• The Korean Journal of Nuclear Medicine
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• v.36 no.2
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• pp.121-132
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• 2002

Purpose : Taxol(Paclitaxel), an antineoplastic agent, has been used in the treatment of ovarian and breast cancers. The determination of optimal Taxol concentrations in human serum was required for enhancing therapeutic effect and maintaining the appropriate Taxol level in blood. This study was aimed to synthesizeradiolabeled Taxol derivatives as radiotracer in competitive radioimmunoassay for monitoring Taxol concentrations in blood and to determine the usefulness of its derivatives. Materials and Methods : Hemisucdcinyltaxol(HT) was synthesized by esterification of Taxol with succinic anhydride. Tyraminehemisuccinyltaxol(THT) was synthesized by coupling of HT with tyramine using isobutylchlormate as coupling agent and purified by HPLC. By using chloramine-T($5.25mg/ml,\;10{\mu}{\ell}$) as oxidant agent, THT($4mg/ml,\;30{\mu}{\ell}$) was labeled wity $^{125}I\;(37MBq,\;1mCi)$. To estimate the stability of purified THT, $^{125}I-iodotyraminehemisuccinyltaxol(^125}ITHT)$ was dissolved in 80% acetonitrile aqueous solution, and the solution was incubated at $4^{\circ}C\;and\;37^{\circ}C$ for 7 days. At various time intervals, the stability of THT and $^{125}ITHT$ was monitored. The titer of Taxol monoclonal antibody, 3G5A7, was determined by competitive radioimmunoassay using $^{125}ITHT$ as a labeled antigen. A standard dose-response curve was demonstated by Taxol competitive radioimmunoassay. Resulls : HT and THT were synthesized with 79.9% and 19.5% yield, respectively. The labeling yield of $^{125}ITHT$ was 93%. After 7 days, the chemical purity of THT was 96.5% at $4^{\circ}C$, and 97.5% at $37^{\circ}C$. After 3 days, $^{125}ITHT$ was stable with 94.7% at $4^{\circ}C$ and 93.4% at $37^{\circ}C$. After 7 days, fadiochemical purity was diminished to 88.1% at $37^{\circ}C$. The titer of Taxol monoclonal antibody, 3G5A7, was determined to 1:256. A standard dose-response curve demonstated good collinearity ($R^2=0.971$) as Taxol concentration-dependent manner. Conclusion : Competitive radioimmunoassay using $^{125}I-iodotyraminehemisuccinytaxol$ as radiotracer could be used to monitor for concentration of Taxol in the human serum.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.3 s.47
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• pp.393-397
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• 2004

L-Carnitine $({\beta}-hydroxy-{\gamma}-trimethyl-ammoniumbutyric{\;}acid)$ is a small water-soluble molecule important in mammalian fat metabolism. It is essential for the normal oxidation of fatty acids by the mitochondria, and is involved in the trans-esterification and excretion of acyl-CoA esters. In this paper, to investigate the relationship between aging and L-carnitine, we investigated the effects of in vitro matrix-metalloproteinase (MMP) inhibition and activity and expression of UYA-induced MMPs in human skin fibroblasts. Also, we studied to develop as anti-aging cosmetics with L-carnitine. Fluorometric assays of the proteolytic activities of MMP-1 (collagenase) were performed using fluorescent collagen substrates. ELISA (enzyme linked immune sorbent assay), gelatin-substrate zymography, RT-PCR ELISA techniques were used for the effects of L-carnitine on MMP expression, activity, and MMP mRNA expression in UVA irradiated fibroblast $(5\;J/cm^2)$, respectively. In addition, we performed clinical study with L-carnitine cream. L-carnitine inhibited the activities of MMP-1 in a dose-dependent manner and the $IC_{50}$ values calculated from semi-log plots were 2.45 mM, and L-carnitine showed strong inhibition on MMP-2 (gelatinase) activity in UVA irradiated fibroblast by zymography. Also, UVA induced MMP-1, 2 expression was reduced $43\%,\;53\%$ by treated with L-carnitine at 1.25 mM, and MMP-1 mRNA expression was reduced dose-dependent manner. Therefore L-carnitine was able to significantly inhibit the MMP activity, and regulate MMP expression in protein and mRNA level. The results of clinical study showed that $1.0\%$ L-carnitine treated group reduced wrinkle significantly compared with placebo treated group (P<0.05). All these results suggest that L-carnitine may be useful as new anti-aging cosmetics for protection against UVA induced Mm expression and activity.

• Applied Biological Chemistry
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• v.47 no.2
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• pp.251-257
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• 2004

The root of lxeris dentata forma albiflora was extracted with 80% aqueous MeOH and solvent fractionated with EtOAc, n-BuOH and water, successively. From the EtOAc and n-BuOH fractions, four sesquiterpene compounds were isolated through the repeated silica gel and ODS column chromatographies. The chemical structures were determined as zaluzanin C (1), $9{\alpha}-hydroxyguaian-4(l5),10(14),11(13)-triene-6,12-olide$ (2), $3{\beta}-O-{\beta}-D-glucopyranosyl-8{\alpha}-hydroxyguaian-4(15),10(14 )-diene-6,12-olide$ (3), and $3{\beta}-O-{\beta}- D-glucopyranosyl-8{\beta}hydroxyguaian-10(14)-ene-6,12-olide$ (4) through the interpretation of several spectral data including 2D-NMR. Some showed the inhibitory effects on DGAT (Diacylglycerol acyltransferase), ($IC_{50}$ values of 1, 2: 0.13, 0.10 mM), the catalyzing enzymes of the intracellular esterification of diacylglycerol and FPTase (Famesyl-protein transferase), ($IC_{50}$ values of 1, 2: 0.15, 0.18 mM), the farnesylation enzyme for Ras protein charge of cancer promotion.