• Bulletin of the Korean Chemical Society
• /
• 제24권9호
• /
• pp.1385-1388
• /
• 2003

• 약학회지
• /
• 제47권5호
• /
• pp.331-338
• /
• 2003

A butyrolactone ester of cefazolin (CFZ-BTL) was synthesized by the esterification of cefazolin (CFZ) with $\alpha$-bromo-${\gamma}$-butyrolactone. The synthesis was confirmed by the spectroscopic analysis. The CFZ-BTL was more lipophilic than the CFZ when assessed by n-octanol/water partition coefficients at various pH. The CFZ-BTL itself did not show any antimicrobial activity in vitro, but after oral administration of CFZ-BTL to rabbits, exerted significant anti-microbial activity in serum samples when measured by the inhibion zone method in nutrient agar plates, due to conversion of CFZ-BTL to an active metabolite, probably CFZ, in the body. The CFZ-BTL was also converted into CFZ as confirmed by in vitro incubation study, with tissue homogenates (liver, blood and intestine) of rabbits. The liver showed the fastest conversion rate, probably via the hydrolysis mechanism. In vivo metabolism of CFZ-BTL to CFZ was also confirmed in vivo serum samples by HPLC. The oral bioavailability of CFZ-BTL in rabbits was 1.6-fold increased when compared to CFZ, resulting from followed by enhanced lipophilicity increased passive absorption in the intestine.

• Clinical and Experimental Reproductive Medicine
• /
• 제24권1호
• /
• pp.1-11
• /
• 1997

It is well known that the zona pellucidae of mouse oocytes become "hardened" when they are allowed to mature in vitro in the absence of serum components. To see if oocytes already undergone meiotic resumption in vivo exhibit similar zona hardening, hardening of ZP of cumulus-enclosed oocytes(CEOs) was examined after culture in vitro since their release from follicles various hours after hCG injection. When CEOs matured in vivo for 3h or longer were subjected to culture in vitro for 14h with BSA alone, zona hardening was significantly reduced compared to those cultured in vitro from the begining of maturation. However, when CEOs matured in vivo for 5h were freed from cumulus cells and then cultured in vitro with BSA alone, little reduction of zona hardening was observed. Preincubation of CEOs for 5h with fetuin, one of the well known inhibitor of in vitro zone hardening, did not prevent zona hardening during its subsequent culture of CEOs for 14h without fetuin. However, when CEOs precultured with both fetuin and PMSG for 5h and then further cultured with BSA alone for 14h, zona hardening was dramatically reduced. Under these conditions, the expansion of cumulus cell was observed. In addition, CEOs cultured with both BSA and dbcAMP to prevent their meiotic resumption showed a significant increase of zona hardening. Whether the observed zona hardening was correlated with the conversion of ZP2 to $ZP2_{f}$ was examined. Zona pellucida, isolated from CEOs matured for 5h in vivo and then further cultured with BSA alone was subjected to SDS-PAGE. Most of ZP2 molecules from these CEOs did not undergo conversion from ZP2 to $ZP2_{f}$. From these results, it is concluded that CEOs undergone meiotic resumption in vivo do not exhibit zona hardening when they were subsequently cultured in vitro without serum components. It appears that cumulus cells play an important role in this phenomenon.

• BMB Reports
• /
• 제28권4호
• /
• pp.301-305
• /
• 1995

Considering the stimulatory effects of ginsenosides from Panax ginseng C. A. Meyer on the release of nitric oxide from bovine aortic endothelial cells in vitro and vasodilatation of rabbit pulmonary artery in vivo, the present study is designed to investigate the mechanism of nitric oxide release by ginsenosides in calf pulmonary artery endothelial cells, Nitric oxide release was determined in endothelial cells treated with ginsenosides and compared with those of the receptor-dependent agonists, bradykinin and ADP and the receptor-independent calcium ionophore $A_{23187}$. The results showed that total saponin and ginsenoside $Rg_1$, not $Rb_1$, stimulated nitric oxide release measured as conversion to L-citrulline. The nitric oxide releasing properties of total saponin and ginsenoside $Rg_1$ were different; total saponin stimulated only conversion to L-citrulline, like $A_{23187}$, while ginsenoside $Rg_1$ stimulated both L-arginine transport and conversion to L-citrulline, as bradykinin or ADP did.

