1.Design, synthesis and antidiabetic activity of novel tetrahydrocarboline PPAR regulators.
Kun PENG ; Yi HUAN ; Quan LIU ; Zhufang SHEN ; Zhanzhu LIU
Acta Pharmaceutica Sinica 2014;49(4):490-6
A series of novel tetrahydrocarboline derivatives was designed and synthesized in order to discover more potent peroxisome proliferator-activated receptor (PPAR) alpha/gamma dual regulators. The structures of these compounds were confirmed by 1H NMR and HR-MS; their PPAR-regulating activities were evaluated in vitro. Compounds 6h, 6n, 6p and 6q exhibited more potent PPARalpha agonistic activities than the control drug WY14643, while compounds 60, 6g, 6i and 6q exhibited more potent PPARgamma agonistic activities than the control drug rosiglitazone. Compound 6q was discovered as a potent PPARalpha/gamma dual agonist and deserves further investigation.
2.Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives.
Ran YU ; Yanli ZHOU ; Yi HUAN ; Quan LIU ; Zhufang SHEN ; Zhanzhu LIU
Acta Pharmaceutica Sinica 2011;46(3):311-6
A series of tetrahydroisoquinoline derivatives were prepared and their peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonistic activities were evaluated to obtain more potent PPAR agonist. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Three compounds exhibited higher agonistic activities of PPARgamma than that of the comparison, six compounds exhibited higher agonistic activities of PPARalpha than that of the comparison, and compound 8a was discovered as a highly potent PPARalpha/gamma agonist that is much more active than that of WY14643 and rosiglitazone. The development of potent PPAR agonists may offer a new choice for the treatment of diabetes.
3. Minimal invasive subcutaneous internal fixator in treatment of anterior pelvic ring instability-analysis of effects and complications
Haiwei YAN ; Juzheng HU ; Ying YANG ; You XIE ; Zhanzhu HUANG ; Xiaosong CHENG ; Lu WEI ; Yansong FENG ; Boyu LIU ; Zhanying SHI
Chinese Journal of Orthopaedics 2019;39(13):826-832
Objective:
To investigate the incidence of complications following minimal invasive subcutaneous internal fixator (INFIX) for the treatment of anterior pelvic ring instability, and to analyze control measures.
Methods:
Data of 42 patients with anterior pelvic ring instability who were treated by anterior subcutaneous internal fixation in our hospital from January 2016 to December 2017 were retrospectively analyzed. There were 15 females and 27 males with an average age of 45.4 years (range, 18-67 years). There were 26 traffic injuries, 10 falling injuries, 3 crush injuries and 3 low energy injuries. According to Tile classification, 24 cases of B2 type, 16 cases of B3 type, 1 case of C1 type and 1 case of C2 type. According to Young-Burgess classification, there were 20 cases of LCI, 18 cases of LCII, 1 case of LCIII, 1 case of APCI, 1 case of APCII, and 1 case of VS. Fourteen cases were combined with limb fractures, and 11 cases were combined with thoracic or abdominal injuries requiring surgical treatment, while 16 cases were with brain injuries. For type APC2, LC1, and some LC2 fractures, fixation for the anterior pelvic ring is enough with INFIX technique alone. For some LC2, LC3, or VS fractures, the anterior and posterior ring were both fixed. Postoperative reduction was evaluated by Matta radiological criteria. Lateral thigh numbness and pain, quadriceps muscle power were recorded during follow-up, and clinical efficacy was evaluated by Majeed score at 6 months after operation.
Results:
All the 42 patients were followed up for 6 to 12 months, with an average of 9.3 months. Matta standard evaluation for fracture reduction showed that 28 cases were excellent, 14 cases good, and the excellent and good rate was 100%. The early complication rate (within 3 month after operation) was 23.8% (10/42) including 6 cases of lateral femoral cutaneous nerve injury and 2 cases of femoral nerve injury. The symptoms were obviously relieved after the treatment of nutrient nerve and hyperbaric oxygen; 1 case had incision infection which was healed after anti-infection therapy and internal plant removal; 1 case suffered from superior gluteal artery injury which was controlled by pressure hemostasis. Six months after surgery, no case had lost reduction. At 6 months follow-up, the Majeed score was 72-96, with an average of 84.96, of which 32 were excellent and 10 were good, thus the excellent and good rate was 100% (42/42).
Conclusion
INFIX is an effective internal fixation method for the treatment of unstable anterior pelvic ring injury. However, it has a high rate of early complications, among which nerve injury has the highest incidence.