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

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

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

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

Esophagus ; Foreign Bodies ; Humans ; Infant ; Male

Desensitization, Immunologic ; methods ; Humans ; Injections, Subcutaneous

Objective To investigate the dual pharmacology characteristics of a new structural telmisartan derivative Tek- 1 based on angiotensin II (ANGII) receptor I (AT1) and peroxisome proliferator-activated receptor-γ (PPARγ) and the influence of Tek- 1 on blood pressure in spontaneously hypertensive rats (SHR). Methods The AT1 receptor affinity of Tek- 1 was explored through radioligand binding assay on rat primary vascular smooth muscle cells; the PPARγ agonistic activity of Tek-1 was explored using PPARγ-responsive element-luciferase report assay; the antagonistic effect of Tek-1 on AT1receptor activation induced by ANGII was explored using intracellular calcium mobilization detection assay; the effect of Tek-1 on the regulation of systolic blood pressure (SBP) was evaluated in SHR in vivo. Results Tek-1 and telmisartan had high affinity to AT1 receptor, their Ki values for AT1 receptor were 1.1×10-9 and 2.3×10-10mol/L, respectively. Tek-1 and telmisartan could activate PPARγ ranging from 0.1 to 10 μmol/L in a concentration-dependent manner. The relative lucifarase activity induced by Tek-1 and telmisartan were 1.56±0.08 and 1.39±0.14 fold at 10 μmol/L. Compared with solvent group, the effect of AT1 agonist ANGII were inhibited by Tek-1 in a concentration-dependent manner with IC50 value of 1.02±0.1 nmol/L ranging from 0.0128 to 1 μmol/L. SHR were randomly administered telmisartan (5 or 10 mg/kg) and Tek-1 (1 mg/kg, 5 mg/kg or 10 mg/kg) orally each day for one week every day. After 1-week treatment, compared with the baseline SBP and DBP in the pretreatment of SHR, telmisartan in the dose of 5 and 10 mg/kg both showed significantly decreased SBP (P < 0.01) and DBP (P < 0.05). Tek-1 in the dose of 1, 5 and 10 mg/kg also significantly decreased SBP (P < 0.05); however, only the high dose of 10 mg/kg Tek-1 showed a significant decrease in DBP (P < 0.05). Conclusion Tek-1 Behaveds as an ATI blocker with partial PPARγ agonist activity in vitro and attenuates the blood pressure in SHR in vivo.