In recent years,with the completion of the Human Genome Project and the development of mapping the Human Ge?nome Methylation Variable Site Map Plan,research on epigenetics and the generation and deveopment of cancer,epigenetic treatment drugs,especially the successful clinical application of the DNA methyltransferase and histone deacetylation inhibitors in the treatment of cancer patients,epigenetic has becoming a hot spot. This article reviews the recent progress in pharmacological action of epigenetics-based anticancer drugs,it may provide some new ideas to the therapy and fundamental research of cancer.

Pediatric drug accessibility has become a global problem,pediatric drug shortages and off-label uses are very seri?ous. In China,lack of suitable varieties,appropriate dosage forms and specifications,weak foundations on clinical trials,irregular prescribing behavior and irrational drug use and other issues on pediatric drugs are still outstanding. To improve pediatric drug accessi?bility,it may need all aspects work together,that is,cooperation of the national macro-policy support,participation of enterprises and medical institutions,to establish realistic goals and programs to address pediatric drug problem. This paper studies the foreign pediat?ric regulation measures and policies and by comparing foreign policies to China′s current situation,we can find out the problems and defects,give appropriate advice,in order to provide advice and reference to promote the development of pediatric drug.

In the first half year of 2016,the U.S. food and drug administration(FDA)approved 9 new molecular entities and 8 new biologic license applications. According to the prescription information for professionals,this article introduces the description, mechanism of action and clinical studies;briefly describes the box warning,indications and usage,dosage and administration,dos?age form and strength,contraindications,warning and precautions,adverse reactions,drug interaction and use in special population of these new drugs. In addition,the first and critical events in the history of new drug development and reaserch are emphasized.

Tamarindus indica Linn. tamarinds,belonging to the family Caesalpiniaceae,is a kind of large subtropical ever?green tree. Every part of tamarind has rich nutritional value and broad usage in traditional medicine since ancient times. Recent studies suggest extraction of leaves,flesh,seeds,and velamina of T. indica Linn. have numerous biological activities such as anti-microbial, anti-inflammatory,detoxification,analgesic,antidiabetic and anti-hyperlipidemiactions. A great interest has been seen in various sec?ondary metabolites isolated and identified from chemical components of T. indica Linn. In this review article,we summarize recent achievement in chemical components and biological activities of T. indica Linn.,aiming to provide a useful reference for further study and exploitation of T. indica Linn..

Parkinson′ s disease(PD) is a common, progressive, multicentric neurodegenerative disorder of insidious onset. This article reviews the research advances of PD, including pathogenic mechanisms, risk factors, epidemiology, incidence, diagnosis, prevention and treatment, representative drugs marketed and in development for the treatment of PD are also summarized.

α-Amino-3-hydroxyl-5-methyl-4-isoxazole propionic acid (AMPA) receptor, a subtype of ionotropic glutamate receptors widely distributed in the central nervous system, mediates the fast excitatory neurotransmission. Meanwhile more and more evidence indicates that AMPA receptor plays an important role in synaptic plasticity as well as central sensitization, and it also has close relationships with nervous system diseases. Over stimulation of AMPA receptor would produce excitotoxicity, leading to neuronal damage and finally resulting in a multitude of nervous system diseases, such as epilepsy, amyotrophic lateral scelerosis,Parkinson′s dis-ease. Competitive AMPA receptor antagonists that downregulate AMPA receptor′s function are of great importance in the prevention and treatment of nervous system diseases. This article reviews the research advances of competitive AMPA receptor antagonists.

Parkinson′s disease(PD)is a common disease caused by multiple factors and characterized by pathological degen?eration in the dopaminergic neural system. Based on its pathogenic factors,PD can be divided into several subtypes,so it is essential to develop therapeutic agents based on the main pathogenic factor of each subtype of PD. Recently it is confirmed that the mutation of leucine-rich repeat kinase 2(LRRK2)gene leads to increased activity of the LRRK2 notably,and then causes neurodegeneration. Thus developing LRRK2 inhibitors to modulate the kinase activity will be a novel therapy for the PD subtype which is caused by LRRK2 gene mutation. LRRK2,either a kinase or a GTPase,has two drug binding sites. Therefore,two types of LRRK2 inhibitors are being studied,one is the kinase inhibitor and the other is GTPase inhibitor. This paper summarizes the recent progress in the dis?covery and development of LRRK2 inhibitors.

