The study of peptide drugs has been an important direction in research and development of new drugs. However, lots of natural macromolecular peptides are limited in clinical use by their metabolic instability and low bioavailability. In recent years, the active small peptidomimetics open up a new hotspot of peptide drug development with the characteristics of low molecular weight, high bioactivity and structural modification. Many peptidomimetics are on the market or on the clinical study. This paper elaborated the small peptidomimetics approved by American Food and Drug Administration (FDA) from 2005 to 2014, and reviewed their researching status with source, synthetic method, chemical structure, marketing time, indication, clinical efficacy and safety. Research prospects in this field were discussed.
Biomedical Research ; trends ; Peptidomimetics ; United States ; United States Food and Drug Administration

Objective: To investigate the effect of different degrees of ischemic white matter lesions on the cognitive function in patients with lacunar infarction. Method: One hundred twelve consecutive patients with lacunar infarction were collected. Age-related white matter changes rating scale (ARWMCRs) was used, and according to the results of ARWMCRs scores, the patients were divided into mild (n = 34, 0-3 scores), moderate (n = 43, 4-7 scores), and severe (n = 35, 8-24 scores) groups. The national health institutes of stroke scale (NIHSS) and the modified Rankin scale (mRS) scores were used to assess the degree of neurological deficit. The mini-mental status scale (MMSE) and the Montreal Cognitive Assessment (MoCA) were used for neuropsychological tests, and event-related potential two-tone sequence auditory P300 (2t-P300) wave was used for neural electrophysiological examination. The cognitive function was evaluated. The cognitive function among all groups was compared. Results: Circled digit oneThere were significant differences in comparison of the MoCA scores among the three groups. Only the mRS score and the MMSE score in the severe group were lower than those in the mild and moderate groups. There were significant differences (P < 0.05). Circled digit twoThe latency of P300 wave in the severe group was higher than that in the moderate and mild groups, and the latency of P300 wave in the moderate group was higher than that in the mild group. There was significant difference (P <0.05). The amplitude of P300 wave in the severe group was lower than that in the moderate group and mild group. There were significant differences (P < 0.05). Circled digit threeThe ARWMCRs score in patients with white matter lesions was negatively correlated with the MMSE score, MoCA score, and amplitude of P300 wave. It was positively correlated with the latency of P300 wave and mRS score. Conclusion: White matter lesions impact the cognitive function in patients with lacunar infarction. The more severe the white matter lesions, the more significant decline in cognitive function.

Mathematics ; Models, Theoretical ; Occupational Health Services ; organization & administration ; Risk Assessment ; methods

Esophagus ; Foreign Bodies ; Humans ; Infant ; Male

Genetic Techniques ; Genomics ; Humans ; Nucleic Acid Amplification Techniques ; Nucleic Acid Hybridization ; Sequence Analysis, DNA ; Viruses ; genetics ; isolation & purification

Adolescent ; Adult ; Female ; Humans ; Male ; Mercury Poisoning ; diagnosis ; therapy ; Middle Aged ; Occupational Diseases ; diagnosis ; therapy ; Retrospective Studies ; Young Adult

Desensitization, Immunologic ; methods ; Humans ; Injections, Subcutaneous

Danshen is one of the traditional Chinese herbal medicines and nas a long history or being used clinically in the treatment of cardiovascular and cerebrovascular conditions such as coronary heart disease and angina pectoris. Tanshinone IIA is a derivative of phenanthrene-quinone isolated from Danshen. It has been reported to be the major bioactive compound of Danshen and has diverse biological effects. Recent studies demonstrated that tanshinone IIA had neuroprotective effects on experimental ischemic stroke through its antiinflammatory, anti-oxidant, anti-apoptosis effects and its inhibitory effect on excitatory amino acid toxicity. In this review, we summarized all the recent progresses on the protective effect of tanshinone IIA on cerebral ischemic stroke. Hopefully, this article will throw some light on further study and application of tanshinone IIA.
Antioxidants ; therapeutic use ; Apoptosis ; Diterpenes, Abietane ; therapeutic use ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Salvia miltiorrhiza ; chemistry ; Stroke ; drug therapy

Aged ; China ; Confusion ; drug therapy ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Medicine in Literature

Objective: To prepare Gualou-Xiebai intragastric floating pellets(18-24 mesh)by extrusion-spheronization method, and investigate their release characteristics in vitro. Methods: Using the floating time of pellets as indicator and the percentage of microcrystalline cellulose (MCC), octadecanol, hydroxypropyl methylcellulose- K4M (HPMC-K4M)and HPMC-K15M in the solid excipients of the prescription as affecting factors on the basis of single factor experiments, the formulation was optimized by star design-response surface optimization method. Taking the content of 3, 29-dibenzoyl karounitriol in the release medium as the index, the release rate of the pellets in vitro was determined and the release characteristics were explored. Results: The optimum prescription of these pellets was as follows: Gualou-Xiebai dry extract 25 g, MCC 6 g, octadecanol 11 g, HPMC-K4M 3 g, HPMC-K15M 11 g, 70% ethanol solution as wetting agent, and 40% polyvinylpyrrolidone(PVP-K30)solution as binder. The floating time in vitro of the pellets prepared by this prescription was 12 hours, and the cumulative release rate data fitted well with the first-order release model (r>0.97). Conclusion: The Gualou-Xiebai intragastric floating pellets prepared in this study had good floating property and sustained release effect, indicating that the preparation method is feasible.