• Archives of Pharmacal Research
• /
• 제19권6호
• /
• pp.441-446
• /
• 1996

The Schizonepeta tenuifolia spikes (STS) have been used as a traditional folk medicine for antiinflammatory, analgesic, anti-pyretic and anti-spasmodic purpose in Korea. Phytosterols (mixture of campesterol 3.68%, stigmasterol 2.30% and ${\beta}$-sitosterol 94.02%) and hesperidin were isolated by chromatography from ether and n-BuOH fractions of STS respectively. These compounds significantly reduced the blood glucose level and lessened the loss of body weight and water consumption dose-dependently when administered at a i.p. doses of 10 and 20 mg/kg for 4 days after the i.v. injection of streptozotocin (I 80 mg/kg). In the morphologic study, these compounds showed protective activity on the pancreatic islets, especially .betha.-cells, from the degenerative changes by streptozotocin.

• 생약학회지
• /
• 제28권4호
• /
• pp.275-279
• /
• 1997

Fruits of Arctium lappa L. (Compositae), which has been used as the antiinflammatory, detoxifying and diuretic agents in the folk remedies, was examined on the in vitro oxidation of human low density lipoprotein (LDL). Several lines of evidence indicate that oxidized LDL (Ox-LDL) may promote atherogenesis. Hence. The role of antioxidants in the prevention of LDL oxidation needs to be determined. The activity of fractions of Arctii Fructus treated with oxidized LDL which was incubated with $16\;{\mu}M$ of $Cu^{2+}$ for metal catalyzed oxidation was investigated. The BuOH fraction (4\;ppm) inhibited the oxidative modification of LDL as evidenced by a decrease in the lipid peroxide content (thiobarbituric acid reacting substances activity), the negative charge of LDL (electrophoretic mobility) and increase of the vitamine E content.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.339.1-339.1
• /
• 2002

Since two selective COX-2 inhibitors. celecoxib and rofecoxib, showed good biological activity as antiinflammatory agents. many medicinal chemists are interested in specific COX-2 inhibitors. The distinguished feature of these drugs is that the 5-membered heterocycle ring is substituted with two aryl groups. Therefore, in this study, we designed a new hydantoin derivatives via the reaction of unnatural amino acids as selective COX-2 inhibitors, In systematically steps. 5-phenyl-1 (or substituted) hydantoin derivatives were prepared through esterification. bromination, C-N bond formation, cyclization from phenyl acetic acid. Particularly. a novel hydantoin ring was converted from unnatural amino acids with potassium isoyanate. In last step. the final analogs were synthesized the substitution at 3-position with alkyl reagents.

• Journal of Ginseng Research
• /
• 제44권3호
• /
• pp.405-412
• /
• 2020

Background: Root rot is a serious destructive disease of Panax notoginseng, a famous cultivated araliaceous herb called Sanqi or Tianqi in Southwest China. Methods: The chemical substances of Sanqi rot roots were explored by chromatographic techniques. MS, 1D/2D-NMR, and single crystal X-ray diffraction were applied to determine the structures. Murine macrophage RAW264.7 and five human cancer cell lines were used separately for evaluating the antiinflammatory and cytotoxic activities. Results and Conclusion: Thirty dammarane-type triterpenes and saponins were isolated from the rot roots of P. notoginseng. Among them, seven triterpenes, namely, 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β,6α,12β,20-tetrol (1), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α,12β,20-triol (2), 20(S)-dammar-12-oxo-23-ene-25-hydroperoxyl-3β,6α,20-triol (3), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-12β,20-diol (4), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid (5), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid methyl ester (6), and 6α-hydroxy-22,23,24,25,26,27-hexanordammar-3,12,20-trione (7), are new compounds. In addition, 12 known ones (12-16 and 19-25) were reported in Sanqi for the first time. The new Compound 1 showed comparable antiinflammatory activity on inhibition of NO production to the positive control, whereas the known compounds 9, 12, 13, and 16 displayed moderate cytotoxicities against five human cancer cell lines. The results will provide scientific basis for understanding the chemical constituents of Sanqi rot roots and new candidates for searching antiinflammatory and antitumor agents.

• Natural Product Sciences
• /
• 제17권3호
• /
• pp.250-255
• /
• 2011

The immune system is finely balanced by the activities of pro-inflammatory and anti-inflammatory mediators or cytokines. Unregulated activities of these mediators can lead to the development of various inflammatory diseases. A variety of safe and effective anti-inflammatory agents are available with many more drugs under development. Of the natural compounds, the sesquiterpenes (nootkatone, ${\alpha}$-cyperone, valencene and ${\alpha}$-selinene) isolated from C. rotundus L. have received much attention because of their potential antiinflammatory effects. However, limited studies have been reported regarding the influence of sesquiterpene structure on anti-inflammatory activity. In the present study, the anti-inflammatory potential of four structurally divergent sesquiterpenes was evaluated in lipopolysaccaride (LPS)-stimulated RAW 264.7 cells, murine macrophages. Among the four sesquiterpenes, ${\alpha}$-cyperone and nootkatone, showed stronger anti-inflammatory and a potent NF-${\kappa}B$ inhibitory effect on LPS-stimulated RAW 264.7 cells. Molecular analysis revealed that various inflammatory enzymes (iNOS and COX-2) were reduced significantly and this correlated with downregulation of the NF-${\kappa}B$ signaling pathway. Additionally, electrophoretic mobility shift assays (EMSA) elucidated that nootkatone and ${\alpha}$-cyperone dramatically suppressed LPS-induced NF-${\kappa}B$-DNA binding activity using 32Plabeled NF-${\kappa}B$ probe. Hence, our data suggest that ${\alpha}$-cyperone and nootkatone are potential therapeutic agents for inflammatory diseases.

