Phytochemical and pharmacological evaluation of the flowers of Sarcostemma brevistigma Wight

KG Lalitha,MG Sethuraman 경희대학교 융합한의과학연구소 2009 Oriental Pharmacy and Experimental Medicine Vol.9 No.3

Shade-dried flowers of Sarcostemma brevistigma Wight Syn (SBF) belonging to Asclepiadaceae yielded a rare flavonol glycoside viz., Quercetin 5a prenyl, 3-O-glucosyl, 7-O-(4c-p-coumaroyl) neohesperidoside which were characterized based on chemical and spectral (including 2D NMR) studies. The ethyl acetate fraction of alcoholic concentrate (test sample) of flowers of this plant (SBF) was evaluated for its hepatoprotective and inhibition of lipid peroxidation activities to investigate the scientific basis of the traditional uses. The oral administration in varying doses viz., 125 and 250 mg/kg of aqueous suspension of SBF to rats for 7 days produced significant (P < 0.01) hepatoprotective effect comparable to that of standard drug silymarin. The SBF afforded good hepatoprotection against CCl4 induced elevation levels of serum marker enzymes, serum bilirubin and liver weight. The free radical scavenging effects of SBF and flavonol glycoside (SA) were assigned by Fe2+/ascorbate induction method (in vitro), which revealed the inhibition of lipid peroxidation. The SBF and SA showed prominent anti-lipid peroxidation activity (IC50 about ~ 180 mg/ml and 11.0 mg/ml respectively), which was comparable to standard drug curcumin (IC50 about ~ 8.25 mg/ml). Thus the hepatoprotective activity of SB could be correlated to the free radical scavenging property of the flavonol glycoside. Shade-dried flowers of Sarcostemma brevistigma Wight Syn (SBF) belonging to Asclepiadaceae yielded a rare flavonol glycoside viz., Quercetin 5a prenyl, 3-O-glucosyl, 7-O-(4c-p-coumaroyl) neohesperidoside which were characterized based on chemical and spectral (including 2D NMR) studies. The ethyl acetate fraction of alcoholic concentrate (test sample) of flowers of this plant (SBF) was evaluated for its hepatoprotective and inhibition of lipid peroxidation activities to investigate the scientific basis of the traditional uses. The oral administration in varying doses viz., 125 and 250 mg/kg of aqueous suspension of SBF to rats for 7 days produced significant (P < 0.01) hepatoprotective effect comparable to that of standard drug silymarin. The SBF afforded good hepatoprotection against CCl4 induced elevation levels of serum marker enzymes, serum bilirubin and liver weight. The free radical scavenging effects of SBF and flavonol glycoside (SA) were assigned by Fe2+/ascorbate induction method (in vitro), which revealed the inhibition of lipid peroxidation. The SBF and SA showed prominent anti-lipid peroxidation activity (IC50 about ~ 180 mg/ml and 11.0 mg/ml respectively), which was comparable to standard drug curcumin (IC50 about ~ 8.25 mg/ml). Thus the hepatoprotective activity of SB could be correlated to the free radical scavenging property of the flavonol glycoside.

Phytochemical and pharmacological evaluation of the flowers of Sarcostemma brevistigma Wight

Lalitha, KG,Sethuraman, MG Kyung Hee Oriental Medicine Research Center 2009 Oriental pharmacy and experimental medicine Vol.9 No.3

Shade-dried flowers of Sarcostemma brevistigma Wight Syn (SBF) belonging to Asclepiadaceae yielded a rare flavonol glycoside viz., Quercetin 5a prenyl, 3-O-glucosyl, 7-O-(4c-p-coumaroyl) neohesperidoside which were characterized based on chemical and spectral (including 2D NMR) studies. The ethyl acetate fraction of alcoholic concentrate (test sample) of flowers of this plant (SBF) was evaluated for its hepatoprotective and inhibition of lipid peroxidation activities to investigate the scientific basis of the traditional uses. The oral administration in varying doses viz., 125 and 250 mg/kg of aqueous suspension of SBF to rats for 7 days produced significant (P < 0.01) hepatoprotective effect comparable to that of standard drug silymarin. The SBF afforded good hepatoprotection against $CCl_4$ induced elevation levels of serum marker enzymes, serum bilirubin and liver weight. The free radical scavenging effects of SBF and flavonol glycoside (SA) were assigned by $Fe^{2+}$/ascorbate induction method (in vitro), which revealed the inhibition of lipid peroxidation. The SBF and SA showed prominent anti-lipid peroxidation activity ($IC_{50}$ about $\sim$180 mg/ml and 11.0 mg/ml respectively), which was comparable to standard drug curcumin ($IC_{50}$ about $\sim$8.25 mg/ml). Thus the hepatoprotective activity of SB could be correlated to the free radical scavenging property of the flavonol glycoside.

