Discussion on the Correlation Between Histamine Receptor and Liver Storage in Traditional Chinese Medicine / 世界科学技术-中医药现代化

The theory of Zang Xiang is the core of the theory of traditional Chinese medicine,and its content mostly comes from the comparison of images.Among them,the liver Zang of"main drainage"and"main blood storage"involves many systems such as nerve,digestion,circulation,hematopoiesis,reproduction and so on.It is difficult to find the corresponding anatomical organs or tissues in western medicine.The author analyzes and believes that the collection of the functional system of the liver system of traditional Chinese medicine,compares the physiological function and pathological changes of the liver system with the histamine receptor distributed in multiple systems of the whole body,as well as the main symptoms and adverse reactions of the drugs regulating the histamine receptor,and believes that the functional system composed of histamine receptors may carry the important functions of the liver system of traditional Chinese medicine.

Molecular Docking Studies Of Siddha Herbal Formulation Kuppaimeni Choornam On Human Histamine Receptor (3rze)

Background: Molecular docking has tremendous applications in the field of Siddha medicine especially herbal formulations were the interactions of the lead molecules of the formulation with that of receptors can be elucidated at the molecular level and furthermore to reach an assumption of its fundamental biochemical processes to which the formulation is targeting. Kuppaimeni Choornam (KC) is a simple herbal formulation used in Siddha medicine for urticaria and other skin allergies. As far as skin allergy is concerned Amino acids such as Asparagine (ASN), Tryptophan (Trp), Aspartate (Asp), Tyrosine (Tyr), Serine (Ser), Isoleucine (Ile), Lysine (Lys), Threonine (Thr), Phenylalanine (Phe) are the main core residues involved in mediating Human histamine receptor (3RZE). Binding of lead compounds with this core residue may inhibit the enzyme activity. Aim & Objectives: Molecular docking studies of Siddha herbal formulation KC and to screen the lead component interaction on the Human Histamine Receptor (3RZE). Methodology: Docking calculations were carried out using Auto Dock 4. Gasteiger partial charges were added to the ligand atoms. Docking simulations were performed using the Lamarckian genetic algorithm (LGA) and the Solis & Wets local search method. Initial position, orientation, and torsions of the ligand molecules were set randomly. All rotatable torsions were released during docking. Results and Conclusion: The compounds present in KC like beta-sitosterol, apigenin, luteolin, cuminaldehyde, kaempferol, and triacetonamine showed maximum interactions with 3RZE when compared to that of the standard cetirizine. Hence, these compounds of test drug possess promising Human histamine 1 receptor (3RZE) inhibition activity. For prospective pharmacological validation of Kuppaimeni Choornam, the docking studies were an important step for its scientific justification.

Expressions of histamine receptors in pediatric mid-urethral striated muscles and mouse striated myogenesis / 中华实用儿科临床杂志

Objective To explore the expressions of histamine receptor subtypes (H1, H2, H3, H4 receptor) in children's mid-urethral striated muscles and during mouse C2C12 striated myogenesis.Methods Children's mid-urethral striated muscle samples were paraffin embedded and tissue sections were made, then immunohistochemical staining was used to check H1, H2, H3, H4 receptors.C2C12 myogenesis was induced, the early differentiation early markers of desmin, middle marker of myogenin, late marker of myosin heavy chain and histamine 4 receptor subtype mRNA were checked by quantitative real-time polymerase chain reaction.Immunofluorescence staining was done to check 3 differentiation markers and histamine H3 receptor protein.Results During myogenesis, the expression of desmin mRNA in the differentiation of 2,4,6 days were 12,68,60 times as many as that of the undifferentiated myoblasts;the expression of myogenin mRNA in the differentiation of 2,4,6 days were 631,1 408,914 times as many as that of the undifferentiated myoblasts;the expression of myosin heavy chain mRNA in the differentiation of 2,4,6 days were 7 718,9 448,286 288 times as many as that of the undifferentiated myoblasts.The expression level of H1 receptor mRNA in the differentiation of 6 days was about 25％ to undifferentiated cells;the expression of H2 receptor mRNA in undifferentiated cells and differentiated cells groups had no significant difference (F =1.47, P ＞ 0.05);the expression of H3 receptor mRNA in the differentiation of 2,4,6 days was 28,103,198 times to undifferentiated cells;H4 receptor mRNA was not detected.In immunofluorescence staining, H3 receptor protein staining intensity increased with the differentiation.Immunohistochemistry of pediatric urethral striated staining indicated that H1, H2, H3 receptor staining was positive,H1 receptor showed strong positive staining, H3 receptor moderate positive staining,and H2 receptor showed weak positive staining.Conclusions Histamine receptor subtypes of H1 receptor, H2 receptor and H3 receptor were found during mouse striated myogenesis and in the children's mid-urethral striated muscles.The increasing expression of H3R with myogenesis might indicate it plays a role in mature striated muscle cells.

