Research progress in immune regulation mechanism of Polygonati Rhizoma polysaccharide / 中国药理学与毒理学杂志

Polygonati Rhizoma is the dry rhizome of Liliaceae plants Polygonatum kingianum coil ethemsl, Polygona?tum sibiricum Redoute and Polygonatum cyrtonem Hua. It tastes sweet and has a flat nature. It belongs to the spleen, lung and kidney channels. Polygonati Rhizoma contains a variety of chemical components, including polysaccharides, alkaloids, steroidal saponins, lignans, phytosterols, and so on. Polygonati Rhizoma polysaccharide (PSP) is one of the main bioactive components of Polygonati Rhizoma. It is widely used. It has the effects of enhancing immunity, anti-inflammatory, anti-virus and regulating blood lipid. In recent years, the immunomodulatory function of PSP has been paid more and more attention by researchers. PSP can play an immunomodulatory role through a variety of mecha?nisms. (1) Effects of PSP on innate immunity. ① Macrophages have a strong ability to phagocytize and clear foreign bodies. When polysaccharides bind to macrophage specific membrane receptors, the immune response will be officially activated. RAW264.7 cells can be activated by PSP MR and TLR4 mediated signal pathway to improve the pinocytosis and phagocytosis of RAW264.7 cells. ② Natural killer cell (NK cell) is a very important immune cell in the body. It is a non-specific immune killer cell naturally existing in the body. It has the dual functions of immune regulation and cytotoxic?ity. It was found that the signal pathway mediated by PSP CR3 and TRL2 may play a major role in the stimulation of NK cells. (2) Effects of PSP on adaptive immune response. ① Lymphocytes can be divided into two forms: T cells and B cells due to different differentiation and maturation sites. T lymphocytes are the general name of thymus dependent lym?phocytes. B lymphocytes differentiate and mature from animal bone marrow cells and exert their humoral immune func?tion by secreting different antibodies. It was found that PSP could activate T/B lymphocytes and increase the ratio of CD4+/CD8+in lymph cells to promote the regulation of immune system.②Thymus and spleen index refers to the level of body immunity through the development of immune organs and the functional status of immune cells. The higher the index of thymus and spleen, the higher the immune activity. A large number of studies have found that PSP can improve immune activity by promoting the proliferation of spleen lymphocytes and regulating organ index, so as to increase the weight and index of thymus and spleen induced by CY. ③ Antibody is a glycoprotein secreted by B cells after antigen stimulation and a series of proliferation and differentiation into plasma cells. Antibody production level is one of the main indicators of nonspecific immune function. PSP can not only improve the serum antibody level of mice by regulating the phagocytosis of mouse macrophages and the level of serum hemolysin, but also enhance the concentration of IL-2 secreted by spleen lymphocytes in vitro to increase the level of antibody response, and then improve the humoral immune function of the body. (3) Effect of PSP on cytokines. ① A large number of experiments have proved that PSP has a significant effect on promoting the production of interleukin (IL). PSP can combine with specific receptors on the surface of immune cells to activate various intracellular signal transduction pathways, enhance the secretion of cytokines such as IL-2, IL-4, IL-6 and IL-10 by spleen lymphocytes in vitro, make them directly kill target cells and regulate the immune function of the body at the molecular level. ② Interferon (IFN) is a special protein or glycoprotein produced by human or animal cells in response to various stimuli. It plays an important role in anti-virus, immune regulation and cell proliferation control. It was found that PSP could increase IFN-γsecreted by T cells and NK cells, activate macrophages to regulate immune function. ③ Tumor necrosis factor (TNF) is mainly produced by activated macrophages, NK cells and activated T cells. It is a cytokine with important biological activity in antitumor immune response.④ Tumor necrosis factor (TNF) is mainly produced by activated macrophages, NK cells and activated T cells. It is a cytokine with important biological activity in antitumor immune response. PSP can promote the proliferation and phagocytic activity of macro?phage RAW264.7 to reduce its apoptosis rate. By increasing the secretion of TNF-α, PSP can promote the dissociation between NF-κВprotein and IκВp65 protein after phosphorylation, so as to start the expression and transcription of related immune genes. In conclusion, PSP can improve immunity and has a good application prospect in the development of immunomodulatory drugs.

Research progress in mulberry leaf polysaccharide in treating diabetic nephropathy / 中国药理学与毒理学杂志

