1.Anti-inflammatory and hepatoprotective triterpenoids from the traditional Mongolian medicine Gentianopsis barbata.
Huizhen CHENG ; Huan LIU ; Xiaoyu QI ; Yuzhou FAN ; Zhongzhu YUAN ; Yuanliang XU ; Yanchun LIU ; Yan LIU ; Kai GUO ; Shenghong LI
Chinese Journal of Natural Medicines (English Ed.) 2025;23(9):1111-1121
Gentianopsis barbata (G. barbata) represents a significant plant species with considerable ornamental and medicinal value in China. This investigation sought to elucidate the primary constituents within the plant and investigate their pharmacological properties. Fifty triterpenoids (1-50), including nine previously undescribed compounds (1, 2, 7, 10, 20, 28, 29, 37, and 41) were isolated and characterized from the whole plants of G. barbata. Notably, compounds 1 and 2 exhibited the novel 3,4;9,10-diseco-24-homo-cycloartane triterpenoid skeleton. The isolated triterpenoids demonstrated substantial anti-inflammatory activity through inhibition of tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6) cytokine secretion in LPS-induced RAW264.7 macrophages, and hepatoprotective effects by preventing tert-butyl hydroperoxide (t-BHP)-induced oxidative injury in HepG2 cells. These results demonstrate both the presence of diverse triterpenoids in G. barbata and their therapeutic potential for inflammatory and hepatic conditions, providing scientific evidence supporting the clinical application of this traditional Mongolian medicinal plant.
Triterpenes/isolation & purification*
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Mice
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Anti-Inflammatory Agents/isolation & purification*
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Animals
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Humans
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RAW 264.7 Cells
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Hep G2 Cells
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Interleukin-6/genetics*
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Tumor Necrosis Factor-alpha/genetics*
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Medicine, Mongolian Traditional
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Macrophages/immunology*
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Protective Agents/isolation & purification*
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Liver/drug effects*
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Gentianaceae/chemistry*
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Plant Extracts/chemistry*
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Molecular Structure
2.Data Mining and Analysis of Adverse Events for Lutetium Lu 177 Vipivotide Tetraxetan
JIANG Cheng ; YUAN Yong ; CHEN Yunwang ; JIANG Xin ; TANG Zhongzhu
Chinese Journal of Modern Applied Pharmacy 2023;40(12):1603-1608
BACKGROUND On March 2022, the United States Food and Drug Administration(FDA) announced the approval of radiolabeled drug lutetium Lu 177 vipivotide tetraxetan for treatment of adult patients with prostate specific membrane antigen(PSMA)-positive metastatic castration-resistant prostate cancer who have been treated with androgen-receptor pathway inhibition and taxane-based chemotherapy. As PSMA is barely expressed on non-prostatic tissue, it has a very low background accumulation in healthy tissue, consequently, avoiding severe adverse drug reaction of lutetium Lu 177 vipivotide tetraxetan. A multicenter phase Ⅲ VISION study(NCT 03511664) showed that about 30% of patients with evaluable disease at baseline demonstrated an overall response with lutetium Lu 177 vipivotide tetraxetan plus standard care, compared to only 2% in the control arm. The high efficacy and mild adverse drug reaction of lutetium Lu 177 vipivotide tetraxetan cause opportunities for the healthcare systems and represent an important next step towards novel oncotherapy, but also cause great challenges in its clinical use due to lack of practical experience. Currently, data on the large sample and real-world comprehensive safety of lutetium Lu 177 vipivotide tetraxetan are still limited. Therefore, it is necessary to employ data mining algorithms to seek out the potential adverse event signals of lutetium Lu 177 vipivotide tetraxetan by post-marketing monitoring. METHODS FDA Adverse Event Reporting System(FAERS) is a publicly available, voluntary, and spontaneous reporting database. In the present study, the adverse events reported from the second quarter of 2022 to the fourth quarter of 2022 with lutetium Lu 177 vipivotide tetraxetan from FAERS were retrospectively analyzed. Seven types of datasets, including patient demographic and administrative information(DEMO), drug information(DRUG), therapy start dates and end dates for reported drugs(THER), adverse event results(OUTC), adverse event sources(PRSP), coded for the adverse events(REAC), and indications for use/diagnosis(INDI) were used. The reports of lutetium Lu 177 vipivotide tetraxetan were identified using generic name(LUTETIUM LU-177 VIPIVOTIDE TETRAXETAN in prod_ai column) and trade name(PLUVICTO in drug name column) in the DRUG dataset. The adverse event reports with the role_cod as the primary suspected(PS) were chose. Next, the report characteristics, demographic characteristics and onset time of lutetium Lu 177 vipivotide tetraxetan-associated adverse events were analyzed. The adverse events were coded using preferred terms(PT) derived from the standardized Medical Dictionary for Regulatory Activities 25.1(MedDRA), which contained 27 system organ classes(SOCs). Four algorithms, including reporting odds ratio(ROR), proportional reporting ratio(PRR), Bayesian confidence propagation neural network(BCPNN) and multi-item gamma Poisson shrinker(MGPS) were used to detect the signals. All the four data mining algorithms were based on the disproportionality analysis. An adverse event signal was detected only when it conformed to all of the four algorithms criteria simultaneously. RESULTS A total of 634 reports associated with lutetium Lu 177 vipivotide tetraxetan were considered. As a whole, the number of reports had increased gradually month-on-month, and 568(89.6%) reports occurred in the United States. The most common age and body weight groups were 61-80 years(75.4%) and 61-80 kg(50.9%), respectively. Most reports occurred within 30 d after administration of lutetium Lu 177 vipivotide tetraxetan, accounting for 41.5%. Based on 4 algorithms of ROR, PRR, BCPNN and MGPS, six effective signals at the PT level were detected, including anaemia(PT: 10002034), thrombocytopenia(PT: 10043554), laboratory test abnormal(PT: 10023547), platelet count decreased(PT: 10035528), full blood count decreased(PT: 10017413) and dry mouth(PT: 10013781). CONCLUSION When using lutetium Lu 177 vipivotide tetraxetan, it is important to strengthen clinical monitoring within one month and pay attentions to laboratory results including complete blood cell and platelet count. This study might provide powerful support for clinical monitoring of lutetium Lu 177 vipivotide tetraxetan.