Hepatoprotective activity of Nyctanthes arbor-tristis (l.)

Wagh AE,Yeotkar US,Nimbhorker MG,Deshmukh TA,Patil VR 경희대학교 융합한의과학연구소 2010 Oriental Pharmacy and Experimental Medicine Vol.10 No.2

The flowers of Nyctanthes arbor-tristis Linn. of Oleaceae widely used in Ayurvedic system of medicine for the treatment of diuresis, liver disorder, spleen enlargement sciatica, bitter,stomachic, carminative and tonic to hair. The aim of the present study was to evaluate the alcoholic and aqueous extracts of the flowers of Nyctanthes arbor-tristis for hepatoprotective effect against carbontetrachloride induced liver damage in rats. Administration of alcoholic and aqueous extracts of the leaves of Nyctanthes arbor-tristis protect the liver from toxic effects of carbontetrachloride by reducing the elevated levels of Serum glutamate pyruvate transaminase,Serum glutamate oxaloacetate transaminase, Alkaline phosphatase and serum bilirubin. Results revealed that both the alcoholic and aqueous extracts showed significant hepatoprotective activity by reducing the elevated levels of biochemical parameters at a dose of 200 mg/kg body weight. The results were supported by histopathological studies of liver samples which showed regeneration of hepatocytes by the extracts.

한국인 중증근무력증의 역학 및 임상적 특성 연구

이광우,김지수,이성현,MG연구회 대한신경과학회 1997 대한신경과학회지 Vol.15 No.4

자궁근염이 고양이 자궁의 감각수용기에 미치는 영향

나중렬,홍승길,이낙우,한희철,이민구 대한산부인과학회 1999 Obstetrics & Gynecology Science Vol.42 No.6

목적: 자궁내 염증을 유발하여 염증 후 일어나는 자궁을 지배하는 감각신경의 변화를 관찰하고, 염증시 유리되어 나오는 물질로 알려진 substance P가 자궁의 구심성 신경에 영향을 미치는 가를 알아보기 위해 실험하였다. 연구방법: 성숙한 암코양이 14마리를 사용하여 자궁동맥에 미세한 polyethylene tube를 삽입하여 자궁근내로 통증유발물질 및 기타 약품의 주입이 가능하게 하였으며 수술현미경하에서 하복신경을 중추 쪽으로 추적하여 확인한 후 기록용 백금전극에 올려놓았다. 기록전극 위에 놓인 하복신경의 활동전위는 증폭 및 여과장치를 거쳐 원하는 임펄스를 취한 후 이를 컴퓨터에 저장하고 분석하였다. 반응이 확인된 신경단위에 5ug의 bradykinin을 투여하고 반응을 기록한 후 자궁강내에 염증유발물질인 10%의 mustard oil을 papain[3mg/ml]처리한 후 주입하여 1시간 동안 방치하여 염증을 유도한 후 염증 후의 반응을 기록하였다. 다른 동물개체에서는 mustard oil 대신 염증시 유리되는 substance P를 5ug 자궁동맥내로 주입하여 주입전후의 bradykinin의 효과를 비교하여 염증시 유리되는 substance P의 효과를 관찰하였다. 결과: bradykinin에 대한 자궁 감각신경체의 반응성은 염증유발 2시간 및 4시간 후에 염증유발전보다 증가하였다. substance P 처리후에는 11개의 가는 유수신경[Aδ fiber] 중 8개가 반응성이 감소한 반면 10개 무수신경[C fiber] 모두에서 반응성이 증가하였다. 결론: 염증이 유발된 자궁에서 염증이 유발되기 전의 자궁에서보다 통증 유발물질인 bradykinin에 더욱 민감하게 반응하는 사실을 알 수 있었으며, 염증시 유리되는 substance P는 염증조직내의 구심성감각신경 중 특히 통증을 전달하는 C섬유군의 활성화에 중요한 역할을 하는 것을 알 수 있었다. 이와 같은 결과는 앞으로 내장감각기관에서 염증에 의한 주요증상의 하나인 통증의 기전을 이해하고 치료 및 약제 개발에 중요한 역할을 할 수 있으리라 생각된다. Objective : To examine whether the inflammation can alter the sensitivity of primary afferents innervating uterus and its adjacent tissues, and to elucidate the role of substance P which are known to be released to the inflamed tissues. Methods : Total fourteen female cats were used, four cats were used for inflammation tests. Uterine inflammation was induced by 10% of mustard oil after papain [3mg/ml] treatment. These chemicals were injected into the uterine cavity. Other 10 cats were used for substance P [5 g] tests which was injected into the uterine circulation. The responses of hypogastric nerve to bradykinin injected into the uterine circulation were recorded before and after either treatments [inflammation or substance P] using electrophysiological method. Results : The neuronal responses to bradykinin were increased at 2 hours and 4 hours after uterine inflammation. As for substance P treatment, the responses of 8 of 11 thin myelinated [A ] nerve fibers were decreased after substance P treatment, those of all 10 of unmyelinated [C] nerve fibers were increased. Conclusions : These results indicated that the afferents from the uterus responded to bradykinin more sensitively after inflammation and substance P which are released after inflammation may play a important role in uterine hyperalgesia.

