1.Determination of genpioside,baicalin and berberine hydrochloride in Gonglao Quhuo Tablets simultaneously by RP-HPLC
Yangrong LI ; Ye JIANG ; Fu HAO ; Xiangyu DING
Chinese Traditional Patent Medicine 1992;0(08):-
AIM: To establish a method of determining genpioside,baicalin and berberine in Gonglao Quhuo Tablets(Caulis Mahoniae,Cortex Phellodendri Chinensis,Radix Scutellariae,etc). METHODS: The mobile phase composed of A acetonitrile,B acetonitrile and 0.5% triethylamine(Ph3.1)(10∶90).The flow rate was 1.0 mL/min with the wavelength at 254 nm. RESULTS:The calibration curves were linear in the ranges of 3.22-206 ?g/mL(r=0.999 9) for genpioside,2.95-186 ?g/mL(r=0.999 9) for baicalin and 1.64-104 ?g/mL(r=0.999 9) for berberine hydrochloride,respectively.The average recoveries were not less than 98.4%. CONCLUSION: This HPLC method is convenient,rapid,accurate and could be used for quality control of production of Gonglao Quhuo Tablets.
2.Effects of nutritional support under energy metabolic monitoring on nutritional indexes and clinical prognosis of elderly patients with critical severe diseases
Li WU ; Yangrong FENG ; Danxia GE ; Yan WU ; Geng ZHANG ; Zhizhen LAI
Chinese Journal of Integrated Traditional and Western Medicine in Intensive and Critical Care 2017;24(6):645-649
Objective To investigate the effects of nutritional therapy under energy metabolic monitoring on nutrition indicators and clinical prognosis of elderly patients with critical severe diseases in the department of Intensive Care Unit (ICU).Methods One hundred and twenty elderly patients admitted to the Department of ICU of Integrate Traditional Chinese Medicine Hospital of Ningbo, from January 2013 to December 2016 were enrolled, and they were divided into a control group (62 cases) and an observation group (58 cases) by randomized block method. The patients in observation group received nutritional support treatment under the guidance of energy metabolic monitoring, the amount of nitrogen needed was measured every day, and appropriate energy was provided according to the amount of nitrogen and the ratio of heat to nitrogen; the patients in the control group were given the nutritional support program according to experience. The clinical efficacy was evaluated after 7 days of treatment in the two groups, the differences in hemoglobin (Hb), serum albumin (Alb), prealbumin (PA), weaning success rate within 7 days, duration of mechanical ventilation, length of stay in ICU, the standard rate of enteral nutrition (EN) in 7 days, parenteral nutrition support rate, reaching EN target calorie time, acute physiology and chronic health evaluation Ⅱ (APACHEⅡ) score on the 7th day after admission and at discharge, the incidence of complications such as abdominal distention, stress ulcer, ventilator associator pneumonia (VAP), heart failure during nutritional treatment and mortality were observed and compared after EN support between the two groups.Results Compared with control group, after treatment Hb (g/L: 136.5±2.5 vs. 90.4±2.3), Alb (g/L: 35.7±4.6 vs. 32.8±4.2), PA contents (g/L: 211.0±20.8 vs. 190.9±30.7), weaning success rate within 7 days [55.2% (32/58) vs. 33.9% (21/62)], the standard rate of EN in 7 days in the observation group were obviously higher [82.8% (48/58) vs. 51.61% (32/62) allP < 0.05], but duration of mechanical ventilation (days: 8.8±3.5 vs. 11.1±4.0), length of stay in ICU (days: 21.2±5.0 vs. 25.9±6.5), parenteral nutrition support rate [29.3% (17/58) vs. 51.6% (32/62)], reaching EN target calorie time (days: 4.4±2.1 vs. 6.2±2.9), APECHE Ⅱ score 7 days after admission (18.7±5.8 vs. 20.8±8.1), APACHEⅡscore at discharge (13.0±5.2 vs. 15.6±4.5) and the incidence of complications such as abdominal distension [10.3% (6/58) vs. 41.9% (26/62)], stress ulcer [3.4% (2/58) vs. 12.9%(8/62)], VAP [22.4% (13/58) vs. 25.8% (16/62)], heart failure [15.5% (9/58) vs. 24.2% (15/62)] etc, were all lower in observation group (allP < 0.05), and 2 weeks later the mortality was significantly lower in the observation group than that in the control group [13.79% (8/58) vs. 22.58% (14/62),P < 0.05].Conclusions Nitrogen required in elderly patients critically ill patients with early determination, the supply of nutrients to guide empirical method is more accurate compared to the nutritional therapy. Nutritional support under energy metabolism monitoring can shorten clinical course, improve nutritional indicators and help reduce the risk of complications and death.
