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c-MYC-mediated TRIB3/P62^(+) aggresomes accumulation triggers paraptosis upon the combination of everolimus and ginsenoside Rh2

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Acta Pharmaceutica Sinica B 2022年第3期12卷 1240-1253页

作者： Min-Xia Su Yu-Lian Xu Xiao-Ming Jiang Mu-Yang Huang Le-Le Zhang Luo-Wei Yuan Xiao-Huang Xu Qi Zhu Jian-Li Gao Jia-Hong Lu Xiuping Chen Ming-Qing Huang Yitao Wang Jin-Jian Lu State Key Laboratory of Quality Research in Chinese Medicine Institute of Chinese Medical SciencesUniversity of MacaoMacao 999078China School of Pharmaceutical Sciences Zhejiang Chinese Medical UniversityHangzhou 310000China College of Pharmacy Fujian University of Traditional Chinese MedicineFuzhou 350000China Mo E Frontiers Science Center for Precision Oncology University of MacaoMacao 999078China

The mammalian target of rapamycin(m TOR) pathway is abnormally activated in lung ***, the anti-lung cancer effect of m TOR inhibitors as monotherapy is modest. Here, we identified that ginsenoside Rh2, an active component of Panax ginseng C. A. Mey., enhanced the anti-cancer effect of the m TOR inhibitor everolimus both in vitro and in vivo. Moreover, ginsenoside Rh2 alleviated the hepatic fat accumulation caused by everolimus in xenograft nude mice models. The combination of everolimus and ginsenoside Rh2(labeled Eve-Rh2) induced caspase-independent cell death and cytoplasmic vacuolation in lung cancer cells, indicating that Eve-Rh2 prevented tumor progression by triggering paraptosis. EveRh2 up-regulated the expression of c-MYC in cancer cells as well as tumor tissues. The increased cMYC mediated the accumulation of tribbles homolog 3(TRIB3)/P62+ aggresomes and consequently triggered paraptosis, bypassing the classical c-MYC/MAX pathway. Our study offers a potential effective and safe strategy for the treatment of lung cancer. Moreover, we have identified a new mechanism of TRIB3/P62+ aggresomes-triggered paraptosis and revealed a unique function of c-MYC.

关键词： everolimus Ginsenoside Rh2 Paraptosis Aggresomes P62 TRIB3 c-MYC Lung cancer

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Piceatannol enhances Beclin-1 activity to suppress tumor progression and its combination therapy strategy with everolimus in gastric cancer

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Science China(Life Sciences) 2023年第2期66卷 298-312页

作者： Longtao Huangfu Xiaoyang Wang Shanshan Tian Junbing Chen Xueying Wang Biao Fan Qian Yao Gangjian Wang Cong Chen Jing Han Xiaofang Xing Jiafu Ji Key Laboratory of Carcinogenesis and Translational Research(Ministry of Education) Division of Gastrointestinal Cancer Translational Research LaboratoryPeking University Cancer Hospital&InstituteBeijing 100142China Department of Pharmacy Peking University Cancer Hospital&InstituteBeijing 100142China National Institute on Drug Dependence Peking UniversityBeijing 100191China Gastrointestinal Cancer Center Peking University Cancer Hospital&InstituteBeijing 100142China Department of Pathology Peking University Cancer Hospital&InstituteBeijing 100142China

The effects and regulation of Beclin-1-an autophagy-related protein-have not been fully defined, however, a negative correlation has been reported between Beclin-1 expression and carcinogenesis. Meanwhile, no compound has been shown to directly inhibit its activity. Here, we evaluate piceatannol, a naturally occurring polyphenolic compound, as a potential targeting agonist of Beclin-1, to assess its efficacy as an antitumor agent against gastric cancer. More specifically, we determine the effects of piceatannol treatment on cell viability using a monitoring system and colony forming assay. Piceatannol was found to efficiently inhibit the proliferation of several human gastric cancer cell lines. Autophagic flux is increased by piceatannol treatment, and correlates with inhibition of cell proliferation and colony formation. Additionally, microscale thermophoresis and surface plasmon resonance results show a direct interaction between piceatannol and Beclin-1, which reduces the phosphorylation activity of Beclin-1 at the Ser-295 site. Notably, piceatannol impairs the binding of Beclin-1 to Bcl-2 and enhances the recruitment of binding of UV radiation resistance-associated gene protein, which further triggers Beclin-1-dependent autophagy signaling. An increase in autophagic activity via treatment with the mTOR inhibitor, everolimus, effectively sensitizes piceatannol-induced antitumor effects. Xenograft models confirmed that piceatannol inhibits tumor development and elicits a potent synergistic effect with everolimus in vivo. Taken together, the findings of this study strongly support the application of combinatorial piceatannol and everolimus therapy in future clinical trials for gastric cancer patients.