Interaction between udenafil and tamsulosin in rats: non-competitive inhibition of tamsulosin metabolism by udenafil via hepatic CYP3A1/2 : PK interaction between udenafil and tamsulosin

Kang, HE,Bae, SK,Yoo, M,Lee, DC,Kim, YG,Lee, MG Wiley (Blackwell Publishing) 2009 British journal of pharmacology Vol.156 No.6

<P>BACKGROUND AND PURPOSE: Orthostatic hypotension has been observed when PDE 5 (cGMP-specific phosphodiesterase type 5) inhibitors are co-administered with alpha-adrenoceptor antagonists. Here we assessed the pharmacokinetic and haemodynamic interactions between udenafil and tamsulosin in rats, as both drugs are metabolized via rat hepatic cytochrome P450 3A1/2. EXPERIMENTAL APPROACH: Interactions between the two drugs were evaluated in rats after simultaneous 1 or 15 min i.v. infusion or after p.o. administration of udenafil (30 mg x kg(-1)) and/or tamsulosin (1 mg x kg(-1)). In vitro metabolism of tamsulosin with udenafil was measured to obtain the inhibition constant (K(i)) and [I]/K(i) ratio of udenafil. KEY RESULTS: The total area under the plasma concentration-time curve from time zero to time infinity (AUC)s (or AUC(0-4 h)) of tamsulosin were significantly greater after 15 min of i.v. infusion or after oral administration with udenafil, compared with tamsulosin alone. The hepatic first-pass metabolism of tamsulosin was inhibited by udenafil, and the inhibition in vitro was in a non-competitive mode. The arterial systolic blood pressure was significantly lower at 5, 10 and 60 min after oral co-administration of the drugs. CONCLUSIONS AND IMPLICATIONS: The significantly greater AUC of tamsulosin after i.v. and p.o. administration of both drugs may be attributable to non-competitive inhibition of cytochrome P450 3A1/2-mediated hepatic tamsulosin metabolism by udenafil. The inhibition was also observed in human liver S9 fractions, suggesting that a reassessment of the oral dosage of tamsulosin is necessary when udenafil and tamsulosin are co-administered to patients with benign prostatic hyperplasia.</P>

Pharmacokinetics of oltipraz in diabetic rats with liver cirrhosis : Pharmacokinetics of oltipraz in LCD rats

Ahn, CY,Bae, SK,Bae, SH,Kim, T,Jung, YS,Kim, YC,Lee, MG,Shin, WG Wiley (Blackwell Publishing) 2009 British journal of pharmacology Vol.156 No.6