Diabetic nephropathy (DN) is one of the most common complications of diabetes. It is an important cause of diabetes disability and death. DN is a systemic metabolic syndrome. In its pathogenesis, the interaction of various cell activities and a large number of cytokine biological activities, the activation of signal pathways and so on are involved in the development of DN. At present, the clinical treatment of DN is mainly Western medicine, but it has limitations such as strong toxicity, high side effects and poor compliance. Therefore, the discovery of natural anti-DN substances has also become an important means to treat DN. Mulberry leaves are the dry leaves of Morus alba L. It is not only a tradi?tional Chinese medicine, but also a dual-purpose medicinal material for medicine and food. It has the effects of dispelling wind and clearing heat, cooling blood and brightening eyes, tonifying and so on. Mulberry leaf polysaccharide (MLP) is a kind of high molecular compound in mulberry leaves. It has many pharmacological effects, such as hypoglycemic, antiox?idant, anti-stress, anti-virus and so on. Therefore, the pharmacological effects of mulberry leaf polysaccharides on dia?betic nephropathy are reviewed in this paper, so as to provide references for further research and application. The patho?genesis of DN is complex, and the mechanism of renal injury has not been completely clarified. The current studies believe that DN is closely related to heredity, abnormal glucose metabolism, abnormal lipid metabolism, microcirculation disorder, cytokine action, oxidative stress and so on. Relevant studies show that the pharmacological effects of mulberry leaf polysaccharide in the prevention and treatment of DN mainly include: ① Effect on transforming factor-β1 (TGF-β1):TGF-β1 has become an important cytokine involved in the formation of renal fibrosis by regulating cell proliferation and differentiation and the production of extracellular matrix (ECM). MLP can significantly inhibit TGF-β1 protein, and then inhibit the synthesis of extracellular matrix by renal interstitial fibroblasts and inhibit the realization of fibrosis.②Effect on insulin receptor substrate (IRS-1): IRS-1 is an important signal molecule at the beginning of IR signal transduction. The decrease of IRS-1 gene expression or the decrease of expression can affect the effective transmission of IR signal and lead to the development and deterioration of diabetes. MPL can significantly increase the expression of IRS-1 mRNA in liver tissue of DN rats, so as to prevent and treat DN. ③ Effect on the expression of resistin protein in adipose tis?sue. Resistin is a secretory polypeptide derived from adipose tissue and is specifically expressed in white adipose tissue and is closely related to type 2 diabetes mellitus (T2DM). Experimental studies show that MLP can effectively reduce the expression of resistin protein in white adipose tissue of T2DM rats, indicating that MLP may reduce the level of IR by inhibiting the expression of resistin in adipose tissue, thereby reducing the insulin resistance state of T2DM rats, so as to achieve the goal of treating diabetes.④Effect on adiponectin receptor 1 (AdipoR1):adiponectin can improve insulin resistance, reduce blood glucose and lipid. AdipoR1 is mainly expressed in skeletal muscle and kidney. Studies have shown that AdipoR1 is closely related to the occurrence and development of DN. The results showed that MLP could reduce the blood glucose and blood lipid level and up regulate the expression of AdipoR1 mRNA in DN rats, suggesting that MLP may delay the occurrence and development of DN. This article reviewed the pharmacological effects of mulberry leaf polysaccharides on diabetic nephropathy, and provided a useful basis for further development and utilization of mul?berry leaf polysaccharides in the treatment of DN.

Research progress in pharmacological effects of polyphenols in Areca catechu L / 中国药理学与毒理学杂志

Betel nut is the dry and mature seed of Areca catechu L., which is originated in Malaysia and cultivated in Yunnan, Hainan and Taiwan and other tropical areas of China. It is also known as big belly, binmen, olive seed, green seed and so on. Betel nut is a dual-use resource for medicine and food, which was first contained in LI Dang's Pharma?ceutical Record. Betel nut tastes bitter, pungent, warm in nature, and belongs to the stomach and large intestine meridian. It contains a variety of chemical components such as alkaloids, phenolic compounds, polysaccharides, fatty acids, amino acids, flavonoids, minerals, terpenoids, and steroids. It has the advantages of promoting digestion, lowering blood pres?sure, anti-depression, anti-oxidation, anti-inflammatory, and anti-parasites, antibacterial and other activities. The content of total phenols in fresh fruits of areca nut was 31.1％, mainly including catechin, isorhamnetin, chrysopanthoxanthin, luteolin, tannin and other polyphenols. The commonly used methods for determination of polyphenols in areca are vanil?lin titration potassium permanganate titration and potassium ferricyanide spectrophotometry. The main activities and mechanisms of areca polyphenols include: ① Antidepressant effect: polyphenols bind to monoamine oxidase type A (MAO-A) receptors that inhibit the production of neurotransmitters, thereby increasing the content of amine transmitters in the brain and playing a therapeutic effect on depression. ② Antioxidant effect: polyphenols contain multiple adjacent hydroxyl groups, which are easily oxidized and can effectively remove superoxide anion free radical, hydroxyl free radi?cal, 1,1-diphenyl-2-picrylhydrazyl radical, showing good antioxidant activity.③Bacteriostatic effect:polyphenols can spe?cifically bind to the surface of bacteria, thus achieving bacteriostatic effect. Studies have found that betel nut polyphenols have varying degrees of inhibitory effects on a variety of bacteria. ④ Inducing apoptosis of lymphocytes: polyphenols deplete the mercaptan in lymphocytes and make them unable to survive, thus inducing apoptosis of lymphocytes.⑤Anti-aging effect: polyphenols have the effect of anti-hyaluronidase and anti-elastase, so as to protect elastin fiber and pro?mote collagen synthesis.⑥Anti-allergic effect:studies have found that polyphenols can reduce ovalbumin induced aller?gic reactions.⑦Other functions:betel nut can freshen breath, eliminate bad breath, and resist the activity of cobra venom. At present, domestic and foreign scholars' research on betel nut mainly focuses on arecoline and its carcinogenicity, mutagenicity, effects on reproductive function, addiction and toxicity to the nervous system, and there are few studies on the positive effects of betel nut, especially on it. There is less research on phenolic ingredients. Therefore, this article reviews the polyphenolic chemical constituents of betel nut, and fully excavates its pharmacological activity to provide a reasonable basis for the scientific use of betel nut.