• Biomolecules & Therapeutics
• /
• 제9권3호
• /
• pp.188-193
• /
• 2001

Free radical scavengers or quenching agents for reactive oxygen species (ROS) present in consumable fruits, vegetables, and beverages have received considerable attention as potential antioxidants, and thus uses for treatment of several human diseases. In this study, grapevine shoot extract (GSE) containing high concentration of resveratrol and viniferine was evaluated for antioxidant potential and inhibition of pro-inflam-matory mediator production. Utilizing 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging activity and xanthine oxidase (XOD) inhibition assay the GSE showed inhibitory effects of DPPH radical scavenging and XOD activity with the $IC_{50}$/ values of 34.5 and 155 $\mu\textrm{g}$/ml, respectively. In addition, GSE also exhibited the inhibition of prostaglandin E$_2$ (PGE$_2$) and nitric oxide (NO) production in lipopolysaccharide (LPS)-induced mouse macrophage RAW264.7 cells with the $IC_{50}$/ value of 6.4 and 14.5 $\mu\textrm{g}$/ml, respectively. This result suggests that grapevine shoot extract has the potential activity as a natural antioxidant or antiinflammatory agent.

• Advances in Traditional Medicine
• /
• 제3권2호
• /
• pp.90-99
• /
• 2003

There are several data in the literature indicating a great variety of pharmacological activities of Polypodium genus, which exhibit antiinflammatory and immunomodulatory activities. Since one of our main interests is to obtain natural immunoregulatory agents devoid of pharmacological adverse effects, we used flow cytometry analysis to highlight relative contributions of a water-soluble fraction of different concentrations of Polypodium rhizome extracts on lymphocyte subpopulations, NK and LAK activity. To measure their potential immunoregulatory activity a T cell proliferation assay in response to phytohemaglutinin (PHA) and mixed lymphocyte reactions were chosen. As a confirmatory bioassay we studied the effect of our extracts on CD45RO and CD95 antigen expressions. The results indicate that CD95 expression dramatically increases after peripheral blood lymphocyte activation and treatment with Polypodium leucotomus, cambricum and vulgare extracts, suggesting a powerful intrinsic pro-apoptotic effect.

• 동의생리병리학회지
• /
• 제24권2호
• /
• pp.236-241
• /
• 2010

The purpose of this study was to investigate the mechanism of ethanol extract of Agrimonia pilosa Ledeb. (EAP)-reduced melanogenesis and diphenyl-picryl-hydrazyl (DPPH) radical scavenging activity. Agrimonia pilosa Ledeb., a perennial herbaceous plant, has been used as an antihemorrhagic, anthelminntic, and antiinflammatory agents in Chinese herbal medicine. In the present study, we observed that melanin synthesis and tyrosinase activity of B16F10 cells were significantly decreased by EAP. However, EAP could not suppress tyrosinase activity in the cell-free system, whereas kojic acid directly inhibited tyrosinase activity. Furthermore, EAP decreased the protein expression of tyrosinase, tyrosinase-related prootein 1 (TRP-1), and tyrosinase-related prootein 2 (TRP-2). EAP scavenged DPPH radical up to 41% with 100 ${\mu}g/m{\ell}$ concentration. These results suggest that the hypopigmentary effect of EPA was due to regulation of tyrosinase protein.

• Bulletin of the Korean Chemical Society
• /
• 제28권4호
• /
• pp.561-566
• /
• 2007

Adenosine kinase (AK) is a ubiquitous intracellular enzyme, which catalyzes the phosphorylation of adenosine (ADO) to adenosine monophosphate (AMP). AK inhibitors have therapeutic potential as analgesic and antiinflammatory agents. A chemical feature based pharmacophore model has been generated from known AK inhibitors (26 training set compounds) by HypoGen module implemented in CATALYST software. The top ranked hypothesis (Hypo1) contained four features of two hydrogen-bond acceptors (HBA) and two hydrophobic aromatics (Z). Hypo1 was validated by 124 test set molecules with a correlation coefficient of 0.905 between experimental and estimated activity. It was also validated by CatScramble method. Thus, the Hypo1 was exploited for searching new lead compounds over 238,819 chemical compounds in NCI database and then the selected compounds were screened based on restriction estimated activity and Lipinski's rules to evaluate their drug-like properties. Finally we could obtain 72 new lead candidates and the two best compound structures from them were posted.

• 한국약용작물학회지
• /
• 제24권2호
• /
• pp.129-135
• /
• 2016

Background: In this study, we investigated the antibacterial and nitric oxide (NO) production inhibitory activities of 75% ethanol extract of Prunus sargentii branches and its fractions against acne pathogens. Methods and Results: The antibacterial activity against acne causing pathogens was determined using the disc diffusion assay. The ethyl acetate fraction showed higher activities against Propionibacterium acnes, Staphylococcus aureus and Staphylococcus epidermidis than those shown by other fractions. In the DPPH radical and NO scavenging assays, the butanol fraction showed strong DPPH radical and NO scavenging abilities. These activities were related to the total polyphenol and flavonoid contents of butanol fraction. On the other hand, the chloroform and ethyl acetate fractions exhibited the highest NO production inhibitory activity in Lipopolysaccharide (LPS)-stimulated Raw 264.7 cells compared to those exhibited by other fractions. Conclusions: The extract and its ethyl acetate fraction from the branches of P. sargentii exhibited antibacterial activity and could be used as functional materials in antimicrobial related fields. Moreover, the chloroform and ethyl acetate fractions are potential antiinflammatory agents and butanol fraction acts as an effective radical scavenger.