1.Phacoemulsification and posterior chamber intraocular lens implantation combined with trabeculectomy
Xinhua, SONG ; Li, CHANG ; Yazhou, JI
Chinese Journal of Experimental Ophthalmology 2001;19(3):271-272
ObjectiveTo evaluate the therapeutic effect of phacoemulsifcation and posterior chamber intraocular lens(IOL) implantation combined with trabeculectomy in patients with cataract and glaucoma.Methods26 cases(26 eyes)were theated by phacoemulsification and IOL implantation combined with trabeculectomy.Follow-up period was for 2~16 months.ResultsThe average intraocular pressure(IOP)was reducded from 24.82 mmHg preoperatively to 16.52 mmHg postoperatively.IOP was less than 21 mmHg in 88.46% eyes.Visual acuity was 0.3 or better in 80.77% of eyes during following-up.61.54% of eyes were found with functional filtering blebs.ConclusionTriple procedure is safe and suitable method for most patiants with glaucoma and cateract
2.Clinical observation of neck Gongfa exercise intervening people at high risk for cervical spondylosis
Ji MA ; Yu ZHANG ; Fei GU ; Yumin LIU ; Junliang WANG ; Cheng WANG ; Yazhou LI ; Kaixin SUN ; Jun ZHANG ; Jue HONG
Journal of Acupuncture and Tuina Science 2024;22(6):489-496
Objective:To observe the clinical efficacy of neck Gongfa exercise in intervening people at high risk for cervical spondylosis. Methods:A total of 212 participants from 8 companies at high risk for cervical spondylosis were divided into two groups using the random number table method,with 105 participants in the control group receiving health education and 107 participants in the trial group receiving an additional neck Gongfa exercise.After successive 3-month interventions,the two groups were compared in terms of cervical soft tissue tension and neck disability index(NDI)score.The incidence of cervical spondylosis was observed 3 months later. Results:During the process,10 cases dropped out in the trial group,and the control group had 9 dropout cases.After the intervention,the cervical soft tissue tension value and NDI score improved in both groups(P<0.05)and showed significant differences between the two groups(P<0.05).At the 3-month follow-up,the trial group had a lower incidence rate of cervical spondylosis than the control group(P<0.05). Conclusion:For people at high risk for cervical spondylosis,neck Gongfa exercise can effectively improve cervical soft tissue tension and motor dysfunction and lower the incidence of cervical spondylosis in the short run.
3.Self-assembly of CXCR4 antagonist peptide-docetaxel conjugates for breast tumor multi-organ metastasis inhibition.
Chen LI ; Jiayan LANG ; Yazhou WANG ; Zhaoxia CHENG ; Mali ZU ; Fenfen LI ; Jingyi SUN ; Yating DENG ; Tianjiao JI ; Guangjun NIE ; Ying ZHAO
Acta Pharmaceutica Sinica B 2023;13(9):3849-3861
As a representative chemotherapeutic drug, docetaxel (DTX) has been used for breast cancer treatment for decades. However, the poor solubility of DTX limits its efficacy, and the DTX based therapy increases the metastasis risk due to the upregulation of C-X-C chemokine receptor type 4 (CXCR4) expression during the treatment. Herein, we conjugated CXCR4 antagonist peptide (CTCE) with DTX (termed CTCE-DTX) as an anti-metastasis agent to treat breast cancer. CTCE-DTX could self-assemble to nanoparticles, targeting CXCR4-upregulated metastatic tumor cells and enhancing the DTX efficacy. Thus, the CTCE-DTX NPs achieved promising efficacy on inhibiting both bone-specific metastasis and lung metastasis of triple-negative breast cancer. Our work provided a rational strategy on designing peptide-drug conjugates with synergistic anti-tumor efficacy.
4.Structure-based drug discovery of novel fused-pyrazolone carboxamide derivatives as potent and selective AXL inhibitors.
Feifei FANG ; Yang DAI ; Hao WANG ; Yinchun JI ; Xuewu LIANG ; Xia PENG ; Jiyuan LI ; Yangrong ZHAO ; Chunpu LI ; Danyi WANG ; Yazhou LI ; Dong ZHANG ; Dan ZHANG ; Meiyu GENG ; Hong LIU ; Jing AI ; Yu ZHOU
Acta Pharmaceutica Sinica B 2023;13(12):4918-4933
As a novel and promising antitumor target, AXL plays an important role in tumor growth, metastasis, immunosuppression and drug resistance of various malignancies, which has attracted extensive research interest in recent years. In this study, by employing the structure-based drug design and bioisosterism strategies, we designed and synthesized in total 54 novel AXL inhibitors featuring a fused-pyrazolone carboxamide scaffold, of which up to 20 compounds exhibited excellent AXL kinase and BaF3/TEL-AXL cell viability inhibitions. Notably, compound 59 showed a desirable AXL kinase inhibitory activity (IC50: 3.5 nmol/L) as well as good kinase selectivity, and it effectively blocked the cellular AXL signaling. In turn, compound 59 could potently inhibit BaF3/TEL-AXL cell viability (IC50: 1.5 nmol/L) and significantly suppress GAS6/AXL-mediated cancer cell invasion, migration and wound healing at the nanomolar level. More importantly, compound 59 oral administration showed good pharmacokinetic profile and in vivo antitumor efficiency, in which we observed significant AXL phosphorylation suppression, and its antitumor efficacy at 20 mg/kg (qd) was comparable to that of BGB324 at 50 mg/kg (bid), the most advanced AXL inhibitor. Taken together, this work provided a valuable lead compound as a potential AXL inhibitor for the further antitumor drug development.