Antithrombus is one of the effective methods to prevent and treat cardiovascular diseases. Based on the theory of traditional Chinese medicine,the author's previous research and relevant literature,it was found that the alkaloids in Houttuynia cordata has potential antithrombotic effect. However,the pharmacological substance basis and antithrombotic mechanism of H. cordata have not been clarified. In this study,molecular docking was used for virtual screening of antithrombotic alkaloids from H. cordata. Seventy alkaloids selected from H. cordata were screened in the docking ligand data-base with teen thrombosis targets with known crystal structures as the receptors. In addition,the small-molecule approved or to be approved drugs of targets from Drug Bank database were set as a positive reference with minimum score(S value) of each target's approved or to be approved drugs as threshold. The Dock module in Molecular Operating Environment(Version 2016) software was applied to screen the potential active compounds which their scores(S value) were lower than the minimum score of reference. At last the mechanism of antithrombotic effect was preliminarily revealed by compared the main active sites of the test alkaloids with original ligands and references. This study provided some useful information to development of antithrombus drugs.
Alkaloids ; pharmacology ; Fibrinolytic Agents ; pharmacology ; Houttuynia ; chemistry ; Molecular Docking Simulation ; Phytochemicals ; pharmacology

Nine compounds were isolated from chloroform fraction of Houttuynia cordata,and the isolates were identified as follows:( S)-5,6,6 a,7-tetrahydro-2,10-dimethoxy-4 H-dibenzo [DE,G] quinoline-1,9-diol( 1),( +)-isoboldine β-N-oxide( 2),liriotulipiferine( 3),telitoxinone( 4),isoboldine( 5),(-)-clovane-2β,9α-diol( 6),benzoic acid( 7),acantrifoside E( 8),and dibutyl phthalate( 9). Among them,compound 1 was new,and compounds 2-9 were reported from this species for the first time.
Chloroform ; Drugs, Chinese Herbal ; chemistry ; Houttuynia ; chemistry ; Phytochemicals ; analysis ; Plant Extracts ; chemistry

Houttuynia cordata polysaccharide (HCP) is extracted from Houttuynia cordata, a key traditional Chinese medicine. The study was to investigate the effects of HCP on intestinal barrier and microbiota in H1N1 virus infected mice. Mice were infected with H1N1 virus and orally administrated HCP at a dosage of 40 mg(kg(d. H1N1 infection caused pulmonary and intestinal injury and gut microbiota imbalance. HCP significantly suppressed the expression of hypoxia inducible factor-1α and decreased mucosubstances in goblet cells, but restored the level of zonula occludens-1 in intestine. HCP also reversed the composition change of intestinal microbiota caused by H1N1 infection, with significantly reduced relative abundances of Vibrio and Bacillus, the pathogenic bacterial genera. Furthermore, HCP rebalanced the gut microbiota and restored the intestinal homeostasis to some degree. The inhibition of inflammation was associated with the reduced level of Toll-like receptors and interleukin-1β in intestine, as well as the increased production of interleukin-10. Oral administration of HCP alleviated lung injury and intestinal dysfunction caused by H1N1 infection. HCP may gain systemic treatment by local acting on intestine and microbiota. This study proved the high-value application of HCP.
Animals ; Cytokines ; metabolism ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; therapeutic use ; Gastrointestinal Microbiome ; drug effects ; Houttuynia ; chemistry ; Hypoxia-Inducible Factor 1, alpha Subunit ; metabolism ; Inflammation ; drug therapy ; pathology ; Influenza A Virus, H1N1 Subtype ; pathogenicity ; Intestinal Mucosa ; drug effects ; metabolism ; microbiology ; pathology ; Lung ; drug effects ; metabolism ; pathology ; Male ; Mice, Inbred BALB C ; Orthomyxoviridae Infections ; drug therapy ; pathology ; physiopathology ; Plant Extracts ; chemistry ; Polysaccharides ; chemistry ; pharmacology ; therapeutic use ; Toll-Like Receptors ; metabolism ; Zonula Occludens-1 Protein ; metabolism

