Ardipusilloside-I stimulates gastrointestinal motility and phosphorylation of smooth muscle myosin by myosin light chain kinase

Ardipusilloside-I is a natural triterpenoid saponin, which was isolated from Ardisia pusilla A. DC. The aim of the study was to evaluate the stimulation of ardipusilloside-I on gastrointestinal motility in vitro and in vivo. The experiment of smooth muscle contraction directly monitored the contractions of the isolated jejunal segment (IJS) in different contractile states, and the effects of ardipusilloside-I on myosin were measured in the presence of Ca²⁺-calmodulin using the activities of 20 kDa myosin light chain (MLC₂₀) phosphorylation and myosin Mg²⁺-ATPase. The effects of ardipusilloside-I on gastro emptying and intestinal transit in constipation-predominant rats were observed, and the MLCK expression in jejuna of constipated rats was determined by western blot. The results showed that, ardipusilloside-I increased the contractility of IJS in a dose-dependent manner and reversed the low contractile state (LCS) of IJS induced by low Ca²⁺, adrenaline, and atropine respectively. There were synergistic effects on contractivity of IJS between ardipusilloside-I and ACh, high Ca²⁺, and histamine, respectively. Ardipusilloside-I could stimulate the phosphorylation of MLC₂₀ and Mg²⁺-ATPase activities of Ca²⁺- dependent phosphorylated myosin. Ardipusilloside-I also stimulated the gastric emptying and intestinal transit in normal and constipated rats in vivo, respectively, and increased the MLCK expression in the jejuna of constipation-predominant rats. Briefly, the findings demonstrated that ardipusilloside-I could effectively excite gastrointestinal motility in vitro and in vivo.

Distinct effect of Wansheng Huafeng Dan containing ardisia crenata on renal transporters, mercury accumulation and Kim-1 expression from mercuric chloride / 中国中药杂志

To study the effect of Wansheng Huafeng Dan (WSHFD) and mercuric chloride on renal mercury (Hg) extraction transporters (Oat1, Oct2), renal mercury excretion transporters (Mrp4, Mate2K), renal mercury accumulation and kidney injury molecule-1 (Kim-1). The ancient prescription of WSHFD containing 10-fold Hg caused much lower renal mercury accumulation and renal toxicity than HgCl2 in rats, with less effect on renal transporters than HgCl2. The above indicators had no significant difference in WSHFDO, WSHFD2 and WSHFD3 groups, indicating no effect of WSHFD with reduced or no cinnabar.

Study on inhibitory effect of triterpenoid saponin from Ardisia japonica TSP02 on proliferation and metastasis of human hepatocellular carcinoma cells and its mechanism / 中国中药杂志

<p><b>OBJECTIVE</b>To study the effect of TSP02, a triterpenoid saponin compound from Ardisia japonica, on proliferation and metastasis of in vitro induced human hepatoma HepG2 cells and its molecular mechanism.</p><p><b>METHOD</b>MTT assay was performed to detect the inhibitory effect of TSP02 of different concentrations on proliferation of human hepatoma HepG2 and normal human hepatic cell HL-7702 cells. The changes in cell cycle and apoptotic of processed HepG2 and HL-7702 cells were detected by using flow cytometry. The effect of TSP02 on expression levels of CDK1, 2, 4, apoptosis-related protein Caspase-8, metastasis-related TGF-beta 1 and E-cadherin was measured by western blot. Wound-healing assay and transwell assay were performed to detect the changes in the metastasis of TSPO2-processed HepG2.</p><p><b>RESULT</b>TSP02 significantly inhibited the proliferation of HepG2 cells, with notable time dependence and concentration dependence, but without remarkable effect on normal human liver HL-7702 cells. Compared with the control group, TSP02 processed for 24 h could eliminate HepG2 cells in S stage, significantly increase the cell apoptotic rate. Furthermore, TSP02 was capable of down-regulating the expression of multiple CDK1, 2, 4, and TGF-beta1, and up-regulating the expression and activity of Caspase-8, without significant effect on cycle and apoptotic rate of normal human liver HL-7702 cells. Additionally, TSP02 caused metastasis and invasiveness HepG2 cells, while down-regulating liver cancer invasiveness-related TGF-beta 1 and E-cadherin.</p><p><b>CONCLUSION</b>TSP02 selectively promotes apoptosis of liver cancer cell HepG2, and inhibits its metastasis and invasiveness. TSP02's in vitro antineoplastic activity is related to the changes in cycle and apoptosis proteins, and the regulation in the expression of invasiveness-related TGF-beta 1 and E-cadherin.</p>

Angio-suppressive triterpenoids from Ardisia cf. elliptica (subgenus Tinus) on duck (Anas platyrynchos L.) chorioallantoic membrane / 中国天然药物

The dichloromethane extract of the air-dried leaves of Ardisia cf. elliptica (subgenus Tinus) afforded a mixture of bauerenol (1a), α-amyrin (1b) and β-amyrin (1c). Their structures were identified by NMR spectroscopy. Mixtures of the triterpenes (1a-1c) at ratios of 2 : 2 : 1, 2 : 2 : 3 and 1 : 1 : 1 were tested for their angio-suppressive effects on duck chorioallantoic membrane (CAM). All three ratios were found to be effective in restricting inter-capillary length, while 1a-1c (2 : 2 : 1) was most effective in reducing branch point density with 100% CAM viability and embryo survivability, suggesting a high impact angio-suppressive potential of 1a-1c (2 : 2 : 1).