Research progress in mechanism of curcumin in treatment of Parkinson disease / 中国药理学与毒理学杂志

Curcumin (Cur) is an important bioactive component of polyphenols in the rhizomes of Curcuma longa L., Tulipa gesneriana L. and other Curcuma plants. It has a wide range of pharmacological effects such as anti-tumor, anti-atherosclerosis, anti-inflammatory, and neuroprotection. Parkinson disease (PD) is a neurodegenerative disease that often occurs in the elderly. Its main pathological characteristics are the characteristic loss of substantia nigra dopaminer?gic neurons, the decrease of dopamine content in the striatum, and the formation of Lewy bodies. At present, the main methods of clinical treatment of PD include drug therapy and surgical operation, but due to its complicated pathogene?sis, they can only play a role in relieving, but cannot be completely cured. Modern pharmacological studies have shown that Cur has certain effects in the treatment of PD. ① Anti-oxidative stress: oxidative stress is closely related to the degeneration of dopaminergic neurons. Studies have found that Cur can increase the activity of superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px), reduce malondialdehyde (MDA) content, thereby reducing oxidative stress damage and protecting dopaminergic neuron.②Reduce inflammation in brain tissue:neuroinflammation plays an impor?tant role in the development of PD. Reducing the level of inflammatory factors can have a certain therapeutic effect on PD. Studies have shown that high-dose Cur can reduce the levels of interleukin-6 (IL-6), IL-1β, and tumor necrosis fac?tor-α (TNF-α) in brain tissue, reduce inflammation, inhibit further neuronal damage, improve learning and memory, and exert neuroprotective effects. ③ Activation of autophagy: the abnormal accumulation of α-Synuclein (α-Syn) in Lewy bodies is closely related to PD, and autophagy dysfunction leads to α-Syn clearance obstacles and an important factor of abnormal aggregation. Cur can increase the expression of microtubule-associated protein 1 light chain 3 (LC3-Ⅱ) and lysosome-associated membrane protein 2A (LAMP2A), and reduce the protein and mRNA expression of α-Syn. It can be seen that Cur promotes the elimination ofα-Syn and protects neurons from damage by activating autophagy.④Inhi?bition of mitochondrial dysfunction:mitochondria plays a central regulatory role in the process of cell apoptosis, and mito?chondrial dysfunction is related to reactive oxygen species, energy and mitochondrial membrane potential, which may cause substantia nigra striatal neuropathy. Experiments have shown that Cur can reduce the active oxygen content in PC12 cells induced by MPP+, maintain the normal membrane potential of mitochondria, thereby stabilizing mitochondrial function and inhibiting PC12 cell apoptosis. This study summarized the action mechanism of Cur in the treatment of PD, and clarified the basis of its pharmacodynamics, providing a reference for the clinical research and new drug develop?ment research of Cur in the treatment of PD.

Study on pharmacological effect of Chuanxiong Rhizoma on vascular neuropathic headache / 中国药理学与毒理学杂志

Chuanxiong Rhizoma is the dry rhizome of Ligusticum chuanxiong in the umbelliferae family. Chuanxiong Rhizoma pungent, warm, go to liver, gallbladder and pericardium. Effective in promoting blood circulation, promoting Qi, dispelling wind and relieving pain, it could treat chest pain, tingling pain in chest and flank, lump, irregular menstruation, amenorrhea, symptomatic abdominal pain, headache and rheumatic pain. Neurovascular headache is a primary disease caused by dysregulation of intracranial vascular movement and nerve function. It has the characteristics of long course, intermittent recurrent attacks, lingering and difficult to heal. Attacks are often accompanied by many plant nervous sys?tem symptoms, such as rapid breathing, accelerated heart rate, vomiting, and gastrointestinal dysfunction. Vascular nerve headache is a common clinical disease, frequently bidity. Studies have shown that Chuanxiong Rhizoma has good pharmacological effects in the treatment of vascular neuropathic headache.① The action of Qi and blood circula?tion: vascular and neurovascular headache is caused by the evil of external wind and cold and damp heat, which leads to the disconnection of the veins, the disorder of Qi and blood, the obstruction of Qi and blood channels, the loss of brain collateral, and finally causes migraine. Modern Chinese medicine points out that"wind, blood stasis, deficiency, phlegm"are the key factors of the disease. Chuanxiong Rhizoma is the medicine of Qi in the blood. It is pungent and warm. It is good at activating blood and promoting Qi, dispelling wind, relieving pain and dispelling cold, so as to achieve the effect of treating vascular headaches. ② Improve brain circulation: angioneurotic headache is caused by dysfunction of the central nervous system related to the regulation of vascular movement, which causes vasospasm or extreme vasodi?lation, and the decrease of intracranial blood flow causes cerebral ischemia and hypoxia. Sodium ferulate is a chemical component in Chuanxiong Rhizoma. It has a relatively good inhibitory effect on platelet aggregation and the release of 5-HT from platelets. It can ensure the normal contraction of intracranial and extracranial blood vessels, improve the patient's brain circulation and nerve function, so as to achieve the effect of treating angioneurotic headaches.③Sedative and analgesic effect:the volatile oil and water decoction of Chuanxiong Rhizoma have sedative and analgesic effects, and the water decoction can counteract the excitatory effect of caffeine. Studies have shown that the ATP activa?tion current of rat dorsal root ganglion neurons can be inhibited by ligustrazine in a non-competitive way, which also indi?cates that Chuanxiong Rhizoma has a good analgesic effect. In this study, the effects of Chuanxiong Rhizoma on angoneeurotic headache were reviewed, and the pharmacological effects of Chuanxiong Rhizoma were further elucidated, providing basis for clinical application and new drug development of Chuanxiong Rhizoma in the treatment of angoneeu?rotic headache.

