Научная статья на тему 'Progressin pharmacological activities of diosmin'

Progressin pharmacological activities of diosmin Текст научной статьи по специальности «Фундаментальная медицина»

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DIOSMIN / PHARMACOLOGICAL

Аннотация научной статьи по фундаментальной медицине, автор научной работы — Kong Xiaoyue

Diosmin is flavonoids compound. It can increase the tension of the vein, improve microcirculation, promote lymphatic reflux, and alleviate edema. In recent years, some new pharmacological effects of diosmin have been stud-ied. In this paper, the pharmacological effect from diosmin of recent years were bebriefly reviewed, which provides scientific basis for the development and utilization of diosmin.

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Текст научной работы на тему «Progressin pharmacological activities of diosmin»

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COMPARATIVE STUDY ON PHARMACOKINETICS OF AMERICAN GINSENG IN THE MAIN COMPONENT OF HUAQIZ-

EREN

Kaixin Liu1, Sun Yu1, JiaXin Li1,Pengyang Yu1, Qijing Huang1,Yu ChiZhang1, Xiaonan Liu1, PengLing Ge1*

1Department of Pharmacology, School of Basic Medical Sciences, Heilongjiang University of Chinese Medicine, Harbin 150040, China; Corresponding authors: Pengling Ge, Department of Pharmacology, School of Basic Medical Sciences, Heilongjiang University of Chinese Medicine, 24 Heping Road, Harbin 150040, China; E-mail: penglingge@126.com

Objectives Comparative study on HuaQiZeRen of ginsenoside Rb1and American ginseng of ginsenoside Rb1 in rat plasma pharmacokinetics.

Materials and methods The establishment of ultra high liquid chromatography tandem mass spectrometry to study the sensitivity and reliability of HuaQiZeren single herbs ginseng in rats in vivo pharmacokinetic characteristics, improve drugability evaluation HuaQiZeren.SD rats were randomly divided into HuaQiZeren group and American ginseng group were orally given HuaQiZeren and Panax quinquefolium decoction, to give medivine before and after a series of time points of blood plasma samples were collected for determination of Pharmacokinetic parameters were calculated by DAS software, the main medicine ginseng group and active ingredient group ZerenHuaQiZeren ginsenoside Rb1 pharmacokinetic parameters were compared, observe the main pharmacokinetic parameters have no significant difference.

Results Between 0.05~10 and g/mL concentrations, ginsenoside Rb1 had a good linear relationship in plasma, with a lower limit of 0.05 g/mL, and the difference between day and day was less than 10%. Citi group and Zeren ginseng group active component ginsenoside Rb1 pharmacokinetic parameters were the main drugs in rats: Cmax (g/L) 779.6 + 70.92 and 608.6 + 85.67; Tmax (H) 2 and 0.75; the elimination half-life t1/2 (H) 15.58 + 7.574 and 9.947 + 4.099; AUC0-t area under the concentration time curve (g/L*h) 9937 + 1503 and 3662 + 301.5; the average residence time of MRT0-t (H) 0.7406 and 14.67. 7.825 + 0.4090; plasma clearance rate of CL (L/h/kg) 0.1968 + 0.04122 and 0.4992 + 0.07002. Comparison of pharmacokinetic parameters and the ginseng group active ingredients of ginsenoside Rb1, Citibank Group HuaQiZeren active ingredients of ginsenoside Rb1CmaxP<0.01, AUC0-tP<0.01, T1/2P<0.05 and MRT0-t were significantly increased in P<0.01, CL and P<0.01 decreased significantly.

Conclusion In vivo the main active ingredients of Citigroup Zeren ginsenoside Rb1 absorption and metabolism is relatively slow, can maintain a high plasma concentration. The compatibility of active ingredients Citibank Zeren of ginsenoside Rb1 in Panax ginseng and absorption.

Key words:Huaqizeren; ginsenoside Rb1; HPLC-MS/MS;Comparative pharmacokinetics References:

[1]Dai min Ta,o, Li Wei. Pharmacological action of.Chineseherbal medicine and edible herbs on prevention and treatment of diabetes meTlitus [J]. northern pharmaceutical science, 2014,05:89.

colmpN GeCi Ys [J]WANGho pharma c^U^ti-^ bSti^^ of Panax notoginseng saponins and its major anti-hyperglycemic-[owm thVeuAsrae,rectaarh.C8ll¿agce-MfзhUuarrítiaonnd,20вe,ri^8nзGins7вg :f8&erging Alternative Therapies for Type 2 Diabetes Mellitus [J].

gftXeJ Wry Je><t ra.cM ei1 ondtaibemHii: ¿'[jfAun gy tcuai e Ci aiAntifi0B,erfll¥&2m[i87effect of the polysaccharides fraction from American

[5] LLWenlan^Mjnamj Riri,, Ji.Yubin, Sun Xiangming, Sun Zhi. Study on .the.mechanism. of in vivo intestinal absorption of ginsenoside Rg1 and Rb1 in ginseng. [C]. Symposium on quality analysis and identification of Chinese crude drugs.

[6] S. Zhou, H.L. Koh, Y. Gao, Z. Gong, E.J.D. Lee, Herbal bioactivation: the good, the bad and the ugly[J], Life sciences, 2004, 74 (8): 935-968.

PROGRESSIN PHARMACOLOGICAL ACTIVITIES OF DIOSMIN Kong Xiaoyue

(School of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin150040, China)

Abstract: Diosmin is flavonoids compound. It can increase the tension of the vein, improve microcirculation, promote lymphatic reflux, and alleviate edema. In recent years, some new pharmacological effects of diosmin have been studied. In this paper, the pharmacological effect from diosmin of recent years were bebriefly reviewed, which provides scientific basis for the development and utilization of diosmin.

