[In vivo transdermal penetration enhancing activity of essential oil from Zanthoxyli Pericarpium by using microdialysis technique].

The aim of this paper is to investigate the topical pharmacodynamics behavior of different lipophilic model drugs after treatment with essential oil from Zanthoxyli Pericarpium by using the cutaneous microdialysis technique, and then evaluate its in vivo transdermal penetration enhancing properties. Two traditional Chinese medicine active components, namely tetramethylpyrazine and puerarin, were chosen as lipophilic and hydrophilic model drugs, respectively. Firstly, the concentration difference method was employed to measure the in vitro recovery rate and loss of the microdialysis probe, and the in vivo recoveries of two model drugs were determined by using the retrodialysis method. Secondly, the skin pharmacodynamics behaviors of two model drugs were studied after treatment with different concentrations of the essential oil, and the well-established and standard penetration enhancer Azone was selected as a positive control. It was found that the recovery of microdialysis probe was equal to its loss for two model drugs, with no interaction between drugs in dialysis membranes. The retrodialysis studies revealed that the in vivo recovery of tetramethylpyrazine and puerarin were 59.17%, 19.85%, respectively. The skin pharmacodynamics studies showed that the essential oil could facilitate the transdermal absorption of tetramethylpyrazine in a concentration-dependent manner, and the enhancement ratio (ER) for 5% essential oil was 98.64, which was higher than that of the optimum concentration of Azone (3% Azone, ER=89.11). Meanwhile, the Zanthoxyli Pericarpium could effectively promote the transdermal permeation of the puerarin in a concentration-dependent manner. Hence, this study further confirmed that the Zanthoxyli Pericarpium had excellent penetration-enhancing activity as a natural transdermal penetration enhancer, providing data support for its application in traditional Chinese medicine external preparations.

[PTP1B inhibitory activities of bromophenol derivatives from algae].

OBJECTIVE: To study the protein tyrosine phosphatase-1B (PTP1B) inhibitory activity of natural products from algae aiming at searching for new way for the treatment of type 2 diabetes mellitus (T2DM) and obesity. METHOD: Bromophenols derivatives from algae were screened against the PTP1B by the colorimetric assay with GST/PTP1B fusion protein. The Me2SO was distributed as the full enzyme activity, and Na3VO4 (IC50 2 micromol L(-1)) was distributed as the positive control. Inhibition rate was assayed and IC50 were calculated by LOGIT method. RESULT: Three bromophenols from Rhodomela confervoides and Leathesia nana, 3, 4-dibromo-5-(methoxymethyl)-1, 2-benzenediol (1), 2-methyl-3-(2, 3-dibromo4, 5-dihydroxy)-propylaldehyde (2) and 3-(2, 3-dibromo-4, 5-dihydroxy-phenyl)-4-bromo-5, 6-dihydroxy-1, 3-dihydroiso-benzofuran (3) showed significant inhibitory activity against PTP1B. IC50 values were 3.4 +/- micromol L(-1), 4.5 micromol L(-1) and 2.8 micromol L(-1), respectively. CONCLUSION: The results prove that three bromophenol derivatives from algae with significant inhibitory activity against PTP1B were potential and effective therapeutic agents for treatment of T2DM and obesity.

[Studies on chemical constitutes of Acantophora spicifera].

OBJECTIVE: To study the chemical constitutes of Acantophora spicifera. METHOD: Compounds were isolated by normal phase silica gel and Sephadex LH-20 gel column chromatography, and reverse-phase HPLC, as well as recrystallization. Their structures were elucidated by spectroscopic methods. RESULT: Seven compounds were isolated from A. spicifera and their structures were identified as aplysin (1), loloilide (2), (R)-(-)-dehydrovomifoliol (3), uracil (4), thymine (5), 1-methoxy-4-(1-propenyl) benzene (6). CONCLUSION: The compounds were obtained from this genus for the first time. Compound 6 was firstly obtained from marine organisms.

Effect of ethanol extract of alga Laurencia supplementation on DNA oxidation and alkylation damage in mice.

Laurencia terpenoid extract (LET) had been extracted from the red alga Laurencia tristicha. The study is to investigate the effects of LET supplementation on DNA oxidation and alkylation damages in mice. Forty healthy Kunming mice weighing between 18g and 25g were randomly assigned into 4 groups, each consisting of ten animals. The mice were orally intubated respectively for 60 days with the designed concentrations of LET (25, 50,100mg/ kg b.w.) for three exposed groups and salad oil (0.2 ml) for the blank group. Food and water were free for the animals. Mice in the blank and exposed groups were sacrificed after the last treatment and the blood of each animal was quickly taken for further experiments. The spontaneous and oxidized DNA damages of peripheral lymphocytes induced by H2O2 were analysed by SCGE. O6-Methy-guanine (O6-MeG) was measured by high performance capillary zone electrophoresis. There was no significantly difference in DNA spontaneous damage on peripheral lymphocytes of all the mice. The oxidative DNA damage in the 50 mg/Kg body weight supplement group are 286AU with the oxidation of 10 micromol/L H2O2, significantly lower than the blank group 332AU (p<0.05). The contents of O6-MeG in plasma in the 50 mg/kg b.w. and 100mg/kg b.w. supplement group were 1.50 micromol/L and 1.88 micromol/L, significantly lower than that of the blank group, which was 2.89 micromol/L(p<0.05). The results from the present study indicated that the LET were rich in terpenoids and safety to be taken orally and it could improve antioxidative and decrease DNA damage effectively.