Gut microbiota(GM)consists of a complex community of microorganism species that live in the digestive tracts of animals including humans. Dysbiosis is believed to involve in the development of some diseases. Recently dysbiosis in the patients with Alzheimer′s disease(AD)and AD rat models was reported. GM may influence the pathogenesis and development of AD in several ways. Some neurotoxic substances produced by GM can invade into the brain via circulation and impair the neural functions. These sub?stances include ammonia,cyanobacteria-producedβ-N-methylamino-L-alanine,saxitoxin,anatoxin-αand amyloid. The decrease in brain-derived neurotrophic factor(BDNF)in hippocampus and cerebral cortex induced by dysbiosis contributes to the cognitive dys?function. Dysbiosis related endotoxin can induce inflammation,which is one important risk factor for obesity,insulin resistance(IR) and type 2 diabetes mellitus(TIDM). AD and diabetes have good correlation and similarity. Probiotics,prebiotics and Chinese herbal medicines can rebuild GM and have been reported to ameliorate the memory loss of AD patients or model rats. However ,whether and how their preventative and therapeutic effects on AD mediated by GM are worthy of further investigation.

Objective To research the protective effect of Ento-Ⅰagainst cerebral ischemia-reperfusion injury in rats,and to evaluate its analgesic and anticoagulating effects in mice. Methods The ischemic model was established with line embolism to block the middle cerebral artery of male rats. The 56 rats were randomly assigned into 7 groups of sham-operation,blank-matrix,nor?
mal saline,Ento-Ⅰplastic of 3 doses(6.67,3.33,1.67 mg/kg),and ozagrel sodium(8.3 mg/kg,ip). The effect of Ento-Ⅰplastic on anti-cerebral ischemia was measured by nervous function scores and the areas of cerebral infarction were determined by TTC staining for the calculation of cerebral infarction rates. The analgesic effect of Ento-Ⅰplastic was determined with acetic acid-induced twisting experiment. Sixty KM mice were randomly allocated into blank-matrix,aspirin,aspirin-plastic,and Ento-Ⅰplastic of 3 doses(5,10 and 20 mg/kg),the number of mouse twisting were recorded right after intraperitoneal injection of 0.7%acetic acid solution at the time of 1 h after the last administration. Moreover,the anticoagulant activity of Ento-Ⅰplastic was tested by glass capillary method. Re?sults The results of acetic acid-induced twisting experiment displayed that Ento-Ⅰplastic of all 3 dose groups(5,10 and 20 mg/kg) could significantly reduce the number of body torsion and increase the inhibitory rates of twisting,compared with that of blank matrix group(the inhibitory rates of twisting for 3 dose groups were 21.79%,48.89%,and 56.15%,respectively),with dose-response man?ner. According to the results of glass capillary test,the clotting time of mouse blood could be significantly prolonged by mid-(10 mg/kg)and low-dose(5 mg/kg)of Ento-Ⅰplastic with corresponding clotting time of(155.20±54.19)s and(155.80±73.84)s,compared with normal saline group at(92.10 ± 24.61)and blank-matrix group at(80.40 ± 48.09,P<0.05). The experiment results of the isch?emia-reperfusion injury by line embolism method in rats exhibited that Ento-Ⅰplastic in mid-dose(3.33 mg/kg)could significantly re?duce the neurological scores after 24 h of reperfusion injury,from(2.33 ± 0.52)of normal saline group to(1.00 ± 0.00)of mid-dose group(P<0.01). The results from TTC staining revealed that the cerebral infarction rates of normal saline group and blank-matrix group were(24.89±7.24)%and(27.72±7.89)%,respectively,whereas those of 6.67 mg/kg and 3.33 mg/kg group of Ento-Ⅰplastic were(14.01±2.65)%and(14.73±4.94)%,respectively. Compared to the 2 negative-control groups,both the high-and mid-dose of Ento-Ⅰplastic could significantly reduce the cerebral infarction rates after ischemic reperfusion injury in rats (P<0.01). Conclu?sion Ento-Ⅰplastic demonstrates strong analgesic and anticoagulant effects,and could substantially reduce the neurological scores and reduce cerebral infarction rates for ischemia-reperfusion injured rats. These are likely to be the mechanism of action for Ento-Ⅰplastic realizing its anti-cerebral ischemia effect.

Epilepsy,especially the status epilepticus(SE),is a kind of common disease which is seriously dangerous for peo-ple′s health. At present,many researchers are focusing on how the epilepsy seizures happen and maintain,but know little about how it stops. It was found that appropriate cell acidification played an important role in patients to slow down or inhibit epilepsy-like seizures in the early 20th century. Recently,more and more researches have confirmed that cell acidification can induce the termination of epi-leptic seizure caused by disbalance of inhibitory and excitatory transmitters of nerve,opening of acid-sensing ion channels and so on. Therefore,these will likely become the new direction to explore new drugs or methods for epileptic treatment in the future.