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This article has reported the results of the study on the outer properties, inter organization and TLC of Herba Hedyotis Diffuse and its confused material Herba Hedyotis Pinifoliae. The results show the two have obvious distinction and can not be confusediy used.
Many species of genus Hedyotis (Rubiaceae) were used as folk medicine for treatment of cold, inflammation, cancer and etc. in China. The alcoholic extract of the whole plant of H. chrysotricha showed good hepatoprotective effects. From the alcoholic extract ten iridoids were isolated and their structures were elucidated as: asperuloside (1), scandoside methyl ester (2), asperulosidic acid (3), deacetyl asperulosidic acid (4), loganin (5), deacetyl asperuloside (6), acetyl scandoside methyl ester (7), 6 beta-hydroxy-genipin (8) and two new compounds named hedyoside (9) and 6'-acetylasperuloside (10), by means of chemical and spectral methods.
Hedyotis corymbosa is used in traditional medicine of India and China to treat various hepatic disorders. In the present study, the hepatoprotective effect of the methanolic extract of the whole plant of Hedyotis corymbosa against paracetamol overdose-induced liver damage in Wistar rats was studied. The methanolic extract of the plant produced significant hepatoprotective effects as evidenced by decreased serum enzyme activities, SGPT, SGOT, SAKP and serum bilirubin and an almost normal histological architecture of the liver, in treated groups, compared to the controls. Hedyotis corymbosa shortened hexobarbitone-induced sleeping time in mice, besides showing significant antilipid peroxidant effect in vitro. The results thus support the use of Hedyotis corymbosa as a hepatoprotective agent.
A method for the determination of p-coumaric acid in Hedyotis diffusa Willd. from different sources by reversed-phase high performance liquid chromatography (RP-HPLC) has been developed. p-Coumaric acid was successfully separated on a Diamonsil ODS column (4.6 mm i.d. x 250 mm, 5 microm) at ambient temperature, using a mixture of CH3CN-20 mmol/L NH4Ac (pH 4.0) (15:85, v/v) as mobile phase and detection at 308 nm. The flow rate was 1.0 mL/min. There was good linear relationship (r = 0.9996) between the mass concentration and the peak area of p-coumaric acid in the range of 4.04 - 202 mg/L. The recoveries were found to be in the range of 97.4% - 102.2%. The results of the experiments have demonstrated that the established method is rapid and simple with good accuracy and reproducibility. The method is suitable for use in quality control of Hedyotis diffusa Willd. from different sources.
A capillary zone electrophoresis (CZE) method based on systematic one-variable-at-a time approach was developed for the analysis of four important bioactive components (geniposidic acid, ursolic acid, quercetin and p-coumaric acid) in the extract of Hedyotis diffusa (HD). Separations were carried out in a fused-silica capillary tube with peak detection at 214 nm. Good separation was achieved using a 20 mM borate buffer containing 5% acetonitrile as organic modifier and pH adjusted to 10.0. Operating voltage was 15 kV and temperature was maintained at 25 degrees C while hydrodynamic injection was 5s. A good linearity, with correlation coefficients in the ranges of 0.997-0.999 was obtained in the calibration curves of each standard. Relative standard deviation (R.S.D.) of migration time was between 0.32 and 0.70% and deviation of corrected peak area was between 8.84 and 11.99%. These results indicate that this method could be used for rapid and simultaneous analysis of the bioactive components in HD and other herbal products.
Four new furanoanthraquinones, 2-hydroxymethyl-3,4-[2'-(1-hydroxy-1-methylethyl)-dihydrofurano]-8-hydroxyanthraquinone, 2-hydroxymethyl-3,4-[1'-hydroxy-2'-(1-hydroxy-1-methylethyl)-dihydrofurano]-8-hydroxyanthraquinone, 2-hydroxymethyl-3,4-[2'-1-hydroxy-1-methylethyl)-dihydrofurano]anthraquinone and 2-methyl-3,4-[2'-(1-hydroxy-1-methylethyl)-dihydrofurano] anthraquinone or capitellataquinone A-D and four known anthraquinones, rubiadin, anthragallol 2-methyl ether, alizarin 1-methyl ether and digiferruginol, together with scopoletin were isolated from the stems of Hedyotis capitellata Wall (Rubiaceae). Lucidin-3-O-beta-glucoside was isolated from the roots of the plant. Characterization of the new compounds was carried out by extensive NMR studies using FGCOSY, FGHMQC, FGHMBC and DEPT-135 in addition to other spectroscopic methods.
