| In vitro: |
| Eur J Pharm Sci. 2012 Dec 18;47(5):952-64. | | QSAR, docking and in vitro studies for anti-inflammatory activity of cleomiscosin A methyl ether derivatives.[Pubmed: 23022518] | A series of five (6a-8b) novel polyhalogenated derivatives and an interesting ester (9a) derivative have been synthesized from cleomiscosin A methyl ether.
METHODS AND RESULTS:
All the six derivatives were subjected to in silico QSAR modeling and docking studies and later the predicted results were confirmed through in vitro experiments. QSAR modeling results showed that compounds 6a and 9a possessed anti-inflammatory activity comparable or even higher than diclofenac sodium. Docking results revealed that compounds 9a and 6a showed very good anti-inflammatory activity due to low docking energies of viz., IL6 (-92.45 and -81.993 kcal mol(-1)), TNF-α (-94.992 and -69.235 kcal mol(-1)) and IL1β (-67.462 and -65.985 kcal mol(-1)). Further all the six novel derivatives were subjected for in vitro anti-inflammatory activity using primary macrophages cell culture bioassay system. At the initial doses of 1 μg/ml and 10 μg/ml, the pro-inflammatory cytokines (IL-1β, IL-6 and TNF-α) were quantified from cell culture supernatant using enzyme linked immunosorbent assay (ELISA). The in vitro effect of 6a-9a on cell viability in mouse peritoneal macrophage cells isolated from mice was evaluated using MTT assay.
CONCLUSIONS:
The in silico and in vitro data suggested that all the derivatives might be considered as potential anti-inflammatory drug-like molecules. | | Eur J Med Chem. 2010 Nov;45(11):5150-6. | | Synthesis and anti-inflammatory activity of derivatives of coumarino-lignoid, cleomiscosin A and its methyl ether.[Pubmed: 20813432] |
METHODS AND RESULTS:
Six novel cleomiscosin A (a coumarino-lignoid), derivatives have been synthesized for the first time by using electrophilic substitution reaction to give nuclear nitrated and halogenated derivatives of cleomiscosin A in good yields. Structures of these compounds were established on the basis of IR, (1)H NMR, (13)C NMR and Mass spectral data. Some of the synthesized derivatives were tested for in-vitro target based anti-inflammatory study using primary macrophages cell culture bioassay system.
CONCLUSIONS:
The results showed that the compounds 1a, 3a and 4a (1 and 10 μg/mL) exhibited potent anti-inflammatory activity. | | Zhongguo Zhong Yao Za Zhi. 2007 Jun;32(12):1175-9. | | Chemical constituents from branch of Macaranga adenantha and their TNF-alpha inhibitory activity.[Pubmed: 17802880] | To investigate the chemical constituents of the brach of Macaranga adenantha, and evaluate their TNF-alpha inhibitory activity.
METHODS AND RESULTS:
The chemical conshifuents were isolated and purified by chromatographic methods. Structures of the compounds were identified by spectroscopic methods. The TNF-alpha secretion inhibitory activity of the mouse peritoneal macrophages was evaluated by MTT methods.
Ten compounds were isolated and their structures were identified as: cleomiscosin A (1), cleomiscosin B (2), ellagic acid 4-O-alpha-D-rhamnopyranside (3), ellagic acid 4-O-beta-D-xylopyranoside (4), vanillic acid (5), (24R) -stigmast-4-en-3-one (6), (24R) -stigmast-3, 6-dione (7), (24R) -6beta-hydroxy-stigmast-4-en-3-one (8), daucosterol (9), beta-sitosteryl glucoside-6'-O-heptadecoicate (10). At a concentration of 10 micromol x L(-1), compounds 1, 3 and 4 showed inhibitory activity to TNF-alpha secretion of the mouse peritoneal macrophages with the inhibitory rates of 57.0%, 64.4%, and 57. 4%, respectively.
CONCLUSIONS:
All compounds were isolated from genus Macaranga for the first time. Compounds 1, 3, and 4 were active against TNF-alpha secretion of the mouse peritoneal macrophages.
CONCLUSION:
All compounds were isolated from genus Macaranga for the first time. Compounds 1, 3, and 4 were active against TNF-alpha secretion of the mouse peritoneal macrophages. | | J Nat Prod. 1984 May-Jun;47(3):550-1. | | Antitumor Agents, 65. Brusatol and Cleomiscosin A, Antileukemic Principles from Brucea javanica.[Pubmed: 6481366] |
METHODS AND RESULTS:
Antitumor Agents, 65. Brusatol and Cleomiscosin A, Antileukemic Principles from Brucea javanica. | | Arch Pharm Res. 2007 Mar;30(3):275-81. | | Antioxidant activity of cleomiscosins A and C isolated from Acer okamotoanum.[Pubmed: 17424931] | Phytochemical investigation of Acer okamotoanum leaf and twig led to the isolation of two coumarinolignans, Cleomiscosin A (1) and cleomiscosin C (2).
METHODS AND RESULTS:
Here, we found that 2 dose-dependently inhibits LDL oxidation mediated by either catalytic copper ions (Cu2+) or free radicals generated with the azo compound 2,2'-azobis-(2-amidinopropane)dihydro-chloride (AAPH) with IC50s of 29.5 and 11.9 microM, respectively. By electrophoretic analysis, we also observed that 2 protects apolipoprotein B-100 (apoB-100) against Cu2+-induced fragmentation (65.3% inhibition at 5 microM). Furthermore, fluorescence analyses clearly indicated that both 1 and 2 protect against the oxidative modification of apoB-100 induced by either Cu2+ or HOCl (1, IC50s of 13.4 and 8.1 microM, respectively; 2, IC50s of 23.6 and 3.9 microM, respectively).
CONCLUSIONS:
These findings suggest that 1 and 2 could be beneficial in preventing LDL oxidation in atherosclerotic lesions. |
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