Species Da cam was identified as being Hedyotis capitellata Wall. Ex G.Don var. molis Piere ex Pit. It is used as a drug in traditional medicine. Primary results on our studies of Da cam have been presented that: the of Da cam contained alkaloid, saponin, iridoid, tanin. We have extracted and isolated from the leaves caulis of Da cam Sapogenin KLD3 and determinated it was Olanaolic acid
chemistry ; Hedyotis ; Pharmaceutical Preparations

OBJECTIVETo investigate the chemical constituents from Hedyotis diffusa.

METHODThe compounds were isolated and purified by various chromatographic techniques and identified by their physicochemical properties and spectral data.

RESULTEight compounds had been reported in last paper, and this time eight more compounds were isolated and identified as 6-hydroxystigmasta-4,22-dien-3-one (1), 3-hydroxystigmasta-4,22-dien-7-one (2), 2-hydroxy-3-methylanthraquinone (3), 2,6-dihydroxy-3-methyl-4-methoxyanthraquinone (4), iso-scutellarein (5), isoetin (6), aesculetin (7), gypsogenic acid (8).

CONCLUSIONCompounds 1-3, 5-8 were obtained from the genus Hedyotis for the first time.

Hedyotis ; chemistry ; Organic Chemicals ; analysis ; isolation & purification

The hedyotis capitellata Wall ex G.Don var. molis Piere ex Pit, called Da Cam, is used in traditional medicine. The biological experiments have revealed: concentrated extracts by boiling water and alcohol, the solutions of total alkaloids of Da Cam had strong antibacterial activity on positive gram strains and candida albicans
Anti-Bacterial Agents ; Hedyotis ; Pharmaceutical Preparations

OBJECTIVEA new method for simultaneous determination of four methyl-3, 4-dihydroxybenzoate ( I ), P-coumaric acid (II), ferulaic acid (III) and E-6-O-P-coumaroyl scandoside methyl ester (IV) in Hedyotis diffusa oral solution by reversed-phase HPLC was developed.

METHODThe separation was performed on a Diamonsil C18 column (4.6 mm x 250 mm, 5 microm) with gradient elution. A-acetonitrile, B-methonal-water-glacial acetic acid (5: 95: 0.25), 0-20 min, 1% -16% A; 2042 min, 16% A; 42-46 min, 16%-20%A; 46-65 min, 20% A. The UV detection was set at 265 nm; flow rate 1.0 mL x min(-1).

RESULTThere was good linearity between the peak area and concentration at the ranges of 2.1-105 (r = 0.999 8), 3.5-175 (r = 0.999 8), 1.72-86 (r = 0.999 9), 4.0-200 mg x L(-1) (r = 1.000 0) for I, II, III and IV respectively. The average recoveries of I, II, III and IV were 99.9%, 97.9%, 98.6% and 98.1%.

CONCLUSIONThe method is rapid, simple and accurate, and it can be used for the evaluation of H. diffusa oral solution.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Hedyotis ; chemistry ; Reproducibility of Results

OBJECTIVETo develop an HPLC method for determination of scandoside methyl ester in Hedyotis chrysotricha.

METHODThe determination was carried out on an HC-C18 column elnted with acetonitrile-water (7:93) as mobile phase, and the detection wavelength was set at 238 nm.

RESULTThere is a good linearity in the range 22.08-552 mg L(-1) of scandoside methyl ester and the average recovery is 97.7% (n = 6), RSD 0.72%.

CONCLUSIONThis method is convenient, quick, and is applicable to the quality control of H. chrysotricha.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Esters ; analysis ; Hedyotis ; chemistry

OBJECTIVE: To investigate the therapeutic effects of Hedyotis diffusa Willd.on type Ⅱ collagen-induced rheumatoid arthritis in rats. METHODS: According to the random number table, 60 SD rats were divided into the normal control group (=10, normal saline) and model group (=50).The collagen-induced arthritis model was established with the injection of type Ⅱ collagen into the back in rats other than the normal group and evaluated by arthritis score, then the model rats were randomly divided into model group (normal saline), tripterygium wilfordii polyglycoside (GTW) 6 mg/kg group (daily dose:0.4 mg/kg), HD 3, 6, 12 g/kg groups (daily dose:3, 6 and 12 g/kg, respectively), with 10 rats in each group. The rats were treated with corresponding agents by intragastric administration.The arthritis index and the pain threshold of all rats at different time points were observed and measured weekly.After treated by intragastric administration for 28 days, all rats were killed to measure the changes of serum cytokine levels including interleukin 1β (IL-lβ), tumor necrosis factor a (TNF-a), prostaglandin (PGE), receptor activator for nuclear factor-kappa B ligand (RANKL) and osteoprotegerin (OPG). RESULTS: Compared with the control group, the arthritis index and the serum levels of IL-lβ, TNF-a, PGE, RANKL, OPG and RANKL/OPG of the model group were increased significantly (<0.05), the pain threshold of the model group was decreased significantly (<0.05); compared with the model group, the arthritis index and the serum levels of IL-lβ, TNF-a, PGE, RANKL, OPG and RANKL/OPG of the GTW group, HD low-dose, medium-dose, high dose groups were decreased significantly (<0.05), the pain threshold of the model group was increased significantly (<0.05). CONCLUSIONS Hedyotis diffusa Willd.can significantly reduce arthritis index and increase pain threshold, reduce the level of IL-lβ, TNF-a, PGE, RANKL, OPG, and RANKL/OPG, then can prevent CIA effectively.
Animals ; Arthritis, Experimental ; Arthritis, Rheumatoid ; Collagen Type II ; Hedyotis ; RANK Ligand ; Rats ; Rats, Sprague-Dawley