Progress in protective effect and mechanism of 6-gingerol on myocardial ischemia/reperfusion injury / 中国药理学与毒理学杂志

The morbidity and mortality of cardiovascular diseases are very high, which has attracted more and more attention all over the world. Common treatment methods for clinical treatment of acute myocardial infarction include direct percutaneous coronary intervention and coronary artery bypass grafting, which can quickly restore blocked coronary blood flow and reduce the infarct size. However, the inevitable ischemia/reperfusion injury will occur during the recovery of coronary blood flow, its pathological mechanism is complicated, and the Western medicine countermeasures are very limited. Among the current drugs for the treatment of cardiovascular diseases, traditional Chinese medicine has become a research hotspot due to its multiple targets, safety, and low side effects. Ginger is the fresh rhizome of Zingiber offici?nale Rosc., a perennial herbaceous plant in the ginger family. It is a dual-purpose resource of medicine and food. Ginger has the functions of relieving the appearance and dispelling cold, warming up and relieving vomiting, resolving phlegm and relieving cough, and relieving fish and crab poison. The chemical components of ginger mainly include volatile oil, gingerol, diphenylheptane, etc.. Among them, 6-gingerol, as the main active component of gingerols, has obvious phar?macological effects in myocardial protection, anti-oxidation, anti-inflammatory, etc.. Studies have shown that 6-gingerol protects myocardium mainly through anti-oxidative stress, anti-inflammatory, inhibiting cell apoptosis, and preventing cal?cium influx. ① Anti-oxidative stress: oxidative stress is a state where oxidation and anti-oxidation in the body are out of balance, and it is also an important factor leading to myocardial damage. Many studies have confirmed that 6-gingerol has an antioxidant effect, and it is considered a natural antioxidant. 6-gingerol can significantly reduce the degree of oxi?dative stress and the level of reactive oxygen species caused by cardiomyocyte damage, and has a significant cardiopro?tective effect. ② Anti-inflammatory: inflammation can cause substantial cell damage and organ dysfunction, which is another important cause of myocardial damage. 6-gingerol can reduce the levels of inflammatory factors such as inter?leukin-6, interleukin-1β, and tumor necrosis factor-αin cardiomyocytes, and at the same time inhibit the TLR4/NF-κB sig?naling pathway, an important regulatory pathway of inflammation, showing that it may improve myocardial damage through anti-inflammatory effects. ③ Inhibition of apoptosis: apoptosis is a complex and orderly process in the autono?mous biochemical process of cells, and one of the main mechanisms of myocardial injury. This process can be roughly divided into three pathways: mitochondria, endoplasmic reticulum, and death receptors. Among them, the mitochondrial pathway plays an important role, and Bcl-2 and Bax located upstream of this pathway can regulate the entire process of cell apoptosis by regulating the permeability of the mitochondrial membrane. Studies have found that the preventive application of 6-gingerol can reduce cell damage, reduce the number of apoptotic cells, reduce the activity of Bax and caspase-3, and increase the expression of Bcl-2. Therefore, 6-gingerol pretreatment can reduce the damage of cardio?myocytes, and its mechanism may be related to the inhibition of apoptosis.④Prevent calcium influx:calcium overload is involved in the pathogenesis of myocardial ischemic injury, which may be related to excessive contracture, arrhythmia, and mitochondrial Ca2+accumulation that impairs myocardial function. 6-gingerol inhibits the increase of intracellular Ca2+concentration by inhibiting L-type calcium current, thereby reducing extracellular Ca2+ influx, thereby avoiding calcium overload and playing a cardioprotective effect. In summary, 6-gingerol can effectively treat and improve myocardial isch?emia/reperfusion injury, and it has great development potential in the fields of medicine and health products.