In the present study, we investigated whether quercitrin, quercetin and afzelin derived from Houttuynia cordata affect the production and gene expression of MUC5AC mucin from airway epithelial cells. Confluent NCI-H292 cells were pretreated with quercitrin, quercetin or afzelin for 30 min and then stimulated with epidermal growth factor (EGF) or phorbol 12-myristate 13-acetate (PMA) for 24 h. The MUC5AC mucin gene expression and production were measured by RT-PCR and ELISA, respectively. The results were as follows: (1) Quercitrin, quercetin and afzelin inhibited EGF- and PMA-induced MUC5AC mucin production from NCI-H292 cells; (2) The three natural products also decreased EGF- and PMA-induced MUC5AC mucin gene expression in NCI-H292 cells. These results suggest that quercitrin, quercetin and afzelin showed the regulatory effect on the steps of gene expression and production of mucin, by directly acting on airway epithelial cells.
Biological Products ; Enzyme-Linked Immunosorbent Assay ; Epidermal Growth Factor ; Epithelial Cells ; Gene Expression ; Houttuynia ; Humans ; Mucins ; Quercetin

Sodium houttuyfonate (SH) is a derivative of effective component of a Chinese material medica, Houttuynia cordata, which is applied in anti-infection of microorganism. But, the antimicrobial mechanisms of SH still remain unclear. Here, we firstly discovered that SH effectively inhibits the three types of virulence related motility of.Pseudomonas aeruginosa, i.e., swimming, twitching and swarming. The plate assay results showed that the inhibitory action of SH against swimming and twitching in 24 h and swarming in 48 h is dose-dependent; and bacteria nearly lost all of the motile activities under the concentration of 1 x minimum inhibitory concentration (MIC) (512 mg x L(-1) same as azithromycin positive group (1 x MIC, 16 mg x L(-1)). Furthermore, we found that the expression of structural gene flgB and pilG is down-regulated by SH, which implies that inhibitory mechanism of SH against motility of P. aeruginosa may be due to the inhibition of flagella and pili bioformation of P. aeruginosa by SR Therefore, our presented results firstly demonstrate that SH effectively inhibits the motility activities of P. aeruginosa, and suggest that SH could be a promising antipseudomonas agents in clinic.
Alkanes ; pharmacology ; Anti-Bacterial Agents ; pharmacology ; Bacterial Proteins ; genetics ; metabolism ; Biofilms ; drug effects ; Drugs, Chinese Herbal ; pharmacology ; Fimbriae, Bacterial ; drug effects ; genetics ; metabolism ; Houttuynia ; chemistry ; Pseudomonas aeruginosa ; cytology ; drug effects ; genetics ; pathogenicity ; Sulfites ; pharmacology ; Virulence ; drug effects

The relationship of nutrients and microorganisms in soils with polyphenols and total flavonoids of Houttuynia cordata were investigated by measuring nutrients, enzyme activity, pH, concentrations of microbe phospholipid fatty acids (PLFAs) in soils, and determining concentrations of polyphenols and total flavonoids of H. cordata. The research is aimed to understand characteristics of the planting soils and improve the quality of cultivated H. cordata. The soils at different sample sites varied greatly in nutrients, enzyme activity, pH, microbic PLFAs and polyphenols and all flavonoids. The content of total PLFAs in sample sites was following: bacteria > fungi > actinomyces > nematode. The content of bacteria PLFAs was 37.5%-65.0% at different sample sites. Activities of polyphenol oxidease, concentrations of available P and content of PLFAs of bacteria, actinomyces and total microorganisms in soils were significantly and positively related to the concentrations of polyphenols and total flavonoids of H. cordata, respectively (P < 0.05) . The Content of fungi PLFAs in soils was significantly and negatively related to concentrations of polyphenols and total flavonoids of H. cordata, respectively (P < 0.05). This study provides evidence that effectiveness of the soil nutrient, which may be improved due to transformation of soil microorganisms and enzymes to N and P in the soils, was beneficial to adaptation of H. cordata adapted to different soil conditions, and significantly affects metabolic accumulation of polyphenols and flavonoids of H. cordata.
Bacteria ; metabolism ; Drugs, Chinese Herbal ; analysis ; metabolism ; Fatty Acids ; metabolism ; Flavonoids ; analysis ; metabolism ; Fungi ; metabolism ; Houttuynia ; chemistry ; metabolism ; microbiology ; Phospholipids ; metabolism ; Polyphenols ; analysis ; metabolism ; Soil ; chemistry ; Soil Microbiology