Key words: Diosmin; pharmacological

38 Амурский медицинский журнал №4 (20) 2017

Diosmin, Molecular formula: C28H32O15 ; Molecular weight: 608, which can also be found in a variety of natural plants, such as Galium verum, Mint, Lobelia, Milia, Toddalia asiatica, Bergamo, we reviewed the latest pharmacological researches and clinical application prospections in recent years.

1 Antidiabetic effect Srinivasan S[1] found that the effect of 2- on the oxidative stress induced by streptozotocin (STZ) has good therapeutic effect on diabetic rats. 2- induced diabetic rat model was established by STZ. The plasma glucose level of model group significantly increased and the plasma insulin level was significantly lower ; Jain D [2] found that diosmin can improve the nerve lesion in early diabetic rats, type 2- diabetic rats by dafion 5~100 mg/kg after four weeks treatment.It can reduce the body weight, elevate blood glucose and lipid levels were restored;

2 Hypotensive effect Silambarasan T[3]established hypertension model rats by subcutaneous injection of deoxycorticosterone acetate and oral Sodium Chloride Solution, resulting in a rat model of cardiac systolic and diastolic blood pressure, serum sodium and chlorine, plasma and tissues (liver, kidney, heart and aorta) in lipid peroxidation increased significantly.

3 Hypotensive effect The protective effect of geraniol on myocardial injury is closely related to scavenging free radicals and reducing lipid peroxidation.[4]

4 Ischemia reperfusion injury Dung TD[5]esearch showed that diosmin can resist against cerebral ischemia reperfusion injury in mice induced by apoptosis, activation of JAK2/STAT3 signaling pathway protects the brain ischemia reperfusion injury, and diosmin in high dose group can significantly relieve nerve injury, brain edema, reduce the infarction area, pJAK2, pSTAT3, Bcl-2 expression and downregulation of Bax.

5 Anti apoptosis effect Many studies showed that increased apoptosis and neurodegenerative diseases, inflammatory factors have a certain relationship, the majority of LPS induced cell apoptosis play a role through TNF- products.

6 Anti Lung injury

Imam F's studies show that Diosmin can inhibit proinflammatory cytokines and activation of NF- protective effects on lung injury induced by lipopolysaccharide receptor, T cell. The protective mechanism mainly involves reducing the number of neutrophils, monocytes, lymphocytes, white blood cells (TLC) and platelet count;

7 Other effects Yoo HH[7]found that diosmin had an inhibitory effect on P-gP in Caco-2 cells, which could increase the absorption of P-gp substrates. Attention should be paid to the combination of drugs in clinical treatment in order to avoid adverse reactions.

Reference:

[1]SRINIVASAN S, PARI L. Ameliorative effect of diosmin, a citrus flavonoid against streptozotocin-nicotinamide generated oxidative stress induced diabetic rats [J]. Chem Biol Interact, 2012, 195(1): 43-51.

[2]JAIN D, BANSAL MK, DALVI R, et al. Protective effect of diosmin against diabetic neuropathy in experimental rats [J]. J Integr Med, 2014, 12(1): 35-41.

[3]SILAMBARASAN T, RAJA B. Diosmin, a bioflavonoid reverses alterations in blood pressure, nitric oxide, lipid peroxides and antioxidant status in DOCA-salt induced hypertensive rats [J]. Eur J Pharmacol. 2012, 679(1-3):81-89.

[4]QUEENTHY SS, JOHN B. Diosmin exhibits anti-hyperlipidemic effects in isoproterenol induced myocardial infarcted rats [J]. Eur J Pharmacol, 2013, 718(1-3):213-218.

[5]DUNG TD, DAY CH, BINH TV, et al. PP2A mediates diosmin p53 activation to block HA22T cell proliferation and tumor growth in xenografted nude mice through PI3K-Akt-MDM2 signaling suppression [J]. Food ChemToxicol, 2012, 50(5):1802-1810.

[6]DHOLAKIYA SL, BENZEROUAL KE. Protective effect of diosmin on LPS-induced apoptosis in PC12 cells and inhibition of TNF-a expression [J]. Toxicol In Vitro, 2011, 25(5):1039-1044.

[7]RAJNARAYANA K, VENKATESHAM A, KRISHNA DR. Influence of some bioflavonoids on the transport of nitrendipine[J]. Drug Metabol Drug Interact, 2008, 23(3-4):299-310.

APPLICATIONS OF OMICS TECHNOLOGY ON TCM SYMPTOMS EXPLORATION

Le Yang, Aihua Zhang, Hui Sun, QI Song, Xijun Wang*

Sino-America Chinmedomics Technology Collaboration Center, National TCM Key Laboratory of Serum Pharmacochemistry, Chinmedomics Research Center of State Administration of TCM, Laboratory of Metabolomics, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Heping Road 24, Harbin, China. E-mail:

xijunwangls@126.com

Abstract: Traditional Chinese medicines (TCMs) have a long history for the treatment or preventing disease. The symptoms classification may guide patient classification of predose phenotype and prescribe traditional Chinese medicines formula according to the phenotype. The accurate classification of symptoms is a prerequisite for the treatment of traditional Chinese medicine. Due to the diversity pathological basis of TCM syndrome and the uniqueness of the diagnostic methods, it is difficult to use modern medicine to explain the scientificity of TCM syndrome and to diagnose it more accurately. Om-ics technology (such as Proteomics, Metabolomics, Transcriptomics, Genomics, etc.) has brought the dawn to clarify the mechanism and accurate diagnosis of TCM syndrome. This paper reviews the widely used of past four kinds of omics technology in the research of TCM syndrome and highlights the key role of modern tools for precise diagnosis of TCM syndrome.

Амурский медицинский журнал №4 (20) 2017

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