• BMB Reports
• /
• 제29권4호
• /
• pp.327-334
• /
• 1996

In this study, the origin of the monovinyl chlorophyll a carboxylic biosynthetic route was investigated in barley (Hordeum vulgare L.) and com (Zea mays L.). Protoporphyrin IX accumulated in vivo or in vitro was found to be all of the divinyl form. Furthermore, the conversion of divinyl protoporphyrin IX to monovinyl protoporphyrin IX in vitro was not observed. In contrast, the biosynthesis and accumulation of monovinyl Mg-protoporphyrin IX and its methyl ester occurred in etiolated leaves and divinyl Mg-protoporphyrin IX was convertible to monovinyl Mg-protoporphyrin IX in vitro. These results suggest that the monovinyl chlorophyll ${\alpha}$ carboxylic biosynthetic route in plants may originate from the divinyl Mg-protoporphyrin IX pool.

• Fisheries and Aquatic Sciences
• /
• 제20권4호
• /
• pp.6.1-6.8
• /
• 2017

The objective of this research was to study the effect of astaxanthin (AST) on growth performance and antioxidant capacity in golden pompano (Trachinotus ovatus) both in vivo and in vitro. In the in vivo study, two diets were formulated with or without astaxanthin supplementation (D1 and D2; 0 and 200 mg/kg) to feed fish for 6 weeks. In the in vitro study, cells from hepatopancreas of golden pompano were isolated and four treatments with or without astaxanthin and $H_2O_2$ supplementation were applied (control group: without both astaxanthin and $H_2O_2$ treated; $H_2O_2$ group: just with $H_2O_2$ treated; $H_2O_2$ + AST group: with both astaxanthin and $H_2O_2$treated; AST group: just with AST treated). Results of the in vivo study showed that weight gain (WG) and special growth rate (SGR) significantly increased with astaxanthin supplemented (P < 0.05). Feed conversion ratio (FCR) of fish fed D2 diet was significantly lower than that of fish fed D1 diet (P < 0.05). Hepatic total antioxidant capacity (T-AOC) and the reduced glutathione (GSH) of golden pompano fed D2 diet were significant higher than those of fish fed D1 diet (P < 0.05). Superoxide dismutase (SOD) was significantly declined as astaxanthin was supplemented (P < 0.05). Results of the in vitro study showed that the cell viability of $H_2O_2$ group was 52.37% compared to the control group, and it was significantly elevated to 84.18% by astaxanthin supplementation ($H_2O_2$ + AST group) (P < 0.05). The total antioxidant capacity (T-AOC) and the reduced glutathione (GSH) of cell were significant decreased by oxidative stress from $H_2O_2$ (P < 0.05), but it could be raised by astaxanthin supplementation ($H_2O_2$ vs $H_2O_2$ + AST), and the malondialdehyde (MDA) was significant higher in $H_2O_2$ group (P < 0.05) and astaxanthin supplementation could alleviate the cells from lipid peroxidation injury. In conclusion, dietary astaxanthin supplementation can improve the growth performance of golden pompano. Moreover, astaxanthin can improve the golden pompano hepatic antioxidant capacity both in vivo and in vitro study by eliminating the reactive oxygen species.

• 한국수산과학회지
• /
• 제15권4호
• /
• pp.263-270
• /
• 1982

해중의 영양학적인 기초자료를 얻기 위하여 multi-enzyme system을 이용한 체외소화율과 아미노산분석을 기초로 한 단백질수를 측정하였다. 김 (P. tenera)의 체외소화율은 $78.5\sim82.2$로서 산지와 건조조건에 따라 약간의 차이를 보였으며, 잎파래(E. linza)나 다른 갈조류 (미역 U. pinnatifida, 톳 H. fusiforme, 모자반 S. fuuellum)에 비하여 높았고 효소활성 저해물질 (trypsin inhibitor)의 함량은 갈조류에서 높았다. 잎과래는 채외소화율이 김보다 낮음에도 불구하고 효소활성저해물질이 가장 낮은 특이한 결과론 보였다. 전체적으로 해조류의 체의소화을이 다른 연구자들의 생체실험에 의한 소화율 (in vivo digestility)보다 높은 결과를 보인 것은multi-enzyme system을 이용한 체외소화율 측정 방법을 해조류의 정확한 소화율 측정에 적용하기에는 문제성이 있는 것으로 밝혀졌다. 일륜 김에 대한 microwave cooking의 영향은 가열시간이 15분 경과하여도 현저한 소화율 증가는 볼 수 없었으며, 효소활성 저해물질함량은 서서히 감소하는 경향을 보였다. 또한 한국식으로 구운김의 체외소화율은 microwave로 15분 가열한 시료와 비슷하였다. 아미노산 분석 결과를 이용한 단백계수(Factor method)는 김의 경우 6.52로 계산되었고, 잎파래는 6.00, 미역 6.11, 모자반 5.85, 톳은 5.83이었으며, Kjeldahl전소분석결과를 이용한 단백계수(Kjeldahl Method)는 김 6.29, 잎파래 5.83, 미역 5.40, 모자반 5.45, 톳 5.49로 나타나, 종래의 조단백계수(6.25)보다 낮은 결과를 보였다. 해조추의 비단백태질소의 정확한 규명이 없는 상태에서, 해조의 단백질함량 측정에는 아미노산 분석결과를 이용한 새로운 단백계수(Factor Method)를 사용함이 바람직한 것으로 생각되었다.