Significance of H1 receptor expression in kidney and bladder tissues of rats after long term ketamine intraperitoneal injection / 中华泌尿外科杂志

Objective To investigate the expression and clinical significance of H1 receptor in kidney and bladder tissue of rats after long term ketamine intraperitoneal injection.Methods This study was conducted from May 2012 to December 2012.Sixty male 2-month-old SD rats,weighted (200±10) g,were randomly divided into Group A and Group B.Each group concluded 30 rats.In the Group A,Ketamine (100 mg/kg) was given as intraperitoneal injection every other day,while normal saline (100 mg/kg) was given in Group B.The dosage was adjusted every week according to the weight of rats.After 2,4 and 6 months,10 rats from each group were randomly chosen.First,the micturition number during 2 h was recorded.Then,urine samples over a 24 h period were collected and the content of Na+ and K+ were determined.Finally,the blood samples were obtained from the apex of heart for the creatinine determination.The kidneys and bladders were harvested after the rats were sacrificed.HE staining was conducted on all the tissues.Immunohistochemical S-P method was used to detect the expression of H1 receptor in the bladder and kidney tissues from Group A and Group B.The average optical density (A Value) in each group was separately calculated by Imagepro-plus 6.0 software.All the parameters,mentioned above,were carefully compared.Results The successive rate of establishing rats model was 90％ (9/10),according to the pathological result after 6 months injection.The urine volume of 24 h in group A and B were (15.9±1.3) and (10.1±0.8) ml,respectively.Micturition frequency during 2 hours in group A and B were (6.9±1.4) and (3.0±0.5) times.The urine volume of 24 h and micturition frequency during 2 hours were significantly increased in group A (P＜ 0.05).The urine sodium within 24 h in group A was (1.7±0.1) mmol,which is increased significantly than that in group B (1.0±0.1 mmol).While the urine potassium was less in group A (1.1±0.1 mmol/d) than in group B (2.6±0.1 mmol/d) (P＜0.05).But the serum creatinine level were (60.5±6.8) and (58.1± 3.9) μmol/L in group A and B,which had no difference between the two groups (P＜0.05).The expression of H1 receptor in kidneys and bladder in group A was significantly raised compared with group B (P＜0.05).In the group A,the expression of H1 receptor level in kidney was 0.008±0.001,0.016±0.001,0.023±0.004 after 2,4 and 6 months drug used.The expression level in group A were significantly difference than that in group B (0.003±0.001,0.004±0.002,0.003±0.001) (P＜0.05) and goes up with prolonging the drug using.While in the bladder tissue,the level of H1 receptor expression was 0.017±0.006,0.031±0.012,0.036±0.007 in group A and 0.015±0.007,0.016±0.005,0.016±0.004 in group B,which could be noticed a significantly increasing in group A (P＜0.05).In 4 and 6 months,the H1 receptor expression level significantly raised than that in 2 months (P＜0.05).Conclusions Long term ketamine addiction exerts toxicity not only on the bladder but also on the kidney.The increased expression of H1 receptor in rats' kidney and bladder tissues of group A indicates that H1 receptor may be related to the ketamine-associated urinary system dysfunction.The urine sodium and potassium within 24 h may be a sensitive index for the assessment of degree of kidney damage in the early stage of ketamine-induced dysfunction than serum creatinine.

Effect of Zataria multiflora Bois L. on histamine (H1) receptor of guinea pig tracheal chains.