Pharmacological effects of Schisandra Chinensis Fructus polysaccharide on intestinal protection / 中国药理学与毒理学杂志

Schisandra Chinensis Fructus (SCF) is the fruit of Schisandra chinensis (Turcz.) Baill., a perennial vine. It was first recorded in Shen Nong's herbal classic and has a long application history. Studies have shown that SCF has anti-inflammatory, protective liver, antioxidant, antibacterial and other pharmacological effects. Ancient prescriptions are commonly used in the treatment of chronic diarrhea and other intestinal diseases and diabetes. Modern clinical phar?macology features of SCF polysaccharide (SCFP) in diabetes, liver diseases, enteritis and other aspects have achieved excellent results. Gut is an important digestive organ of human body, but intestinal diseases are varied, including Crohn's disease, ulcerative colitis, intestinal flora imbalance, etc.. It is a chronic and non-specific inflammatory disease. The disease is persisted for a long time and the incidence rate is expected to rise. Most of the symptoms are recurrent diarrhea, bloody stool and abdominal pain. It is considered by the World Health Organization as a refractory disease. At present, there is little possibility of complete cure, which is closely related to complex environmental factors, eating hab?its and heredity. In recent years, clinical studies have found that SCFP has a variety of pharmacological effects on intes?tinal protection.①Reduce inflammatory factors:intestinal mucositis is a common adverse reaction in patients with chemo?therapy. The development of mucositis is related to pro-inflammatory factors such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), IL-1β, Interferon-γ(IFN-γ). SCFP can significantly reduce IL-6 TNF-α, IL-1β, and IL-8, as well as the accumulation of T cells in the process of resisting apoptosis, reduce the inflammatory reaction and protect the dam?age to villi and crypts, improve the symptoms of small intestinal mucositis caused by weight loss and diarrhea. ② Pro?mote immunoglobulin A secretion: intestinal mucosal immunity is the first line of defense of the body's immune system. Its main antibody is secretory immunoglobulin A, which can destroy and phagocytize microorganisms, bacteria and viruses. SCFP can improve intestinal immunity by increasing the number and activity of T lymphocytes, promoting the secre?tion of secretory immunoglobulin A, and affecting the activity of a variety of cytokines. ③ Regulation of intestinal flora:the flora in the intestine has the functions of auxiliary nutrient absorption, biological antagonism and immune regulation, and can form a natural barrier for the host's intestine. When the human intestinal flora is disordered, probiotics will be greatly reduced, harmful bacteria will proliferate and destroy the intestinal environment. Under these conditions, the intake of SCFP significantly increased the number of beneficial bacteria such as bifidobacteria and lactobacillus, and sig?nificantly decreased the number of conditional pathogens such as enterococcus and escherichia coli, indicating that SCFP can indeed regulate the intestinal disorder caused by lincomycin hydrochloride to a certain extent. This may be because beneficial bacteria in the intestine metabolize polysaccharides produce short chain fatty acids such as lactic acid and acetic acid, which reduces the pH value in the intestine and inhibits the growth of enterococcus and Escherichia coli. In conclusion, SCFP can treat and protect intestinal diseases to a certain extent, which provides a favorable basis for the treatment of intestinal diseases.

Pharmacological effects of volatileoil from Alpinia officinaruim in treating cardiovascular diseases / 中国药理学与毒理学杂志

Galangal (Alpinia officinaruim Hance) is the rhizome of the perennial herb belonging to Zingiberaceae family. There are many active components in galangal, such as volatile oil, flavonoids, terpenoids, phenylpropanoids and glycosides, among which the content of volatile oil is higher. The bioactivities of galangal volatile oil on health effect includesanti-inflammatory, anti-hypertension, anti-oxidation and prevention of cardiovascular diseases. Cardiovascular disease (CVD) is a kind of diseases related to circulatory system, which is also called circulatory system diseases. Over the past decade, the number of people dying from CVD has increased by 12.5％ worldwide, and it is now the leading cause of human death worldwide. Studies have shown that galangal volatile oil has good pharmacological effects in treating CVD. ① Regulation of glucose and lipid metabolism: studies have found that abnormal lipid metabolism can lead to obesity, diabetes, CVD and other diseases. The serum total triglyceride (TG) content in liver and serum will increase in patients with abnormal fat metabolism. The results showed that the volatile oil of galangal could increase the excretion of neutral cholesterol, significantly reduce liver TG and serum TG, and thus regulate glucose and lipid metabo?lism, prevent lipid deposition and prevent CVD. ② Improving insulin resistance (IR): inhibition of inflammatory cytokines such as IL-1, IL-6 activation and expression of TNF-α, improves IR, thereby protecting myocardium from IR-mediated damage. Through the establishment of endothelial cell injury model induced by high glucose in vitro, it was found that the volatile oil of galangal can significantly reduce the secretion of pro-inflammatory cytokines TNF-αand IL-8, and inhib?it the expression of ICAM-1 and VCAM-1 induced by high glucose, suggesting that it has protective effect on endothelial dysfunction and inflammation induced by high glucose.③Regulate blood oxygenation:during acute myocardial hypoxia, the activity of free radical scavenging system is decreased, and oxygen free radicals are produced in large quantity, which reacts with unsaturated fatty acids on the cell membrane and forms lipid peroxidation, resulting in myocardial structural damage. The results showed that the water extract of Galangal could reduce the content of MDA in blood and protect the SOD activity of ischemic and hypoxic myocardium.④ Protective effect of vascular endothelial cells (ES):ES injury is the pathological basis of some cardiovascular diseases. The results showed that the volatile oil of galangal had a protective effect on ES apoptosis. Compared with the morphology and activity of ES treated with oxidized LDL, galan?gal volatile oil could ameliorate these morphological changes and improve cell viability. ⑤ Antiplatelet agglutination:inhibit platelet aggregation and thromboxane release, improve blood circulation, and have obvious anti-thrombotic effect, which has a good effect on the treatment and prevention of cardiovascular diseases. The results showed that the volatile oil of galangal had inhibitory effect on platelet aggregation and anticoagulant effect. In conclusion, the volatile oil of galangal can be used to prevent and treat cardiovascular diseases. Based on the mechanism of CVD, this study summa?rized the role of the essential oil of Alpinia officinaruim in CVD, providing basis for the clinical application of alpiniaoffici?nalis essential oil in the prevention and treatment of CVD and the development of new drugs.