• IMMUNE NETWORK
• /
• 제16권1호
• /
• pp.13-25
• /
• 2016

Dendritic cells (DCs) are considered to play major roles during the induction of T cell immune responses as well as the maintenance of T cell tolerance. Naive CD4⁺ T cells have been shown to respond with high plasticity to signals inducing their polarization into effector/helper or regulatory T cells. Data obtained from in vitro generated bone-marrow (BM)-derived DCs as well as genetic mouse models revealed an important but not exclusive role of DCs in shaping CD4⁺ T cell responses. Besides the specialization of some conventional DC subsets for the induction of polarized immunity, also the maturation stage, activation of specialized transcription factors and the cytokine production of DCs have major impact on CD4⁺ T cells. Since in vitro generated BM-DCs show a high diversity to shape CD4⁺ T cells and their high similarity to monocyte-derived DCs in vivo, this review reports data mainly on BM-DCs in this process and only touches the roles of transcription factors or of DC subsets, which have been discussed elsewhere. Here, recent findings on 1) the conversion of naive into anergic and further into Foxp3^- regulatory T cells (Treg) by immature DCs, 2) the role of RelB in steady state migratory DCs (ssmDCs) for conversion of naive T cells into Foxp3⁺ Treg, 3) the DC maturation signature for polarized Th2 cell induction and 4) the DC source of IL-12 for Th1 induction are discussed.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1997년도 춘계학술대회
• /
• pp.90-90
• /
• 1997

Natural products, which have been used for the treatment of hypertension, diuresis and nephritis in traditional oriental medicine, were selected for the screening of nitric oxide (NO) production in endothelial cells and kidney tissues in vitro as well as in vivo by measuring the conversion of [$\^$14/C]-L-arginine to [$\^$14/C]-L-citrulline, a coproduct of the enzyme reaction with NO. Confluent monolayer of endothelial cells were used for the screening of 16 natural products. Among the natural products, Zizyphus jujuba and Codonopsis pilosula stimulated endothelial NO synthase activity. Thus, both confluent monolayer of endothelial cells and kidney homogenates (glomeruli, cortical tubules, meudllae) were treated with Zizyphus jujuba and Codonopsis pilosula (final concentration 10 $\mu\textrm{g}$/$m\ell$) and NO releases were compared with those by receptor - dependent agonists, bradykinin and ADP and receptor - independent calcium ionophore A23187 in vitro. In rat experiment, NO releases in glomeruli, cortical tubules and medullae and plasma renin activity were assessed after intraperitoneal injection of Zizyphus jujuba and Codonopsis pilosula (10 mg/kg/day for 4 days). As a result, both Zizyphus jujuba and Codonopsis pilosula significantly increased NO releases in cultured endothelial cells, kidney tissues in vitro as well as in vivo. Stimulation of NO releases by Zizyphus jujuba and Codonopsis pilosula was similar to those by receptor - dependent agonists, bradykinin and ADP and receptor - independent calcium ionophore A23187 in cultured endothelial cells. However, plasma renin activity was not influenced by these two natural products. In conclusion, stimulatory effects of Zizyphus jujuba and Codonopsis pilosula on NO release in kidney may contribute their hypotensive effects and antinephritic action possibly by increasing renal blood flow.

• 대한한의학회지
• /
• 제22권3호
• /
• pp.31-41
• /
• 2001

Objectives : This study was performed to investigate the effects of Cordyceps Sinensis (CS) and Cordyceps Militaris (CM) on anti oxidation in the livers of ${CCl_4}-treated$ rats. Methods : Hepatotoxicity in rats was induced by carbon tetracWoride. $CCl_4-induced$ rats were administered with the extract of CS and CM. Results : In vitro, CS and CM didn't affect levels of lipid peroxide and the activities and type conversion ratio of xanthine oxidase. However, hydroxyl radicals and DPPHL radicals were decreased. In vivo, in the ${CCl_4}-treated$ rats, lipid peroxide, the activities and type conversion ratio of xanthine oxidase and superoxide radicals were increased but superoxide dismutase was decreased. After CS and CM were administered to ${CCl_4}-treated$ rats, levels of lipid peroxide, the activities and type conversion ratio of xanthine oxidase and superoxide radicals were decreased but superoxide dismutase was increased. Conclusions : These results suggest that CS and CM decrease the activities of free-radical-generating enzymes which form lipid peroxide and increase the activities of oxygen free radical scavenging enzymes.