The effects of three concentrations (2.5, 5 and 10 mg/ml) of aqueous-ethanolic extract of Z. multiflora bois, 10 nM chlorpheniramine, and saline on histamine (H1) receptors were tested on two groups of guinea pig tracheal chains [trachea incubated with indomethacin (Gr. 1), and indomethacin and propranolol (Gr. 2)]. The effective concentration of histamine causing 50% of maximum response (EC50) obtained in presence of chlorpheniramine in both groups, all concentrations of the extract in group 1 and its two higher concentrations in group 2 were significantly greater than those of saline. The values of concentration ratio minus one (CR-1) obtained in presence of all the three concentrations of the extract in group 1 and 10 mg/ml concentration in group 2 were significantly greater than those of chlorpheniramine. The values of EC50 obtained in presence of all the three concentrations of extract and CR-1 obtained in the presence of 2.5 and 5 mg/ml concentrations in group 2 were lower than group 1. There was not significant difference in maximum response obtained in presence of different concentrations of extract between two groups. There were parallel right ward shift in concentration response curves obtained in presence of all concentrations of the extract in both the groups. These results indicated an inhibitory effect of Z. multiflora at histamine H1 receptors.

Prevention of ischemia-reperfusion injury in rat skin island flap: comparison of histamine receptor blocking agents with l-arginine

Role of Endogenous Histamine on the Pathogenesis in the Endotoxin-Induced Acute Lung Injury / 결핵

BACKGROUND: Histamine is widely distributed in the lung. It increases capillary permeability and the P-selectin expression on vascular endothelial cell surfaces. We studied the role of endogenous histamine on the pathogenesis of endotoxin-induced acute lung injury (ALI) in rats. METHODS: We instilled either normal saline (control group) or lipopolysaccharide (3 mg/Kg, LPS group) to tracheas of Sprague-Dawley rats. H1-receptor blocker (mepyramine, 10 mg/Kg, H1RB group), H2-receptor blocker (ranitidine, 10 mg/Kg, H2RB group), and H3-receptor blocker (thioperamide, 2 mg/Kg, H3RB group) were administered through vein or peritoneum along with intratracheal LPS administration. Statistical significance was accepted at p<0.05. RESULTS: LPS increases the histamine level in BAL fluid significantly at 2 h after the treatment compared with control group. LPS significantly increases protein concentration, PMN cell count in bronchoalveolar lavage (BAL) fluid, and myeloperoxidase (MPO) activity in the lung tissue at 6 h compared to control group. PMN cell count in BAL fluid and MPO activity in lung tissue were significantly lower in H2RB-group compared to LPS-group. However, protein concentration in BAL fluid showed no significant differences between the LPS alone and LPS with histamine receptor blockade. CONCLUSIONS: Endogenous histamine might be involved in the recruitment of PMNs in LPS-induced ALI via H2 receptor. However, its role in ALI would not be significant in this model.

Role of Endogenous Histamine on the Pathogenesis in the Endotoxin-Induced Acute Lung Injury / 결핵

BACKGROUND: Histamine is widely distributed in the lung. It increases capillary permeability and the P-selectin expression on vascular endothelial cell surfaces. We studied the role of endogenous histamine on the pathogenesis of endotoxin-induced acute lung injury (ALI) in rats. METHODS: We instilled either normal saline (control group) or lipopolysaccharide (3 mg/Kg, LPS group) to tracheas of Sprague-Dawley rats. H1-receptor blocker (mepyramine, 10 mg/Kg, H1RB group), H2-receptor blocker (ranitidine, 10 mg/Kg, H2RB group), and H3-receptor blocker (thioperamide, 2 mg/Kg, H3RB group) were administered through vein or peritoneum along with intratracheal LPS administration. Statistical significance was accepted at p<0.05. RESULTS: LPS increases the histamine level in BAL fluid significantly at 2 h after the treatment compared with control group. LPS significantly increases protein concentration, PMN cell count in bronchoalveolar lavage (BAL) fluid, and myeloperoxidase (MPO) activity in the lung tissue at 6 h compared to control group. PMN cell count in BAL fluid and MPO activity in lung tissue were significantly lower in H2RB-group compared to LPS-group. However, protein concentration in BAL fluid showed no significant differences between the LPS alone and LPS with histamine receptor blockade. CONCLUSIONS: Endogenous histamine might be involved in the recruitment of PMNs in LPS-induced ALI via H2 receptor. However, its role in ALI would not be significant in this model.

Advances in the study on histamine / 中国药理学通报

The effect of histamine on cardial vascular ,gland,tumor and allergic reaction were reviewed and the development of its antagonist is summarized.