3.3-D conformal radiotherapy for malignant thoracic tumors
Yuan ZHU ; Luying LIU ; Zhongzhu TANG
China Oncology 1998;0(04):-
Purpose: To evaluate the efficacy and the side effects of 3 D-conformal radiotherapy for malignant thoracic tumor. Methods: Between September 1999 and August 2002, 36 patients with malignant thoracic tumor were treated with 3D-conformal radiotherapy. Twenty-two patients had primary lung cancer, 12 patients had metastatic lung cancer, and 2 patients had malignant mediastinal tumor. All 36 patients were pathologically confirmed. Squamous cell carcinoma 16 cases, adenocarcinoma 15 cases, small cell carcinoma 2 cases, embryonal carcinoma 1 case, malignant thymoma 1 case and sarcoma 1 case. For the primary tumor, conventional radiotherapy was first used to 50Gy/25F/5W, followed by 3D-conformal radiotherapy 16-20Gy(4Gy per fraction, 3 fractions per week) with MLC or cone from 5 ~6 non coplanar or coplanar static ports. For metastatic tumor, using arc therapy to only 28-40Gy(4Gy per fraction, 3 fractions per week, 7-10 fractions) with cone from 1 ~ 4 arcs. Tumor volumes from 1. 85 cm3 to 104. 61 cm3 with a median of 24. 96 cm3 in 3D-CRT. Results: To evaluate the effects, thoracic CT scan was taken two months after completion of 3D-conformal radiotherapy. In 34 evaluated patients, 13 cases obtained CR, 14 PR, 5 NC, and 2PD. The overall 1 and 2-year survival rates were 74. 1% and 38.4%. Toxicity consisted of grade 1 acute radiation pneumonitis in 17 patients, grade 2 in 10 patients, grade 3 in 1 patients, and 2 patients dead of radiation pneumonitis ( with non coplanar technique), late complication was radiation pulmonary fibrosis, grade 1 in 20 cases, grade 2 in 8 cases. Conclusions: 3D-conformal radiotherapy as complement of conventional external beam radiotherapy for malignant thoracic tumor can obtain better short-term effects, although the survival is yet to be investigated. But attention must be given to the irradiation technique, the irradiation volume should not be too large and beams angles appropriately adjusted to avoid excessive irradiated volume in normal lung.
4.Late course accelerated hypofractionated three-dimensional conformal radiotherapy for stageⅢnon-small cell lung cancer
Zhongzhu TANG ; Yuan ZHU ; Qinghua DENG ; Jian WANG ; Shenglin MA
Chinese Journal of Radiation Oncology 1992;0(04):-
Objective Objective To evaluate the efficacy and comphcations of late course acceler- ated hypofractionated three dimensional conformal radiation therapy (3DCRT) for patients with stageⅢnon small cell lung cancer (NSCLC). Methods Sixty patients with stageⅢNSCLC were randomized into 2 groups: Late course accelerated hypofractionated 3DCRT group(group A—30 patients) and conventional fractionated radiation therapy group (group B—30 patients). In group A, 30 patients, at first, received a dose of 40 Gy at 2 Gy per fraction, 5 times a week, which followed by late course accelerated hypofractionat- ed 3DCRT with a dose of 16-20 Gy at 4 Gy per fraction, 3 times a week. In group B, 30 patients received a dose of 60-66 Gy at 2 Gy per fraction, 5 times a week. Chemotherapy, including vinorelbine and cisplatin, was given one cycle during radiotherapy and 3 cycles after radiotherapy for all patients. Results Group A had a higher complete response rate (47% vs 20%, P


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