SC 50, 100, 200?g/kg reduced the vascular resistance index 13.1 ?1.6%, 20.5?4.6%, 27.8?4.1% respectively when perfused into the femoral artery .Measurement of the changes of hemodynamics with constant voltage transthoracic admittance plethysmograph in 5 intact anesthetized dogs showed that SC iv 25mg/ kg enhenced the index of myocardial contractility 18% and heart beat index 40%, shortened Q -Y interval 37%.These results suggest that hypotensive action of SC should be realized by both relaxing the peripheral vascular smooth muscules and blocking the transmission of impulse through the sympathetic ganglia.