Using the bioactivity-guided fractionation method, three new 6-oxygenated 8,9-dihydrofurocoumarin-type compounds, hedyotiscones A, B, and C were isolated from the methanol extract of Hedyotis biflora together with seven known compounds. The structures of all isolated compounds were determined on the basis of mass and spectroscopic evidence. Compounds, oleanolic acid, and 6'-(beta-sitosteryl-3- O-beta- D-glucopyranosidyl) pentadecanoate showed marginal cytotoxicity against Hep G2 cells (human liver cancer cells) with IC50 values of 14.4, 17.4, 4.9, 8.0, and 9.2 microg/mL, respectively. Ursolic acid showed significant cytotoxicity against MDA-MB-231 cells (human breast carcinoma cells) with an IC50 value of 1.49 microg/mL.
OBJECTIVE: This study established a rat model of lipopolysaccharide (LPS)-induced acute lung injury (ALI) to evaluate pathological damage, collagen deposition, inflammatory cytokine levels, and key gene/protein expression following Hedyotis diffusa water extract (HDWE) intervention. Combined with ultra-high-performance liquid chromatography-quadrupole Orbitrap high-resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS), transcriptomic analysis, and molecular simulation, this study identified the bioactive components of HDWE, evaluated their potential interactions with ALI-related targets, and explored the multi-omics-based protective mechanisms of HDWE. METHODS: Thirty-six Sprague-Dawley (SD) rats were randomly divided into six groups: Control group, ALI group, DXMS group, HDWE-L group (100 mg/kg), HDWE-M group (200 mg/kg), and HDWE-H group (300 mg/kg). Hematoxylin and eosin (H&E) and Masson's trichrome staining were used to evaluate lung pathological changes and collagen deposition. Enzyme-linked immunosorbent assay (ELISA) was used to measure serum tumor necrosis factor-α TNF-α interleukin-1β IL-1β, erleukin-6 (IL-6), and interleukin-10 (IL-10) levels. Transcriptomic analysis identified differentially expressed genes (DEGs), followed by Gene Ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG), receiver operating characteristic (ROC), and immune infiltration analyses. Quantitative real-time polymerase chain reaction (qRT-PCR) detected the mRNA expression levels of SPHK1, RELA, and NFKBIA. Immunohistochemistry evaluated the expression of eight hub targets, including endothelin-1 (EDN1), sphingosine kinase 1 (SPHK1), intercellular adhesion molecule 1 (ICAM1), interleukin-17 (IL-17), prostaglandin-endoperoxide synthase 2 (PTGS2/COX-2), NF-κB p65 (encoded by RELA), WT1-associated protein (WTAP), and myeloperoxidase (MPO). UHPLC-Q-Orbitrap HRMS characterized HDWE constituents. Molecular docking analysis was performed between 22 compounds and eight hub targets, followed by 100 ns molecular dynamics simulations and molecular mechanics-Poisson-Boltzmann surface area (MM/PBSA) binding free energy calculations for five core targets. Compared with the control group, the ALI group showed increased levels of TNF-α (86%), IL-1β (107%), and IL-6 (66%), accompanied by a 43% reduction in IL-10 and a 300% increase in lung collagen deposition. All HDWE doses alleviated inflammatory responses, with medium-dose HDWE showing the most pronounced effects. Specifically, medium-dose HDWE increased IL-10 levels by 52% and reduced IL-6, TNF-α, and IL-1β levels by 18%, 22%, and 11%, respectively. Transcriptomic analysis identified 2512 DEGs between the control group and ALI groups, 832 exclusive DEGs between the ALI group and HDWE-M groups, and 876 overlapping DEGs enriched in TNF, IL-17, and NF-κB signaling pathways. The eight-hub-gene diagnostic model achieved an area under the curve (AUC) of 0.969. RELA, SPHK1, and four other hub genes showed positive correlations with Th1, Th17, and neutrophil infiltration. In