UPLC Fingerprint Analysis of Acanthopanacix Cortex from Different Origins / 中国实验方剂学杂志

Objective::To established fingerprint of Acanthopanacix Cortex by UPLC method, in order to provide reference for quality control and evaluation. Method::UPLC method was performed on Waters BEH C18 (2.1 mm×100 mm, 1.7 μm), with acetonitrile-0.1% glacial acetic acid as the mobile phase for gradient elution.The detection wavelength was 282 nm, the flow rate was 0.3 mL·min-1, the column temperature was 25 ℃, and the injection volume was 2 μL.With syringin as reference substance, the fingerprint of 20 batches Acanthopanacix Cortex were analyzed under the same chromatographic conditions.The Similarity Evaluation System for Chromatographic Fingerprint of Chinese Materia Media (version 2012) was used to analyze the similarity of 20 batches of Acanthopanacix Cortex, and the SPSS 21.0 was applied for cluster analysis. Result::The UPLC fingerprint of the Acanthopanacix Cortex was established.The similarity results showed that the 7 batches of the 20 batches of Acanthopanacix Cortex was less than 0.800, and the remaining medicinal materials were similar within the range from 0.800 to 0.924.Besides, 12 common fingerprint peaks were calibrated and 4 components were identified, namely protocatechuic acid (peak 1), chlorogenic acid (peak 3), syringin (peak 4), and 4-methoxysalicylaldehyde (peak 12). The clustering results showed that the 20 batches of Acanthopanacix Cortex were divided into four groups.Among these batches, S1, S3, S9, S13 and S20 were clustered into one category, S11 was a category, S14 was a category, and the remaining samples belonged to a category. Conclusion::With a good precision, repeatability and stability, short analysis time as well as superior specificity, the method will provide a scientific basis to evaluate and control the quality of Acanthopanacix Cortex.

New situation and new strategies——research and development and internationalization of new drugs and health products of traditional Chinese medicine / 中国药理学与毒理学杂志

The 2017 China (Lianyungang) International Medical Technology Conference was held in Lianyungang,Jiangsu Province during November 15-17,2017.During this conference,the Division for Traditional Chinese Medicine and Natural Products Pharmacology of Chinese Pharmacological Society (CNPHARS) and Jiangsu Kanion Pharmaceutical Co. Ltd.jointly held the Forum on R&D and Interna-tionalization of New Drugs and Health Products of Traditional Chinese Medicine.The forum was co-chaired by Professor ZHANG Yong-xiang, President of CNPHARS, Chair of Division for Traditional Chinese Medicine and Natural Products Pharmacology of CNPHARS,and Chair of the Natural Product Section of Inter-national Union of Basic&Clinical Pharmacology(IUPHAR), Professor DU Guan-hua,former President of CNPHARS and Vice-Chair of Division for Traditional Chinese Medicine and Natural Products Pharmacology of CNPHARS,and Dr.XIAO Wei,Chairman of the Board of Jiangsu Kanion Pharmaceutical Co. Ltd. And Vice-Chair of Division for Traditional Chinese Medicine and Natural Products Pharmacology of CNPHARS. More than 70 scholars attended the forum, including four foreign experts [Michael SPEDDING, Secretary-General of IUPHAR; Professor Valérie B. SCHINI-KERTH, Vice-Chair of the Natural Product Section of IUPHAR; Professor Cherry WAINWRGHT, Director of Centre for Natural Product Drugs of Robert Gordon University; Professor InKyeom KIM, Director of the Korean Society of Pharmacology], members of the Division for Traditional Chinese Medicine and Natural Products Pharmacology of CNPHARS and leading researchers at Jiangsu Kanion Pharmaceutical Co.,Ltd.GU Jin-hui,Director of the Division of National Science and Technology Major Project for Drug Innovation,Department of Health Science,Technology and Education,National Health and Family Planning Commission of the People's Republic of China was also invited to attend the forum. Representatives discussed the R&D and internationalization of new drugs and health products of traditional Chinese medicine.The summary of views and advice of some experts was published here for the purpose of promoting domestic and overseas academic exchange, and playing an active role in improving the level of R&D and internationalization of new drugs and health products of traditional Chinese medicine in China.