<P>BACKGROUND AND PURPOSE: The incidence of diabetes mellitus is increased in patients with liver cirrhosis. Oltipraz is currently in trials to treat patients with liver fibrosis and cirrhosis induced by chronic hepatitis types B and C and is primarily metabolized via hepatic cytochrome P450 isozymes CYP1A1/2, 2B1/2, 2C11, 2D1 and 3A1/2 in rats. We have studied the influence of diabetes mellitus on pharmacokinetics of oltipraz and on expression of hepatic, CYP1A, 2B1/2, 2C11, 2D and 3A in rats with experimental liver cirrhosis. EXPERIMENTAL APPROACH: Oltipraz was given intravenously (10 mg x kg(-1)) or orally (30 mg x kg(-1)) to rats with liver cirrhosis induced by N-dimethylnitrosamine (LC rats) or with diabetes, induced by streptozotocin (DM rats) or to rats with both liver cirrhosis and diabetes (LCD rats) and to control rats, and pharmacokinetic variables measured. Protein expression of hepatic CYP1A, 2B1/2, 2C11, 2D and 3A was measured using Western blot analysis. KEY RESULTS: After i.v. or p.o. administration of oltipraz to LC and DM rats, the AUC was significantly greater and smaller, respectively, than that in control rats. In LCD rats, the AUC was that of LC and DM rats (partially restored towards control rats). Compared with control rats, the protein expression of hepatic CYP1A increased, that of CYP2C11 and 3A decreased, but that of CYP2B1/2 and 2D was not altered in LCD rats. CONCLUSIONS AND IMPLICATIONS: In rats with diabetes and liver cirrhosis, the AUC of oltipraz was partially restored towards that of control rats.</P>

SIGN-R1, a C-type lectin, enhances apoptotic cell clearance through the complement deposition pathway by interacting with C1q in the spleen

MG Prabagar,Y Do,S Ryu,J-Y Park,H-J Choi,W-S Choi,TJ Yun,J Moon,I-S Choi,K Ko,K Ko,C Young Shin,C Cheong,Y-S Kang 한국당과학회 2013 한국당과학회 학술대회 Vol.2013 No.1

Complements, such as C1q and C3, and macrophages in the splenic marginal zone (MZMs) play pivotal roles in the efficient uptake and processing of circulating apoptotic cells. SIGN-R1, a C-type lectin that is highly expressed in a subpopulation of MZMs, regulates the complement fixation pathway by interacting with C1q, to fight blood-borne Streptococcus pneumoniae. Therefore, we examined whether the SIGN-R1-mediated classical complement pathway plays a role in apoptotic cell clearance and immune tolerance. SIGN-R1 first-bound apoptotic cells and this binding was significantly enhanced in the presence of C1q. SIGN-R1-C1q complex then immediately mediated C3 deposition on circulating apoptotic cells in the MZ, leading to the efficient clearance of them. SIGN-R1-mediated C3 deposition was completely abolished in the spleen of SIGN-R1 knockout (KO) mice. Given that SIGN-R1 is not expressed in the liver, we were struck by the finding that C3-deposited apoptotic cells were still found in the liver of wild-type mice, and dramatically reduced in the SIGN-R1 KO liver. In particular, SIGN-R1 deficiency caused delayed clearance of apoptotic cells and aberrant secretion of cytokines, such as TNF-α, IL-6, and TGF-β in the spleen as well as in the liver. In addition, anti-double- and single-stranded DNA antibody level was significantly increased in SIGN-R1-depleted mice compared with control mice. These findings suggest a novel mechanism of apoptotic cell clearance which is initiated by SIGN-R1 in the MZ and identify an integrated role of SIGN-R1 in the systemic clearance of apoptotic cells, linking the recognition of apoptotic cells, the opsonization of complements, and the induction of immune tolerance.

An Update on the Role of Tiotropium in the Management of COPD

( David Mg Halpin ) 대한결핵 및 호흡기학회 2011 대한결핵 및 호흡기학회 추계학술대회 초록집 Vol.112 No.-

저온에서 혈관수축력의 변화(흰쥐 흉부대동맥 수축에 미치는 저온의 영향)

이만기 ( Lee Mg ) 국군의무사령부 1989 대한군진의학학술지 Vol.20 No.1