the ALI group, SPHK1, RELA, and NFKBIA mRNA expression levels were 1.30-, 0.96-, and 0.71-fold of those in the control group, respectively. Compared with the ALI group, high-dose HDWE treatment and low-dose HDWE treatment reduced SPHK1 expression to 0.62- and 0.57-fold, respectively, and increased NFKBIA expression to 1.68- and 1.58-fold, respectively. High-dose HDWE treatment reduced RELA expression to 0.43-fold. The expression levels of inflammation-related proteins were increased in the ALI group and were reduced after HDWE treatment. Twenty-two HDWE components were identified, 16 of which met the docking criteria. Asperulosidic acid exhibited favorable predicted binding affinities with all eight targets, with calculated binding free energies of -14.74, -14.92, -17.58, -23.04, and -16.10 kcal/mol for MPO, IL-17, NF-κB p65, PTGS2/COX-2, and SPHK1, respectively. CONCLUSIONS: This study provides systematic in vivo pharmacodynamic and in silico component-target evidence regarding the protective effects of HDWE against LPS-induced ALI. HDWE treatment increased NFKBIA expression and reduced SPHK1, RELA, and multiple inflammatory protein levels, suggesting that HDWE may regulate the IL-17/NF-κB-associated inflammatory network, although direct causal relationships require further validation. Asperulosidic acid may represent a key bioactive component with broad target-binding potential. This study was limited by the use of an LPS-induced rat ALI model without gene knockout or target inhibitor validation; therefore, further functional experiments are required to confirm the proposed regulatory mechanisms.
The present work enunciats the phenophase and plant organ development of Hedyotis diffusa Willd, at Nanjing region. These results can give a reference for the plant growing practice.
OBJECTIVE: To develop a convenient and effective method for the identification of Hedyotis diffusa. METHODS: DNA templates were extracted from H. diffusa and its adulterants samples on commercial markets. And DNA fragments of rDNA ITS-2 regions were amplified and sequenced subsequently. ITS-2 sequences of all samples were aligned. The allele-specific primer was designed for distinguishing H. diffusa. RESULTS: The nucleotide difference between H. diffusa and 8 other species is obvious in the ITS-2 region. In addition, the allele-specific primers were employed to amplify the DNA from H. diffusa and 8 other species. The result indicated that a 392 bp DNA fragment was amplified from H. diffusa, whereas no any fragment was amplified from 8 other species under the same reaction condition. CONCLUSION: The primers designed in the present study were highly specific for H. diffusa. They could be used as key components in the H. diffusa identification kit.
Five flavonoids were isolated from Hedyotis diffusa Willd. Their structures were elucidated as kaempferol (I), kaempferol 3-O-beta-D-glucopyranoside (II), kaempferol 3-O-(6"-O--L-rhamnosyl)-beta-D-glucopyranoside (III), quercetin 3-O-beta-D-glucopyranoside (IV) and quercetin 3-O-(2"-O-beta-D-glucopyranosyl)-beta-D-glucopyranoside (V) by spectroscopic analysis. Compounds I - III and V were originally isolated from H. diffusa.
Two new iridoid glycosides, asperulosidic acid ethyl ester (1) and 6'-acetyl deacetylasperuloside (2), were isolated from Hedyotis chrysotricha (Palib) Merr. Their structures were elucidated by spectroscopic means.
A new anthraquinone, 2-hydroxymethyl-10-hydroxy-1,4-anthraquinone (1), was isolated from Hedyotis herbacea along with three other known derivatives: 1,4-dihydroxy-2-hydroxymethylanthraquinone (2); 2, 3-dimethoxy-9-hydroxy-1,4-anthraquinone; and 1,4-dihydroxy-2, 3-dimethoxyanthraquinone. The structure of 1 was determined based on analysis of its spectroscopic data.