Effects of Jiji decoction on the cognitive function and oxidative stress in mice with vascular dementia induced by cerebral ischemia/reperfusion / 中国应用生理学杂志

<p><b>OBJECTIVE</b>To determine the effects of Jiji decoction (Traditional Chinese Medicine) on the cognitive function and oxidative stress in mice with vascular dementia (VD) induced by cerebral ischemia/reperfusion.</p><p><b>METHODS</b>Thirty-two mice were randomly divided into nonnal group (n = 8), sham group (operation, but no cerebral ischemia/reperfusi6n, n = 8), model group (vascular dementia model induced by cerebral ischemia/reperfusion, n = 8), and Jiji decoction-treated group (vascular dementia model plus treatment with Jiji decoction, n = 8). Fourteen days of treatment after operation, the cognitive behavior was measured in step-through test, spatial probe test and platform test. Afterwards, to assess the levels of oxidative stress, the activity of superoxide dismutase(SOD) and content of malonaldehyde (MDA) in brain of these mice were measured.</p><p><b>RESULTS</b>Data from step-through test indicated that the escaping latency of Jiji decoction-treated group was prolonged and the error counts were decreased significantly ( P <0.01) compared with those of model group. Data from spatial probe test indicated that the time of entering darkroom, the time of climbing height and the time of entering bright room in Jiji decoction-treated group were shortened and the counts of climbing height were increased (P < 0.05-0.01) significantly compared with those of model group. Data from platform test showed that the escaping latency of Jiji decoction-treated group was prolonged significantly (P < 0.01) compared with that of model group. Compared with normal and sham group, the activity of SOD was decreased and the content of MDA was increased in model group significantly (P < 0.01). Compared with those of model group, the levels of SOD and MDA in Jiji decoction-treated group were improved significantly (P < 0.01).</p><p><b>CONCLUSION</b>Jiji decoction could improve cognitive function of VD mice. Its mechanism might be related with the inhibition of oxidative stiess in the brain.</p>

Differential gene expression profiles of DNA repair genes in esophageal cancer cells after X-ray irradiation / 癌症

<p><b>BACKGROUND AND OBJECTIVE</b>Various factors affect the radioresistance of tumor cells, with unknown molecular mechanism(s). Many genes have been found to associate with the radioresistance of tumor cells, however, the precise mechanism of these genes have not been elucidated. This paper was to analyze the differential expressions of DNA repair genes in esophageal carcinoma cells at different time after X-ray irradiation, and to investigate the role of these DNA repair genes in radiation resistance.</p><p><b>METHODS</b>Esophageal cancer parental cells Seg-1 were treated with continuous 2 Gy of fractionated irradiation until the total dose reached 60 Gy to establish the radioresistant cell line Seg-1R. Total RNA was extracted from each cell line at 0, 8, and 24 h after irradiation. Illumine Human-6 V3 microarray was used to identify differentially expressed genes between parental and radioresistant cells. Ten genes involved in DNA repair were obtained and their expressions at different time points after irradiation were analyzed by Gene Ontology analysis.</p><p><b>RESULTS</b>Ten DNA repair associated genes were found to be differentially expressed. Three of these genes, SLK, HMGB1, and PMS1, were not only differentially expressed between parental and radioresistant cell lines, but also expressed differently at different time points after irradiation in the same cell line.</p><p><b>CONCLUSIONS</b>PMS1 may be an important factor involved in the mechanism of radioresistance of esophageal carcinoma cells.</p>

High throughput screening for glutathione S-transferase inhibitors / 药学学报

To identify the inhibitor of glutathione S-transferase (GST), a high-throughput screening method was established in a 384-well microplate with total 35 microL volume, and the absorbance at 340 nm is detected. The concentrations of substrates, CDNB and GST were determined by chromatometry. The optimal enzyme kinetics reaction time and temperature are 2 h and 30 degrees C , respectively. The established model was evaluated by NaOCl, a known GST inhibitor, and the parameter Z' was 0.77, which showed a high feasibility and stability of the assay. A total of 31,098 compounds were screened, of which 4 compounds were shown to inhibit GST activity, high inhibiting activity for their IC50 of GST inhibition was 3.94, 4.05, 74.85, and 77.41 mg x L(-1), separately. The results indicated that the colorimetric method by using CDNB and GSH as substrate is stable, sensitive, reproducible and also suitable for high throughput screening.