Skin is the outermost organ and acts as a barrier between the organism and environment. Skin protects the organism from environmental insults, such as chemicals, pathogens, and UV light. Much of the protective function of skin is dependent on the epidermis, a multi-layered epithelium that is composed of various cell types such as keratinocytes and melanocytes. Keratinocytes produce protective components through a sophisticated differentiation process. Disturbance of keratinocyte differentiation is related to several skin diseases such as psoriasis and atopic dermatitis. In this study, we prepared extract of combined medicinal plants (ECMP) consisting of Taraxacum platycarpum H. Dahlstedt, Heartleaf Houttuynia, Glycyrrhiza uralensis Fischer, and root bark of Ulmus davidiana. We demonstrated that ECMP enhanced keratinocyte differentiation and barrier functionality using an in vitro cell culture system and in vivo animal test. Treatment of cultured keratinocytes with ECMP resulted in induction of keratinocyte differentiation, as evidenced by increased differentiation markers such as involucrin, loricrin, and filaggrin. In line with these results, ECMP decreased proliferation of keratinocytes cultured in vitro. ECMP applied topically to tape-stripped mouse skins accelerated reduction of transepidermal water loss (TEWL), indicating fast recovery of barrier function. Immunohistochemistry showed that ECMP increased the filaggrin level in tape-stripped mouse skins. These results suggest that ECMP may be applicable for keratinocyte differentiation-related skin diseases.
Animals ; Antigens, Differentiation ; Cell Culture Techniques ; Dermatitis, Atopic ; Epidermis ; Epithelium ; Glycyrrhiza uralensis ; Houttuynia ; Immunohistochemistry ; Keratinocytes* ; Melanocytes ; Mice ; Plants, Medicinal* ; Psoriasis ; Skin ; Skin Diseases ; Taraxacum ; Ulmus ; Ultraviolet Rays

Cognitive impairment is a result of dementia of diverse causes, such as cholinergic dysfunction and Alzheimer's disease (AD). Houttuynia cordata Thunb. (Saururaceae) has long been used as a traditional herbal medicine. It has biological activities including protective effects against amyloid beta (Abeta) toxicity, via regulation of calcium homeostasis, in rat hippocampal cells. To extend previous reports, we investigated the effects of water extracts of H. cordata herb (HCW) on tauopathies, also involving calcium influx. We then confirmed the effects of HCW in improving memory impairment and neuronal damage in mice with Abeta-induced neurotoxicity. We also investigated the effects of HCW against scopolamine-induced cholinergic dysfunction in mice. In primary neuronal cells, HCW inhibited the phosphorylation of tau by regulating p25/p35 expression in Abeta-induced neurotoxicity. In mice with Abeta-induced neurotoxicity, HCW improved cognitive impairment, as assessed with behavioral tasks, such as novel object recognition, Y-maze, and passive avoidance tasks. HCW also inhibited the degeneration of neurons in the CA3 region of the hippocampus in Abeta-induced neurotoxicity. Moreover, HCW, which had an IC50 value of 79.7 microg/ml for acetylcholinesterase inhibition, ameliorated scopolamine-induced cognitive impairment significantly in Y-maze and passive avoidance tasks. These results indicate that HCW improved cognitive impairment, due to cholinergic dysfunction, with inhibitory effects against tauopathies and cholinergic antagonists, suggesting that HCW may be an interesting candidate to investigate for the treatment of AD.
Acetylcholinesterase ; Alzheimer Disease ; Amyloid ; Animals ; Calcium ; Cholinergic Antagonists ; Dementia ; Herbal Medicine ; Hippocampus ; Homeostasis ; Houttuynia* ; Inhibitory Concentration 50 ; Memory ; Mice ; Neurons ; Phosphorylation ; Rats ; Tauopathies ; Water

