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.
Animals ; Ardisia ; Atropine ; Blotting, Western ; Epinephrine ; Gastric Emptying ; Gastrointestinal Motility* ; Histamine ; In Vitro Techniques ; Muscle, Smooth* ; Myosin Light Chains* ; Myosin-Light-Chain Kinase* ; Myosins* ; Phosphorylation* ; Rats ; Saponins

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.
Animals ; Ardisia ; chemistry ; Biological Transport ; drug effects ; Cell Adhesion Molecules ; genetics ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; adverse effects ; Gene Expression ; drug effects ; Kidney ; drug effects ; metabolism ; Male ; Mercuric Chloride ; metabolism ; Multidrug Resistance-Associated Proteins ; genetics ; metabolism ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo 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.

METHODMTT 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.

RESULTTSP02 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.

CONCLUSIONTSP02 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.

Antineoplastic Agents ; chemistry ; isolation & purification ; pharmacology ; Apoptosis ; drug effects ; Ardisia ; chemistry ; Carcinoma, Hepatocellular ; pathology ; Caspase 8 ; metabolism ; Cell Cycle ; drug effects ; Cell Proliferation ; drug effects ; Enzyme Activation ; drug effects ; Hep G2 Cells ; Humans ; Liver Neoplasms ; pathology ; Neoplasm Metastasis ; Saponins ; chemistry ; isolation & purification ; pharmacology ; Triterpenes ; chemistry ; Up-Regulation ; drug effects

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).
Angiogenesis Inhibitors ; chemistry ; pharmacology ; Animals ; Ardisia ; chemistry ; Chorioallantoic Membrane ; blood supply ; drug effects ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Ducks ; Plant Leaves ; chemistry ; Triterpenes ; chemistry ; pharmacology

OBJECTIVETo study chemical constituents of Ardisia punctata,in order to find pioneering compounds.

METHOD95% 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.

RESULTEight 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).

CONCLUSIONCompound 1 was a new compound, and compounds 4 and 6 were separated from this plant for the first time.

Ardisia ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure

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.
Adenosine Triphosphatases ; Alanine Transaminase ; Animals ; Ardisia ; Aspartate Aminotransferases ; Blood Platelets ; Cardiovascular Diseases ; Cholesterol ; Diet ; Erythrocytes ; Guinea ; Guinea Pigs ; Hydroxymethylglutaryl-CoA Reductase Inhibitors ; Liver ; Plasma ; Platelet Aggregation ; Platelet-Rich Plasma ; Simvastatin ; Thiobarbiturates ; Triglycerides ; Ubiquinone

OBJECTIVETo study the anti-tumor metastatic constituents from Ardisia Crenata.

METHODChemical 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.

RESULTNine 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%.

CONCLUSIONCompounds 2-6 and 9 were isolated from this plant for the first time. compounds 1, 5 and 8 showed significant anti-tumor metastatic activities.

Antineoplastic Agents ; pharmacology ; therapeutic use ; Ardisia ; chemistry ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Humans ; Neoplasm Metastasis ; drug therapy

OBJECTIVETo study the chemical constituents of the dried rhizome of Ardisia gigantifolia.

METHODThe 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.

RESULTNine 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).

CONCLUSIONCompounds 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.

Ardisia ; chemistry ; Rhizome ; chemistry

OBJECTIVEOur research studied the fast-breeding technology of Ardisia crenata sims by using tissue culture and provided the scientific foundation for industry production.

METHODThe effects of axillary buds and plant regeneration of different basic medium, hormones and additives on induction and multiplication were studied.

RESULTThe 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.

CONCLUSIONA. crenata sims can be regenerated integratedly and breeded fast by using axillary bud proliferation technology.

Ardisia ; growth & development ; physiology ; Culture Media ; metabolism ; Regeneration ; Tissue Culture Techniques ; methods

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.
Ardisia ; chemistry ; Benzoquinones ; chemistry ; isolation & purification ; Molecular Structure ; Phenylacetates ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry