Chemical constituents from whole herb of Hedyotis scandens / 中国中药杂志

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.

Effect of "Hedyotis Diffusae Herba-Smilacis Glabrae Rhizoma" in treatment of lung adenocarcinoma based on network pharmacology / 中国中药杂志

To explore the mechanism of Hedyotis Diffusae Herba-Smilacis Glabrae Rhizoma(HDH-SGR) in treating lung adenocarcinoma based on big data bioinformatics combined with network pharmacology analysis and molecular docking technology. The chemical components and potential therapeutic targets of HDH-SGR were obtained from Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP). Lung adenocarcinoma-related genes were obtained from The Cancer Genome Atlas(TCGA), Therapeutic Target Database(TTD), Pharmacogenetics and Pharmacogenomics Knowledge Base(PharmGKB), Online Mendelian Inheritance in Man(OMIM), DrugBank, and GeneCards. "Drug component-target" network was constructed using Cytoscape to screen out key compounds. STRING was used to build protein-protein interaction(PPI) network and core targets were screened out by Cytoscape-CytoNCA topology analysis. Gene Ontology(GO) and Kyoto Encyclopedia of Genes and Genomes(KEGG) analyses of target genes were performed by R-clusterProfiler. Finally, key compounds were docked to core target genes using AutoDock. The results showed that 22 active compounds and 499 potential therapeutic targets were obtained from HDH-SGR. A total of 14 332 lung adenocarcinoma-related targets were screened out through six data platforms, including 182 common targets. Fifteen core targets were screened out from the PPI network. GO and KEGG analyses revealed significant enrichment of relevant target genes in various biological processes, cellular functions(e.g., response to lipopolysaccharide, nuclear receptor activity, and ligand-activated transcription factor activity) and close relationship between target genes and non-small cell lung cancer signaling pathways. Based on the results of molecular docking validation, diosgenin, quercetin, naringenin, taxifolin, 2-methoxy-3-methyl-9,10-anthraquinone, stigmasterol, and β-sitosterol were able to bind tightly to the core targets. HDH-SGR can intervene in lung adenocarcinoma through multiple targets and signaling pathways, such as non-small cell lung cancer signaling pathways. The binding of active components in Chinese medicine to key targets is presumedly one of the mechanisms that produce therapeutic effects.

Therapeutic effects of Hedyotis diffusa Willd. on type II collagen-induced rheumatoid arthritis in rats / 中国应用生理学杂志

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.

Chemical constituents from stems of Hedyotis hedyotidea and their immunosuppressive activity / 中国中药杂志

Hedyotis hedyotidea has been traditionally used for the treatment of arthritis, cold, cough, gastro-enteritis, headstroke, etc. But few studies have screened the active compounds from extracts of H. hedyotidea. In this study, the structure of the chemical constituents from stems of H. hedyotidea were determined and the immunosuppressive activity of the compounds was evaluated. The compounds were separated and purified with silica gel, gel column chromatographies and preparative HPLC, and their structures were identified by spectral methods such as MS and NMR. Eleven compounds were obtained and identified as(6S,9S) -vomifoliol (1), betulonic acid (2), betulinic acid (3), betulin(4), 3-epi-betulinic acid (5), ursolic acid (6), β-sitosterol (7), stigmast-4-en-3-one (8), 7β-hydroxysitosterol (9), (3β,7β) -7-methoxystigmast-5-en-3-ol (10) and morindacin (11). This is the first report of compounds 1, 2, 4, 8, 9, 10 and 11 from H. hedyotidea. Compounds 1, 2 and 8-11 were firstly isolated from the genus Hedyotis, and compounds 9 and 10 were isolated from the family Rubiaceae for the first time. The immunosuppressive activity of these compounds was tested using the lymphocyte transsormationtest. Compounds 4, 6 and 9 showed significant immunosuppressive activity.

Mechanism of apoptosis of nasopharyngeal carcinoma cells induced by polysaccharides extracts from Hedyotic diffusa / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To explore the proliferation inhibition and apoptosis of polysaccharides extracts from polysaccharides extracts from Hedyotic diffusa (PEHD) on Human Nasopharyngeal Carcinoma (NPC)cell line CNE2 cells in vitro.@*METHOD@#CNE2 cells treated with various concentrations of PEHD were detected by MTT assay at 24 h, 48 h, and 72 h. The apoptotic cells were analyzed by flow cytometry with Annexin V/PI staining. The expression levels of Bax, Bcl-2 and caspase-3 protein were examined by Western blotting method.@*RESULT@#The growth of CNE2 cells were suppressed after treatment with PEHD (P < 0.05), MTT assay showed that the highest cell inhibition rate reached to 76.5%, the inhibition in the doses from 2 to 6 mg/ml showed dose-and-time-dependent. The percent of apoptosis in 4 and 6 mg/ml PEHD treatment groups for 48 h were 31.32%, 46.28%, respectively, and significantly higher than that in control groups, 4.86% (P < 0.01). After the cells being treated with PEHD for 48 h, the expression of Bax and caspase-3 protein increased, and the expression of Bcl-2 protein decreased gradually.@*CONCLUSION@#PEHD could inhibited the growth of CNE2 cells and was dose-and-time-dependent, the mechanism may involve induction of cell apoptosis, which was associated with the activation of Bax and caspase-3 protein and the down-regulation of Bcl-2 protein expression.

Apoptosis of multiple myeloid cells induced by polysaccharides extracts from Hedyotis diffusa and its mechanism / 中华血液学杂志

<p><b>OBJECTIVE</b>To explore the proliferation inhibition and apoptosis effects of polysaccharides extracts from Hedyotis diffusa (PEHD) on multiple myeloma (MM) cell line RPMI 8226 cells in vitro, so as to provide experimental theory for the clinical application in the treatment of MM.</p><p><b>METHODS</b>MTT assay was used to examine the effects of PEHD on cell growth. The apoptotic cells were analyzed by flow cytometry with AnnexinⅤ/PI staining. Hoechst staining was used to observe the morphological changes of RPMI 8226 cell apoptosis. The expression levels of caspase-3,-8,-9, PARP, nucleoprotein NF-κB protein and other channel protein were assayed by Western blotting method.</p><p><b>RESULTS</b>The growth of RPMI 8226 cells were suppressed after treatment with PEHD, the highest inhibition rate reached to 92.3%, the results in the doses from 1 to 4 mg/ml showed a dose-and-time-dependent manner. The proportion of apoptotic cells in 1, 2 and 3 mg/ml PEHD treatment groups for 24 h were 22.52%, 62.31% and 69.94%, respectively, and significantly higher than that of control 8.93%. After treated with PEHD, apoptotic body appeared in RPMI 8226 cells nucleus and the number of apoptotic body increased in a dose-dependent manner. With the increasing of PEHD concentration, the expression of caspase-8,-9,-3 and PARP protein increased. The expression of Mcl-1, Bcl-xl, Bid and Bim protein decreased gradually, but the expression of Bax, Bak and Bad protein increased, and the expression of p-AKT protein (60 kDa) and NF-κB obviously decreased.</p><p><b>CONCLUSION</b>PEHD could inhibited the growth of RPMI 8226 cells and displayed a dose-and-time-dependent manner, its mechanism may involve cell apoptosis induction, which was associated with the activation of caspase-8, caspase-9, and caspase-3 protein and the down-regulation of p-AKT and NF-κB protein expression.</p>

Effects of Hedyotis diffusa Willd injection on the proliferation of RPMI 8226 cells / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To explore the inhibition of Hedyotis diffusa Willd Injection (HDI) on the proliferation of RPMI 8226 cells and its mechanisms.</p><p><b>METHODS</b>The 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.</p><p><b>RESULTS</b>HDI 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).</p><p><b>CONCLUSIONS</b>HDI 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.</p>

HPLC-TOF-MS analysis of metabolites of Diffusa effective extracts in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To 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.</p><p><b>METHOD</b>Rat 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.</p><p><b>RESULT</b>In rat plasma, only one metabolite was detected. The structure was identified by reference substance to be p-coumaril acid.</p><p><b>CONCLUSION</b>The 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.</p>

Effects of three Chinese herbal antidotes (Herba artemisiae annuae, Herba hedyotis diffusae and Rhizoma cimicifugae) and their different combinations on regulated on activation normal T cell expressed and secreated expression in MRL/lpr mice / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To explore the effects of three Chinese herbal antidotes, i.e. Herba Artemisiae annuae (A), Herba Hedyotis diffusae (H) and Rhizoma Cimicifugae (C), all were ingredients of Jiedu Quyu Ziyin Recipe, for adjusting the regulated on activation normal T cell expressed and secreated (RANTES), gene expression in serum and renal tissue of MRL/lpr mice.</p><p><b>METHODS</b>Fifty-four MRL/lpr mice were randomized into 9 groups, with 6 in each, and intragastrically infused with A, H, C, A+H, H+C, A+C, A+H+C (all in dosage-form of decoction), prednisone suspension and physiological saline, respectively for 12 weeks. RANTES expression in serum and renal tissue of animals were detected with ELISA and RT-PCR at the end of the study.</p><p><b>RESULTS</b>Levels of RANTES expression was significantly reduced in the prednisone treated group after treatment. Excepting no significant change being observed in the groups treated with A and C, the changes in the other groups were all milder than those in the group treated with A+H+C.</p><p><b>CONCLUSION</b>Chinese herbal antidotes A, H and C in combination can significantly inhibit the RANTES expression in serum and renal tissue of MRL/lpr mice.</p>

Chemical constituents from Hedyotis diffusa / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents from Hedyotis diffusa.</p><p><b>METHOD</b>The compounds were isolated and purified by various chromatographic techniques and identified by their physicochemical properties and spectral data.</p><p><b>RESULT</b>Eight 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).</p><p><b>CONCLUSION</b>Compounds 1-3, 5-8 were obtained from the genus Hedyotis for the first time.</p>

Determination of scandoside methyl ester in Hedyotis chrysotricha by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To develop an HPLC method for determination of scandoside methyl ester in Hedyotis chrysotricha.</p><p><b>METHOD</b>The 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.</p><p><b>RESULT</b>There 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%.</p><p><b>CONCLUSION</b>This method is convenient, quick, and is applicable to the quality control of H. chrysotricha.</p>

Chemical constituents from Hedyotis diffusa / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the chemical constituents from Hedyotis diffusa.</p><p><b>METHOD</b>The compounds were isolated and purified by various chromatographic techniques and identified by their physicochemical properties and spectral data.</p><p><b>RESULT</b>Eight compounds were isolated and identified as octadecyl (E)-p-coumarate (1), p-E-methoxy-cinnamic acid (2), ferulic acid (3), scopoletin (4), succinic acid (5), aurantiamide acetate (6), rubiadin (7), robustaquinone D (8).</p><p><b>CONCLUSION</b>Compounds 1-8 were obtained from genus Hedyotis for the first time.</p>

Simultaneous determination of four components in Hedyotis diffusa oral solution by reversed-phase HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>A 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.</p><p><b>METHOD</b>The 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).</p><p><b>RESULT</b>There 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%.</p><p><b>CONCLUSION</b>The method is rapid, simple and accurate, and it can be used for the evaluation of H. diffusa oral solution.</p>

Analysis of the chemical constituents of Hedyotis diffusa / 南方医科大学学报

<p><b>OBJECTIVE</b>To analyze the chemical constituents of Hedyotis diffusa.</p><p><b>METHODS</b>Column chromatographies were used to isolate and purify the chemical constituents of this plant, and their structures were identified by spectral analysis and physicochemical properties.</p><p><b>RESULTS AND CONCLUSION</b>Seven compounds were isolated and identified as p-coumaric acid (I), methyl-p-coumarate (II), 2-formyl-5- hydroxymethylfuran (III), quercetin (IV), kaempferol (V), beta-sitosterol(VI) and daucosterol(VII), respectively, among which the compounds II and III were isolated from Hedyotis diffusa for the first time.</p>

Some results of study on the chemical components of Da cam-Hedyotis sp. Rubiaceae

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

Investigation on antibacterial activities of hedyotis capitellata Wall ex G.Don var. molis Piere ex Pit

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