Relation between adenosine A1 receptor and NMDA receptor on synaptic transmission in dentate gyrus of hippocampus / 药学学报

<p><b>AIM</b>To observe the effect of adenosine A, receptor antagonist on synaptic transmission in the dentate gyrus of hippocampus and its relations with NMDA receptor.</p><p><b>METHODS</b>Using electrophysiological technique to record the long-term potentiation (LTP), the relation between selective adenosine A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) and NMDA receptor agonist/antagonist, in both basic synaptic transmission and 200 Hz high-frequency stimulation (HFS) induced LTP of the dentate gyrus of hippocampus in anesthetized rats, was studied.</p><p><b>RESULTS</b>DPCPX (6 mg x L(-1), 5 microL, icv) or NMDA (0.2 mg x L(-1), 5 microL, icv) was shown not to affect the synaptic transmission in the dentate gyrus in rats. DPCPX was found not to affect the keeping of LTP induced by HFS after icv NMDA. But the basic synaptic transmission and the magnitude of LTP induced by HFS in the dentate gyrus after icv NMDA could be enhanced significantly by icv DPCPX in advance. DPCPX could not affect the magnitude of LTP inhibited by AP5 (0.5 mg x L(-1), 5 microL) NMDA receptor antagonist, but the inhibitory effect of AP5 on LTP could be antagonized by icv DPCPX in advance.</p><p><b>CONCLUSION</b>The selective adenosine A1 receptor antagonist DPCPX could not affect the synaptic transmission in the dentate gyrus of hippocampus, but could significantly enhance the effect of NMDA receptor in both basic synaptic transmission and HFS induced LTP in the dentate gyrus of hippocampus in anesthetized rats.</p>

Effect of adenosine A1 receptor antagonist on learning and memory and analysis of its mechanism / 药学学报

<p><b>AIM</b>To study the effect of blocking adenosine A1 receptors on learning and memory and the relation with cholinergic and aminoacidergic nerve.</p><p><b>METHODS</b>Using step through test, spectrophotometry and HPLC method, the effect of selective adenosine A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX, 0.3, 0.15, 0.075, 0.03, 0.015 microgram, icv) on memory impairment by scopolamine (Scop, 3 mg.kg-1 i.p.) or 2-amino-5-phosphonovaleric (AP5, 2.5 ng, icv), acetylcholinesterase (AChE) activity and aminoacid level in brain of mice was studied.</p><p><b>RESULTS</b>DPCPX was shown to significantly improve scopolamine-induced memory impairment, but not AP5-induced. The activity of AChE in mouse brain was significantly inhibited by large doses of DPCPX in vitro and in vivo test. DPCPX(0.3 microgram, icv) was shown to significantly increase the content of glutamate and aspartic acid in brain of mice. DPCPX (0.3, 0.15 microgram, icv) significantly decrease GABA and increase Glu/GABA in brain of mice.</p><p><b>CONCLUSION</b>The selective adenosine A1 receptor antagonist DPCPX was shown to significantly improve scopolamine but not AP5-induced memory impairment. Large doses of DPCPX was shown to influence the AChE activity and the changes in aminoacid level in brain, especially increase Glu/GABA.</p>

Pharmacokinetics of osthole in rabbits / 药学学报

<p><b>AIM</b>To investigate the pharmacokinetics of osthole in rabbits and obtain the main pharmacokinetic parameters.</p><p><b>METHODS</b>A simple high-performance liquid chromatography (HPLC) method was developed to study the pharmacokinetics of osthole in rabbits by joining an internal standard (paeonal). Methanol-water (80:20) was used as the mobile phase. According to the 3P87 pharmacokinetic program, the main parameters were calculated.</p><p><b>RESULTS</b>The osthole pharmacokinetics conforms to a two compartment open model after i.v. administration, T1/2 alpha = 5.81 min, T1/2 beta = 42.2 min, K21 = 0.036 0.min-1, K12 = 0.045 0.min-1, K10 = 0.054 0.min-1, AUC = 235 mg.min.L-1, CLs = 0.043 0 L.min-1.kg-1, Vc = 0.780 L.kg-1.</p><p><b>CONCLUSION</b>The pharmacokinetics of osthole after i.v. administration showed a rapid distribution and elimination process in rabbits.</p>

Effect of osthol on memory impairment of mice in AlCl3-induced acute senile model / 药学学报

<p><b>AIM</b>To study the protective effect and mechanism of osthol on learning and memory impairment of mice with acute senile model induced by AlCl3.</p><p><b>METHODS</b>After s.c. AlCl3 60 mg.kg-1 for 7 d and i.p. osthol 15 and 7.5 mg.kg-1 for 12 d, using step-through test and step-down test, the effect of osthol on learning and memory was observed and the glutathione peroxidase (GSH-PX) activities in blood and superoxide dismutase (SOD) activities in plasma and cerebrum were measured.</p><p><b>RESULTS</b>Osthol 15 and 7.5 mg.kg-1 significantly improved the capability of memory and enhanced the activities of GSH-PX and SOD in AlCl3 treated mice.</p><p><b>CONCLUSION</b>Osthol shows protective effect on brain memory impairment of mice in acute senile model induced by AlCl3. Perhaps the mechanism is involved in enhancing the activities of GSH-PX and SOD, clearing away the free radical, protecting the brain neuron from the harm of lipoperoxide.</p>