[Studies on chemical constituents of Laurencia tristicha ( II )].

OBJECTIVE: To search for chemical constituents with structural diversity from Laurencia tristicha to supply for biological assay. METHOD: Compounds were isolated by means of column chromatography over normal phase silica gel and Sephadex LH-20, recrystallization and HPLC. Structures were identified by spectroscopic methods including 1D NMR, IR and MS. Cytotoxicities of the purified compounds were evaluated by MTT method. RESULT: Seven compounds were isolated from L. tristicha. Their structures were elucidated as cholesterol (1), cholesta- 5-en-3beta, 7alpha-diol (2), beta-stigmasterol (3), phytol (4), zeaxanthin (5), 4 -hydroxybenzaldehyde (6), indolyl-3-carbaldehyde (7). In the cytotoxic assay compound 2 was active against human cancer cell lines HCT-8, Bel-7402, BGc-823, A549 and HELA with IC50 values of 1.90, 2.02, 1.99, 6.52 and 1.20 microg x mL(-1), respectively. Compound 4 showed cytotoxicity against HCT-8 and HELA with IC50 value of 3.51 and 2.04 microg x mL(-1), and other compounds were inactive ( IC50 > 10 microg x mL(-1)). CONCLUSION: Compounds 1-7 were isolated from L. tristicha for the first time. In additon, compounds 2 and 4 were cytotoxic against several human cancer cell lines.

[Chemical constituents from red alga Corallina pilulifera].

OBJECTIVE: To investigate the chemical constituents of red alga Corallina pilulifera. METHOD: Compounds were isolated by normal phase silica gel and Sephadex LH - 20 gel column chromatography, reverse phase HPLC and recrystallization. Their structures were elucidated by spectroscopic methods including MS, 1H-NMR, 13C-NMR, HSQC, HMBC. Cytotoxicity of the compounds was screened by using standard MTT method. RESULT: Seven compounds were isolated from red alga C. pilulifera, their structures were identified as (E) -phytol epoxide (1), phytenal (2), phytol (3), dehydrovomifoliol (4), loliolide (5), 3beta-hydroxy-5alpha, 6alpha-epoxy-7-megastigmene-9-one (6), 4-hydroxybenzaldehyde (7). CONCLUSION: All of the compounds were obtained from this species for the first time. These compounds were inactive (IC50 > 10 microg x mL(-1)) in the MTT assay.

[Studies on chemical constitutes of green alga Chaetomorpha basiretorsa and their bioactivity].

OBJECTIVE: To study the chemical constituents of Chaetomorpha basiretorsa and screen for bioactive leading compounds. METHOD: Compounds were isolated by normal phase silica gel and Sephadex LH-20 gel column chromatography, reverse phase MPLC and reverse phase HPLC. Their structures were elucidated by spectroscopic methods including MS, IR and 1D, 2D NMR. Cytotoxicity of the compounds was screened by using standard MTT method. The purified compounds' inhibition against proliferation of dog vascular smooth muscle cells was also screened by MTT assay. RESULT: Five compounds were isolated from C. basiretorsa and their structures were identified as euphol (I), loloilide (II), 4-cumylphenol (III), zeaxanthin (IV) and lactucaxanthin (V). CONCLUSION: All these compounds were obtained from this genus for the first time. Compound (III), 4-cumylphenol, was a new nature product. All compounds were inactive (IC50 > 10 microg x mL(-1)) in cytotoxicity screening. In inhibition against proliferation of dog vascular smooth muscle cells test, the cell survival ratio to compound I was (0.32 +/- 0.056)% which indicate its potential anti-atherosclerotic bioactivity.

[Chemical constituents from marine alga Chaetomorpha basiretorsa].

OBJECTIVE: To investigate the chemical constituents of marine alga Chaetomorpha basiretorsa. METHOD: Compounds were isolated by normal phase silica gel and Sephadex LH-20 gel colum chromatography, reverse phase MPLC, reverse phase HPLC and recrystallization. Their structures were elucidated by spectroscopic methods including MS, IR, NMR, and X-ray crystalography. Cytotoxicity of the compounds were screened by using standard MTT method. RESULT: Nine compounds were isolated from C. basiretorsa and their structures were identified as N-phenyl-2-naphthalenamine( I ), dibutyl phthalate( II ), diisobutyl phthalate( III ), 1-phenyl-ethane-1, 2-diol( IV ), 2-hydrox-gamma-benzaldehyde( V ), diethyleneglycol monobenzoate( VI ), uracil( VII ), thymine( VIII ) and thymidine( IX ). CONCLUSION: All these compounds were obtained from this genus for the first time, N-phenyl-2-naphthalenamine and diethyleneglycol monobenzoate were first reported from the marine organisms. Compound I and VII showed moderate activity against KB cell(IC50 10.15 microg x mL(-1) for I and 3.79 microg x mL(-1) for VII ) and MCF-7 cell(IC50 3.24 microg x mL(-1) for VII).