This study aimed to investigate the chemical constituents in the water extract of the whole herb of Hedyotis scandens by silica gel, ODS, and MCI column chromatographies together with preparative high-performance liquid chromatography(HPLC). The structures of isolated constituents were identified by NMR, HR-ESI-MS, etc. Thirteen compounds were isolated and identified as methyl 4-benzoyloxy-3-methoxybenzeneacetate(1), 4-benzoyloxy-3-methoxybenzeneacetic acid(2), 3-(4-hydroxy-3-methoxyphenyl)-propanoic acid(3), salicylic acid(4), 3-hydroxy-4-methoxypyridine(5), syringic acid(6), hydroxycinnamic acid(7),(R)-6-methyl-4,6-bis(4-methylpent-3-enyl)cyclohexa-1,3-dienecarbaldehyde(8), 1,2-bis(4-hydroxy-3-methoxyphenyl)-1,3-propanediol(9), 1H-indole-3-carboxaldehyde(10), isoscopoletin(11), syringaresinol(12), and pinoresinol(13). Among them, compounds 1 and 2 were new phenolic acid compounds, compounds 3-5, 8-11, and 13 were isolated from this genus for the first time, and compounds 6, 7, and 12 were obtained from H. scandens for the first time. The activity test showed that compounds 1 and 10 had a certain inhibitory effect on Mycobacterium smegmatis, with MIC_(50) values of 58.5 and 33.3 μg·mL~(-1), respectively.
Hedyotis/chemistry* ; Drugs, Chinese Herbal/chemistry* ; Magnetic Resonance Spectroscopy ; Salicylic Acid

Apoptosis ; Autophagy ; Endoplasmic Reticulum ; Endoplasmic Reticulum Chaperone BiP ; Endoplasmic Reticulum Stress ; Hedyotis ; Humans ; Laryngeal Neoplasms/drug therapy* ; Polysaccharides

OBJECTIVETo analyze p-coumaril acid, trans-6-O-p-coumaroyl scandoside methyl ester and its metabolites in rat plasma after intragastric administration of exocarpium Diffusa effective extracts.

METHODRat blood samples were collected 1.0 h after oral administration of 0.4 g x kg(-1) exocarpium Diffusa effective extracts, and then were analyzed by using HPLC-Q-TOF-MS.

RESULTIn rat plasma, only one metabolite was detected. The structure was identified by reference substance to be p-coumaril acid.

CONCLUSIONThe methyl glucoside metabolite in rat from the main component parts of trans-6-O-p-coumaroyl scandoside methyl ester droppings of vines in Diffusa effective extracts is p-coumaril acid. This experiment provides a theortical basis for studying chemical compositions and pharmacodynamic action of Diffusa.

Animals ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; metabolism ; Hedyotis ; chemistry ; Male ; Mass Spectrometry ; methods ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo explore the inhibition of Hedyotis diffusa Willd Injection (HDI) on the proliferation of RPMI 8226 cells and its mechanisms.

METHODSThe inhibition of HDI on the proliferation of RPMI 8226 cells was detected by MTT and the drug concentrations for further researches were screened out. The apoptosis rate was detected using Annexin V-PI of flow cytometry. The cell cycle distribution was detected by PI. The expressions of adhesion molecule FITC-CD44 and PE-CD49d were detected. The IL-6 and VEGF concentrations of cell supernatants were tested by ELISA. The mRNA expressions of Bax, Bcl-2, Caspase-3, Survivin, IL-6, and VEGF were detected by RT-PCR.

RESULTSHDI could inhibit the proliferation of RPMI 8226 cells. Meanwhile, it induced their early apoptosis, arresting them at G1 phase in a concentration-dependent manner. The VEGF concentrations were down-regulated after acted by 0, 20, 40, and 60 microL/mL HDI in a dose-dependent manner (P< 0.01). The IL-6 content increased (P<0.01). The expressions of CD44 and CD49d were up-regulated in a concentration-dependent manner. After acted by 40 microL/mL HDI, the Survivin mRNA level was significantly downregulated (P<0.01), the mRNA levels of Bcl-2, IL-6, and VEGF were significantly up-regulated (P<0.01), but the up-regulation of Bax and Caspase-3 mRNA levels were not so obvious (P>0.05).

CONCLUSIONSHDI could inhibit the proliferation of RPMI 8226 cells. Its mechanisms might be correlated with early apoptosis induction, G1 phase arresting, VEGF secretion lowering, and Survivin mRNA transcription level down-regulating.

Apoptosis ; drug effects ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Hedyotis ; Humans ; Inhibitor of Apoptosis Proteins ; metabolism ; Interleukin-6 ; metabolism ; Vascular Endothelial Growth Factor A ; metabolism