3.Application of 125I radioactive particles in mediastinal lymph node metastasis
Zhigang LIU ; Kaige ZHANG ; Guangyan LEI ; Weidong LÜ ; Xi ZHANG ; Yangrong SONG ; Li YAN ; Hongbing MA ; Jun WANG ; Qi CHENG
Chinese Journal of Clinical Oncology 2019;46(7):351-356
Objective: To investigate the safety and efficacy of 125I radioactive seed implantation in the treatment of mediastinal lymph node metastasis. Methods: Records of 53 patients enrolled in Shaanxi Provincial Tumor Hospital from June 2014 to June 2018 with me-diastinal lymph node metastasis treated by computed tomography (CT)-guided 125I seed implantation were analyzed retrospectively. The preoperative treatment planning system was validated after the surgery. Intraoperative and post-operative complications were re-corded. The improvement in quality of life was observed. Chest CT follow-up was conducted 1 month, 3 months, 6 months, 1 year, and 2 years after treatment. The local focus control was evaluated. The median survival and total survival were recorded, and the survival prognosis and causes of death were analyzed. Results: The median survival time was 254 days (8.5 months), one-year survival rate was 48.67%, and complete and partial response rate was 83.02% (44/53). Multivariate Cox model analysis showed that the survival progno-sis was related to the Eastern Cooperative Oncology Group (ECOG) score, distant metastasis at the time of implantation, concurrent chemotherapy after implantation, and secondary seed implantation (P<0.05). The rates of developing pneumothorax and hemoptysis during and after the surgery were 20.75% (11/55) and 13.20% (7/55), respectively. No patients died. After implantation, the remission rate of cough, shortness of breath, pain, hoarseness, and superior vena cava syndrome was 60.00%-82.61%. Conclusions: CT-guid-ed 125I seed implantation in the treatment of mediastinal lymph node metastasis has the advantages of minimal trauma, remarkable cu-rative effect, safety, and feasibility. It has important application value and is worthy of further clinical application.
4.Synthesis and formation mechanism of ocotillol and its epimer
Wenzhi WANG ; Yangrong XU ; Xinli LI ; Jingjing YANG ; Qingguo MENG
Journal of China Pharmaceutical University 2016;47(3):282-287
Ocotillol(3)and its epimer(4)have been synthesized from 20(S)-protopanaxatriol [20(S)-PPT] via two routes, and their formation mechanism has been speculated. Route 1: Compounds 3 and 4 were obtained from 20(S)-PPT by oxidation with m-CPBA at the yield of 44. 1% and 28. 6%, respectively. Route 2: Compounds 3 and 4 were prepared from 20(S)-PPT by acetylation, oxidation and saponification at the yield of 16. 4% and 16. 2%, respectively. The formation mechanism of compounds 3 and 4 is speculated as below: 1)The chemical environments of both sides of C24(25)double bond in 20(S)-PPT are different due to the existence of intramolecular hydrogen bond, which led to the different oxidation ratio of the two sides, and the different yields of compounds 3 and 4. 2)There is not intramolecular hydrogen bond in acetylated 20(S)-PPT, and the chemical environments of both sides of C24(25)double bond are similar, which resulted in almost equal yields of compounds 3 and 4 synthesized through oxidation with m-CPBA, intramolecular SN2 and saponification.
5.Dosimetric study of 125I seed implantation guided by 4D template for advanced malignant tumors
Zhigang LIU ; Guangyan LEI ; Yongchun SONG ; Ruifang SUN ; Weidong LYU ; Yangrong SONG ; Xi ZHANG ; Jia LIU ; Hao CHENG ; Le HAN ; Kun ZHAO ; Wei GAO ; Xiaolong LI ; Xiaoju NING ; Libin QIANG
Chinese Journal of Radiation Oncology 2022;31(1):55-58
Objective:To investigate the safety and dose of 4D template (real-time adjustable angle template) in the treatment of advanced malignant tumors with 125I seeds. Methods:98 patients with advanced malignant tumors admitted to Department of Thoracic Surgery of Shaanxi Provincial Tumor Hospital were treated with 4D template-navigated radioactive 125I seed implantation from June 2018 to December 2019. Preoperative TPS plan, intraoperative optimization, postoperative verification of immediate dose and postoperative evaluation of implantation dose were performed. The treatment results were observed. Results:All 98 patients completed the seed implantation. The implantation dose of GTV of implantation site receiving external irradiation was (12 489±414) cGy and the dose of no external irradiation was (15 036±514) cGy. V 100% was 84.7%-94.1%, and 88.2%-93.7%. The implantation dose of CTV was (7 450±621) cGy, and (9 080±761) cGy. The quality of dose implantation was evaluated as: excellent in 89 cases (91%, 89/98), good in 7 cases (7%, 7/98), fair in 2 cases (2%, 2/98), and poor in 0 case, respectively. The symptom relief rate of patients with pain was 92%(36/39). The 1-and 2-year local control rates were 61%, 36% and 82%, 54% in patients treated with and without external irradiation, respectively. The difference was statistically significant ( P=0.02). The incidence rates of pneumothorax and hemoptysis were 19%(9/48) and 10%(5/48). No corresponding complications were observed in other parts of the patients. Conclusion:4D template-assisted 125I seed therapy is safe and effective for malignant tumors, and intraoperative adjustment of needle angle and dose optimization can realize the precise control of implantation dose.
6.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.