Chemical constituents of Ardisia punctata / 中国中药杂志

<p><b>OBJECTIVE</b>To study chemical constituents of Ardisia punctata,in order to find pioneering compounds.</p><p><b>METHOD</b>95% ethanol extracts of A. punctata was separated and purified by using normal phase silica gel column chromatographies, Sephadex LH-20 gel column chromatography and high-pressure preparative HPLC,and their structures were identified by such spectroscopic techniques as NMR and MS.</p><p><b>RESULT</b>Eight compounds were separated from 95% ethanol extract of A. punctata and identified as 6-methoxy-8-hydroxy-benzoic acid butylester-5-O-beta-D-glucoside (1), aridisiacrispin B (2), ardisicrenoside A (3), dibutyl phthalate (4), bergenin (5), quercetin-3-O-alpha-L-rhamnoside (6),3-methoxy-4-acetoxy-6-tridecyl-phenol(7) and belamcandaquinone C(8).</p><p><b>CONCLUSION</b>Compound 1 was a new compound, and compounds 4 and 6 were separated from this plant for the first time.</p>

Effect of coenzyme Q10 and Ardisia japonica Blume on plasma and liver lipids, platelet aggregation, and erythrocyte Na efflux channels in simvastatin-treated guinea pigs

Forty guinea pigs were divided into four groups and fed 0.04% cholesterol based control diet, plus 0.05% simvastatin, and statin plus 0.1% CoQ10 or 10% Ardisia Japonica Blume (AJB) leave powder for 4 weeks. Plasma total cholesterol levels decreased significantly in all groups fed the statin-containing diet compared with that in guinea pigs fed the control diet (P < 0.01). Plasma and liver triglycerides decreased significantly in the statin plus CoQ10 group compared with those in the control (both P < 0.05). Maximum platelet aggregation was significantly higher in the statin plus CoQ10 group than that in the other groups (P < 0.05). Na-K ATPase activity increased in the statin group and decreased in the statin plus CoQ10 group (P < 0.01). Na-K co-transport and Na passive transport decreased significantly in the control group compared with those in the other groups (both P < 0.05). Intracellular Na was highest in the statin group and lowest in the statin plus CoQ10 group and was correlated with Na-K ATPase activity. Thiobarbituric acid reactive substance production in platelet-rich plasma and liver tended to decrease in the statin plus CoQ10 group compared with those in the other groups. Plasma glutamic-pyruvic transaminase and glutamic-oxaloacetic transaminase increased significantly in the statin group compared with those in the control (P < 0.05). These result suggest that antioxidant rich AJB did not have positive effects on cardiovascular disease parameters. The statin plus CoQ10 seemed to decrease cholesterol more efficiently than that of statin alone.

Studies on anti-tumor metastatic constituents from Ardisia Crenata / 中国中药杂志

<p><b>OBJECTIVE</b>To study the anti-tumor metastatic constituents from Ardisia Crenata.</p><p><b>METHOD</b>Chemical constituents were isolated and purified by repeated column chromatography( silica gel, Toyopearl HW40C and preparative HPLC). Their structures were elucidated on the basis of spectral data analysis. The anti-tumor metastasis assay was applied to evaluate the isolated compounds of their activities.</p><p><b>RESULT</b>Nine compounds(1-9) were isolated and their structures were identified by comparison of their spectral data with literature values as follows: 5-hydroxymethyl-2-furalclehyde(1), ethyl-beta-D-fructopyranoside(2), syringic acid(3), n-butyl-beta-D-fructofuranoside(4), n-butyl-alpha-D-fructofuranoside(5), methyl-alpha-D-fructofuranoside(6), (+)-bergenin(7), ardisiacrispins B(8), asperuloside acid(9). The isolated compounds(1-9) showed positive anti-tumor metastatic activities, and compounds 1, 5, and 8 showed significant anti-tumor metastatic activities. At the concentration of 0.8 mg x L(-1), compound 5 revealed the value of metastatic inhibition ratio on MDA-MB-231 was 93.8%.</p><p><b>CONCLUSION</b>Compounds 2-6 and 9 were isolated from this plant for the first time. compounds 1, 5 and 8 showed significant anti-tumor metastatic activities.</p>

