Chemical constituents from Clausena excavata and their inhibitory activities against proliferation of synoviocytes / 中国中药杂志

The chemical constituents from the stems and leaves of Clausena excavata were isolated and purified by column chromatography with silica gel, ODS, Sephadex LH-20 and RP-HPLC. The chemical structures of the isolated compounds were identified on the basis of physicochemical properties, spectroscopic analysis, as well as the comparisons with the data reported in literature. Nineteen compounds were isolated from the 90% ethanol extract of the stems and leaves of C. excavata, which were identified as methyl orsellinate(1), syringaresinol(2), lenisin A(3), scopoletin(4), osthenol(5), N-benzoyltyrarnine methyl ether(6), N-p-coumaroyltyramine(7), aurantiamide acetate(8), 1H-indole-3-carboxaldehyde(9), furostifoline(10), clausenalansine E(11), 3-formylcarbazole(12), clausine L(13), clausine E(14), methyl carbazole-3-carboxylate(15), glycosinin(16), murrayafoline A(17), clausine H(18) and 2,7-dihydroxy-3-formyl-1-(3'-methyl-2'-butenyl)carbazole(19). Among these isolated compounds, compounds 1-11 were isolated from C. excavata for the first time, and compounds 1, 2 and 10 were isolated from the genus Clausena for the first time. In addition, this study evaluated the anti-rheumatoid arthritis activities of compounds 1-19 by measuring their anti-proliferative effects on synoviocytes in vitro according to MTS method. Compounds 10-19 displayed remarkable anti-rheumatoid arthritis activities, which exhibited the inhibitory effects on the proliferation of MH7 A synovial fibroblast cells with the IC_(50) values ranging from(27.63±0.18) to(235.67±2.16) μmol·L~(-1).

Methanolic extract of Clausena excavata promotes wound healing via antiinflammatory and anti-apoptotic activities

Objective: To investigate the anti-inflammatory properties of methanolic extract of Clausena excavata in lipopolysaccharide (LPS)-activated macrophages (J774A.1) and the effect on skin wound in a rat model through determining cytokine levels and gene expressions. Methods: The effects of methanolic extract of Clausena excavata on in vitro viability and TNF-α, IL-6, IL-10, and nitric oxide release by LPS-activated J774A.1 cells were determined. In addition, relative expressions of BAX, BCL-2 and COX-2 genes were examined in healed wounds of rats. Results: The methanolic extract of Clausena excavata was not toxic to J774A.1 cells at the highest dose of 400 μg/mL. It decreased levels of TNF-α and IL-6, while increasing IL-10 level in LPS-activated J774A.1 cells and in the healed wounds of rats. The methanolic extract of Clausena excavata also inhibited nitric oxide production in LPS-activated J774A.1 cells. The BAX and COX-2 genes were downregulated while the BCL-2 gene was upregulated in the healed wound of rats. Conclusions: The methanolic extract of Clausena excavata promotes wound healing via its anti-inflammatory and anti-apoptotic activities.

Methanolic extract of Clausena excavata promotes wound healing via anti-inflammatory and anti-apoptotic activities

Objective: To investigate the anti-inflammatory properties of methanolic extract of Clausena excavata in lipopolysaccharide (LPS)-activated macrophages (J774A.1) and the effect on skin wound in a rat model through determining cytokine levels and gene expressions.Methods: The effects of methanolic extract of Clausena excavata on in vitro viability and TNF-α, IL-6, IL-10, and nitric oxide release by LPS-activated J774A.1 cells were determined. In addition, relative expressions of BAX, BCL-2 and COX-2 genes were examined in healed wounds of rats. Results: The methanolic extract of Clausena excavata was not toxic to J774A.1 cells at the highest dose of 400 μg/mL. It decreased levels of TNF-α and IL-6, while increasing IL-10 level in LPS-activated J774A.1 cells and in the healed wounds of rats. The methanolic extract of Clausena excavata also inhibited nitric oxide production in LPS-activated J774A.1 cells. The BAX and COX-2 genes were downregulated while the BCL-2 gene was upregulated in the healed wound of rats. Conclusions: The methanolic extract of Clausena excavata promotes wound healing via its anti-inflammatory and anti-apoptotic activities.

Analysis of the Difference of Volatile Oil Components from the Leaves of Clausena lansium and Clausena excavata by GC-MS / 中国药房

OBJECTIVE： To analyze the difference of volatile oil components from the leaves of Clausena lansium and Clausena excavata. METHODS： The volatile oil was extracted from the leaves of C. lansium and C. excavata by steam distillation. GC-MS method was adopted to analyze volatile oil to obtain TIC. After mass spectra scanning of the chromatographic peaks in the TIC diagram by HPMSD chemical workstation， chemical components of volatile oil in 2 kinds of samples were identified by retrieving and comparing mass spectrum database NIST Version 1.7. The peak area normalization method was used to calculate the relative mass fraction of each component. RESULTS： A total of 43 and 31 kinds of components were identified in volatile oil from the leaves of C. lansium and C. excavata； total relative mass fractions were 97.59％ and 98.57％. Relative mass fractions of 19 and 18 components in volatile oil from the leaves of C. lansium and C. excavata were more than 1％， mainly being sesquiterpenoids. Relative mass fractions of 7 and 5 components in volatile oil from the leaves of C. lansium and C. excavata were more than 5％； the volatile components in volatile oil from the leaves of C. lansium were mainly （-）-spatol （12.35％） and （E）-5-{（1R，3R，6S）-2，3-dimethyltricyclic [2.2.1.02，6] heptane-3-yl}-2-methyl pentane-2-enol （14.70％）； those from the leaves of C. excavata were mainly （E）-sesquihydrated betuline （24.94％） and 1-（1， 5-dimethy-4-hexenyl）-4-methyl-benzene （16.15％）. A total of 4 components were found in volatile oil from the leaves of C. lansium and C. excavata， mainly being α-humulene， （E）-5-{（1R，3R，6S）-2，3-dimethyltricyclic [2.2.1.02，6] heptane-3-yl}-2-methylpentaeryl-2-enol， caryophyllene oxide and （-）-spatol； the content differences of them were not significant. CONCLUSIONS： The components of volatile oils from the leaves of C. lansium and C. excavata are basically similar However， the composition and comtent of specific components are quiet different and can not substituted for each other.

Antiproliferative Properties of Clausine-B against Cancer Cell Lines

Background: Clausine B, a carbazole alkaloid isolated from the stem bark of Clausena excavata, was investigated for its antiproliferative activities against five human cancer cell lines: HepG2 (hepatic cancer), MCF-7 (hormone-dependent breast cancer), MDA-MB-231 (non-hormone-dependent breast cancer), HeLa (cervical cancer), and CAOV3 (ovarian cancer). Methods: Chang liver (normal cells) was used as a control. The effect of clausine-B was measured using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Results: Clausine-B was found to be active (IC50<30 μg/mL) against four of the cancer cell lines tested. The IC50 values for these four lines were: 21.50 μg/mL (MDA-MB-231), 22.90 g/ml (HeLa), 27.00 μg/mL (CAOV3) and 28.94 μg/mL (HepG2). Clausine-B inhibited the MCF-7 cancer cell line at 52.90 μg/mL, and no IC50 value was obtained against Chang liver. Conclusion: It is possible that the phenolic group in clausine-B responsible for the antiproliferative activities found in this study.