• Biomolecules & Therapeutics
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• 제5권1호
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• pp.87-93
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• 1997

DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

• Journal of Applied Biological Chemistry
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• 제43권3호
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• pp.152-155
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• 2000

The contents of various capsaicinoids viz. nordihydrocapsaicin (NDC), capsaicin (CAP), and dihydrocapsaicin (DHC) were determined in different parts of fruits (placenta, pericarps, seeds, and whole fruits) at different developmental stages after flowering and compared with the capsaicinoid synthetase (CS) activity. The capsaicinoid contents were very low up to 24 days after flowering (DAF), and there was a significant increase at 36 DAF in all parts of fruits. The enzyme activity of placenta increased to maximum at 24 DAF, and thereafter it gradually decreased. There were no significant amounts of enzyme activities in other parts of the fruits. In Subicho (inbred line) the content of DHC was slightly higher than CAP in all parts. of the fruits throughout the development stages of fruits, whereas in Chung Yang the CAP content was higher compared to the DHC content. The contents of total capsaicinoids in Chung Yang were also higher than Subicho. However, the crude enzyme extract obtained from Chung Yang led to the synthesis of DHC almost exclusively when the substrate, 8-methyl nonanoic acid, was added to the reaction mixture. Our results suggest that the composition of individual analogue of capsaicinoids depends upon the substrate available in the fruits.

• 동아시아식생활학회지
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• 제16권5호
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• pp.585-591
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• 2006

We report a novel HPLC method for analyzing the capsaicinoids and nonivamide. The following conditions were used: a total column and column temperature of $3^{\circ}C$, a detection wavelength of 280 nm, an eluent containing acetonitrile : 0.5% formic acid(31:69, v/v). The experimental data was compared with standard nonivamide and capsaicin. The results showed that nonivamide was eluted in 96.7 minutes with a recovery ratio of 96.5% after adding known nonivamide. In addition, the detection limit for nonivamide was 18.6 ng. The capsaicinoids from Korean pepper were extracted (after blooming 60th) from 3 breeds cultivated in Korea, Buchon, Chungyang and Hanbando. and crisis it analyzed sympathizes the nonivamide in the result nonivamide from the Buchon and the Chungyang which are not detected from the Hanbando $0.16{\sim}0.24{\mu}g/g$ it detects with very small amount it contains it confirmed the each capsaicinoid with the HPLC and the LC-MS. These results are expected contribute to the quality control of various product processes, which includes product delivery inspection as well as examining the capsaicinoids present in the product for possible medicine manufacture and various foodstuff, and the nonivamide content, which may be a feed for various manufacturing processes involving chemical synthesis.

• 셀메드
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• 제3권3호
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• pp.21.1-21.5
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• 2013

Cholesterol gallstones are a digestive disease of high prevalence that has many risk factors; for this reason, research has focused mainly on how to prevent it rather than how to treat it. Many molecules of the hepatic, bile and intestinal systems are involved in the pathophysiology of this disease, making it very difficult to find a therapeutic target. The pharmacological treatment is limited, so when gallstones generate symptoms, medical treatment indicates gallbladder removal. Ursodeoxycholic acid is used to dissolve cholesterol stones, and ezetimibe and statins are other drugs with possible applications in the treatment of this disease. Given the small number of drugs that have been developed for treating this disease, the research of natural products becomes of paramount importance. Resources such as black radish, glucosinolates, fenugreek, capsaicin, curcumin, garlic, and onion, have all shown significant effects in the prevention and treatment of cholesterol gallstones. In this review, we made a synthesis of the scientific reports that deal with these natural products and that can serve as antecedents for finding a way to treat the most common disease of the gallbladder.