Study on chemical constituents of rhizome of Ardisia gigantifolia / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the dried rhizome of Ardisia gigantifolia.</p><p><b>METHOD</b>The 60% ethanol extract was extracted with EtOAc, and then separated and purified by column chromatography using silica gel and preparative HPLC. Their structures were identified on the basis of spectral analysis and physico-chemical properties.</p><p><b>RESULT</b>Nine compounds were isolated and identified as 11-O-galloylbergenin (1), 11-O-syringylbergenin (2), 11-O-protocatechuoylbergenin (3), 4-O-galloylbergenin (4), 11 -O-vanilloylbergenin (5), (-) -epicatechin-3-gallate (6), stigmasterol-3-O-beta-D-glucopyranoside (7), (-) -4'-hydroxy-3-methoxyphenyl-beta-D-[6-O-(4"-hydroxy-3", 5"-dimethoxybenzoyl)] -glucopyranoside (8), and beta-sitosterol (9).</p><p><b>CONCLUSION</b>Compounds 3, 4 and 7 were isolsted from the genus Ardisia for the first time, while compounds 1, 2, 5 and 6 were isolated from this plant for the first time.</p>

Tissue culture and plant regeneration of Ardisia crenata / 中国中药杂志

<p><b>OBJECTIVE</b>Our research studied the fast-breeding technology of Ardisia crenata sims by using tissue culture and provided the scientific foundation for industry production.</p><p><b>METHOD</b>The effects of axillary buds and plant regeneration of different basic medium, hormones and additives on induction and multiplication were studied.</p><p><b>RESULT</b>The best culture medium for the induction of axillary buds, which took the stems of A. crenate were as explants, was MS + 6-BA 0.5 mg x L(-1) + NAA 0.1 mg x L(-1), and the best medium for multiplication was MS + 6-BA 2.0 mg x L(-1) + NAA 0.1 mg x L(-1) + KT 0.5 mg x L(-1), the best medium for roots generation was 1/2MS + IBA 0.2 mg x L(-1). We also found that the roots'generation, roots rate and mean number of roots can be promoted by adding 0.2% Ac, and the most suitable ground substance was river sand-perlite-vermiculite (1:1:1) or perlite-vermiculite (1:1). With axillary buds and plant regeneration methode, more than 80% A. crenata sims could be regenerated integratedly.</p><p><b>CONCLUSION</b>A. crenata sims can be regenerated integratedly and breeded fast by using axillary bud proliferation technology.</p>

Two novel compounds from Ardisia punctata Lindl / 药学学报

To study the chemical constituents of Ardisia punctata, compounds were isolated with a combination of multi-chromatography. Their structures were determined on the basis of spectral analysis and comparison to those of the known compounds. A 1,4-benzoquinone derivative and a alkylphenol were isolated from the petroleum ether extract of the roots of Ardisia punctata. Their structures were elucidated as 2-tridecyl-3-[(2-tridecyl-4-acetoxy-6-methoxy)-phenoxyl] -6-methoxy-1,4-benzoquinone (1) and 2-methoxy-4-hydroxy-6-tridecyl-phenyl acetate (2). The two compounds are both new.

Chemical constituents from roots of Ardisia punctata / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents from the roots of Ardisia punctata.</p><p><b>METHOD</b>Compounds were isolated by chromatographic techniques on silica gel and Rp-HPLC column. Their structures were elucidated by chemical and spectroscopic methods.</p><p><b>RESULT</b>Twelve compounds were identified as 3-hydroxy-5-tridecyl-methyl phenyl ether (1), 5-pentadecyl-1, 3-benzenediol (2), 2-methoxy-6-tridecyl-1, 4-benzoquinone (3), 2-methoxy-6-pentadecyl-1, 4-benzoquinone (4), glutinol (5), ardisicrenoside A (6), ardisiacrispin B (7), 24-ethyl-5a-cholesta-7, 22(E)-dien-3-one (8), 24-ethyl-5alpha-cholesta-7, 22(E)-dien-3beta-ol (9), daucosterol (10), vanillin acid (11), tetratriacontanoic acid (12).</p><p><b>CONCLUSION</b>All the compounds were obtained from this plant for the first time.</p>

Three new belamcandaquinones from Ardisia punctata / 药学学报

<p><b>AIM</b>To study the chemical constituents of Ardisia punctata.</p><p><b>METHODS</b>Compounds were separated with a combination of multi-chromatography. Their chemical structures were determined on the basis of spectral analysis and single crystal X-ray diffraction.</p><p><b>RESULTS</b>Three compounds were isolated from chloroform extract of the roots of Ardisia punctata. Their structures were elucidated as 2-tridecyl-3-[(2-tridecyl-3-acetoxy-4-methoxy-6-hydroxy) -phenyl]-6-methoxy-1, 4-benzoquinone (1), 2-tridecyl-3-[(2-tridecyl-4,6-dihydroxy) -phenyl]-6-methoxy-1,4-benzoquinone (2) and 2-tridecyl-3-[(2-pentadecyl-4,6-dihydroxyl) -phenyl]-6-methoxy-,4-benzoquinone (3).</p><p><b>CONCLUSION</b>The three compounds are new 1,4-benzoquinone derivatives.</p>