A study on the bioactive principles of Hedyotis diffusa Willd., led to the isolation of a new acyl flavonol di-glycoside which was characterized as kaempferol 3-O[2"-O-(E-6'"-O-feruloyl)-beta-D-glucopyranosyl]-beta-D-galactop yranoside by spectral and chemical methods from the methanolic extract. In addition, three known flavonol glycosides and six known iridoid glycosides were also obtained. The above-mentioned glycosides were tested for antioxidant effects on xanthine oxidase inhibition, xanthine-xanthine oxidase cytochrome c and TBA-MDA systems.
The antioxidant, radical-scavenging, anti-inflammatory, cytotoxic and antibacterial activities of methanolic extracts of seven Hedyotisspecies were investigated. The antioxidant activity was evaluated by the ferric thiocyanate (FTC) and thiobarbituric acid (TBA) methods while the radical scavenging activity was measured by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. The anti-inflammatory activity related to NO inhibition of the plant extracts was measured by the Griess assay while cytotoxicity were measured by the MTT assay against CEM-SS cell line. The antibacterial bioassay (against 4 bacteria, i.e. Bacillus subtilis B28 (mutant), Bacillus subtilis B29 (wild-type), Pseudomonas aeruginosa UI 60690 and methicillin resistant Staphylococcus aureus, (MRSA) was also carried out using the disc-diffusion method. All tested extracts exhibited very strong antioxidant properties when compared to Vitamin E (alpha-tocopherol) with percent inhibition of 89-98% in the FTC and 60-95% in the TBA assays. In the DPPH method, H. herbacea exhibited the strongest radical scavenging activity with an IC50 value of 32 microg/ml. The results from the Griess assay showed that the tested extracts are weak inhibitors of NO synthase. However, all tested extracts exhibited moderate cytotoxic properties against CEM-SS cell line giving CD50 values in the range of 21-41 microg/ml. In the antibacterial bioassay, the stems and the roots of H. capitellata showed moderate activity against the 4 tested bacteria while the leaves showed moderate activity towards B. subtilis B28, MRSA and P. aeruginosa only. The roots of H. dichotoma showed strong antibacterial activity against all 4 bacteria. All other extracts did not exhibit any antibacterial activity.
OBJECTIVE: To isolate a homogeneous polysaccharide RP from RDP (a crude polysaccharide from Dioscorea opposita Thunb.), and study its preliminary com-position and structure. METHODS: RP was obtained with water extraction, alcohol sedimentation, CTAB deprotein, cellulose column and SephadexG-100 column. The purities of RP were identified by SephadexG-200. PC analysis on its acidic hydrolysates was used to determine the sugar components. Sephadex chromatography was used to mensurate its molecular weight. IR was used to analysis RP. RESULTS: RP was homogeneous. IR indicated that RP had P configurations. The compositon was identified by paper chromatography as glucose, D-mannose, D-galactose. CONCLUSION: The research could provide a theoretical foundation for further development and utilization.
In a bioassay-guided search for neuroprotective compounds from medicinal plants, a MeOH extract of whole plants of Hedoytis diffusa yielded five flavonol glycosides, kaempferol 3-O-[2-O-(6-O-E-feruloyl)-beta-D-glucopyranosyl]-beta-D-galactopyranoside (1), quercetin 3-O-[2-O-(6-O-E-feruloyl)-beta-D-glucopyranosyl]-beta-D-galactopyranoside (2), quercetin 3-O-[2-O-(6-O-E-feruloyl)-beta-D-glucopyranosyl]-beta-D-glucopyranoside (3), kaempferol 3-O-(2-O-beta-D-glucopyranosyl)-beta-D-galactopyranoside (4), and quercetin 3-O-(2-O-beta-D-glucopyranosyl)-beta-D-galactopyranoside (5), and four O-acylated iridoid glycosides (6-9). Compounds 1 and 2 are previously unreported natural products, and all nine compounds exhibited significant neuroprotective activity in primary cultures of rat cortical cells damaged by L-glutamate.
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