Development of a therapy providing protection from, or reversing gentamicin-sulfate (GS)-induced oxidative stress and nephrotoxicity would be of great clinical significance. The present study was designed to investigate the protective effects of Houttuynia cordata Thunb. (HC) against gentamicin sulfate-induced renal damage in rats. Twenty-eight Sprague-Dawley rats were divided into 4 equal groups as follows: group 1, control; group 2, GS 100 mg/kg/d, intraperitoneal (i.p.) injection; group 3, GS 100 mg/kg/d, i.p. + HC 500 mg/kg/d, oral; and group 4, GS 100 mg/kg/d i.p. + HC 1000 mg/kg/d, oral administration). Treatments were administered once daily for 12 d. After 12 d, biochemical and histopathological analyses were conducted to evaluate oxidative stress and renal nephrotoxicity. Serum levels of creatinine, malondialdehyde (MDA), and blood urea nitrogen (BUN), together with renal levels of MDA, glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT) were quantified to evaluate antioxidant activity. Animals treated with GS alone showed a significant increase in serum levels of creatinine, BUN, and MDA, with decreased renal levels of GSH, SOD, and CAT. Treatment of rats with HC showed significant improvement in renal function, presumably as a result of decreased biochemical indices and oxidative stress parameters associated with GS-induced nephrotoxicity. Histopathological examination of the rat kidneys confirmed these observations. Therefore, the novel natural antioxidant HC may protect against GS-induced nephrotoxicity and oxidative stress in rats.
Animals ; Blood Urea Nitrogen ; Catalase ; Cats ; Creatinine ; Drug Combinations ; Gentamicins ; Glutathione ; Glycerides ; Houttuynia ; Kidney ; Malondialdehyde ; Monoterpenes ; Oxidative Stress ; Rats ; Rats, Sprague-Dawley ; Superoxide Dismutase

OBJECTIVETo establish and optimize the preparation procedures of the anti-complementary polysaccharides from Houttuynia cordata.

METHODBased on the yield and anti-complementary activity in vitro, the conditions of extraction and alcohol precipitating process were optimized by orthogonal tests. The optimal condition of deproteinization was determined according to the results of protein removed and polysaccharide maintained. The best decoloring method was also optimized by orthogonal experimental design.

RESULTThe optimized preparation procedures were given as follows: extract the coarse powder 3 times with 50 times volume of water at 90 degrees C for 2 hours every time, combine the extracts and concentrate appropriately, equivalent to 0.12 g of H. cordata per milliliter. Add 4 times volume of 90% ethanol to the extract, allow to stand for 24 hours to precipitate totally, filter and the precipitate was successfully washed with anhydrous alcohol, acetone and anhydrous ether. Resolve the residue with water, add trichloroacetic acid (TCA) to a concentration of 20% to remove protein. Decoloration was at a concentration of 3% with activated carbon at pH 3.0, 50 degrees C for 50 min. The above procedures above were tested 3 times, resulting in the average yield of polysaccharides at 4.03% (RSD 0.96%), the average concentrations of polysaccharides and protein at 80.97% (RSD 1.5%) and 2.02% (RSD 2.3%), and average CH50 at 0.079 g x L-(-1) (RSD 3.6%).

CONCLUSIONThe established and optimized procedures are repeatable and reliable to prepare the anti-complementary polysaccharides with high quality and activity from H. cordata.