关键词： piceatannol Beclin-1 autophagy everolimus gastric cancer drug synergy

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everolimus *** for Treating Diabetic Nephropathy in Diabetic Mouse Model

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Journal of Huazhong University of Science and Technology(Medical Sciences) 2011年第4期31卷 457-462页

作者：程澜陈璟莉毛小露 Department of Internal Medicine and Institute of Hypertension Tongji HospitalTongji Medical CollegeHuazhong University of Science and Technology Department of Anesthesiology Wuhan Central Hospital Department of Clinical Laboratory Wuhan Central Hospital

In order to evaluate the effectiveness of everolimus *** in the treatment of diabetic nephropathy,8-week old diabetic（db/db） mice received everolimus（2 mg/kg every day） or rapamycin（2 mg/kg every day） for 4 weeks or 12 weeks *** and 24-h urine samples were collected for biochemical *** kidney from each mouse was homogenized for protein analysis and the other was removed for histological *** expression levels of transforming growth factor-β1（TGF-β1）and phospho-p70s6k were detected by using ELISA and Western blot,respectively in the renal tissue as well as in mesengial cell culture *** was significantly more effective than rapamycin in improving indexes of renal function and glomerular hypertrophy,and in decreasing accumulation and expansion of the extracellular ***,everolimus inhibited TGF-β1 secretion and p70s6k phosphorylation induced by high glucose in vitro less efficiently than rapamycin at the same *** was more effective than rapamycin in preventing diabetic nephropathy in vivo,which may be contributed to the fact that everolimus has better bioavailability and a higher oral absorption rate.

关键词： db/db mice diabetic nephropathy everolimus mammalian target of rapamycin mesangial cells

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Oral everolimus inhibits intimal proliferation in injured carotid artery in rats

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Chinese Medical Journal 2013年第10期126卷 1906-1912页

作者： WANG Xiao-fang SHEN De-liang ZHAO Xiao-yan N1NG Hong-jie FENG Ri-sheng ZHANG Jin-ying Department of Cardiology First Affiliated Hospital College ofMedicine Zhengzhou University Zhengzhou Henan 450052 China

Background everolimus, a derivative of sirolimus, is a potent immunosuppressant that has important anti-proliferative properties. In the present study, we demonstrated the inhibiting neointimal hyperplasia in injured carotid arteries in rats by using two different doses of everolimus administrated via the oral route for a long time. Methods A rat model of carotid artery injury was established by balloon inflation. Eighty rats were randomly divided into the sham-operated group （n=20）, injury group （n=20）, low dosage of everolimus group （n=20）, and high dosage of everolimus group （n=20）. The low close of everolimus （1.5 mg/kg） was given one day before injuring the carotid artery by balloon, followed by 0.75 mg/kg per day for 28 days via intragastric gavage. High dose everolimus （2.5 mg/kg） was given one day before injuring the carotid artery by balloon, followed by 1 mg/kg per day for 28 days. Expression of eukaryotic translation initiation factor 4E （elF-4E） and phosphorylation of ribosomal proteinS6 kinase 1 （P70S6K） were determined by reverse transcription-polymerase chain reaction and Western blotting analysis. Results In the injured carotid artery, neointimal hyperplasia was normally observed four weeks after injury. everolimus inhibited neointimal hyperplasia after balloon injury in a dose dependent manner. At the same time, the study demonstrated that everolimus reduced the expression of P-P70S6K, elF-4E, transforming growth factor （TGF）-131 and of proliferating cell nuclear antigen （PCNA）. Conclusions everolimus significantly inhibited neointimal hyperplasia of the injured carotid artery. The effect depended on dosaqe and was associated with the reduction of phosphorylation of P70S6K and the elF-4E expression level.

关键词： everolimus ribosomal protein S6 kinase 1, eukaryotic translation initiation factor 4E

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Benefit of everolimus in treatment of an intrahepatic cholangiocarcinoma patient with a PIK3CA mutation

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World Journal of Gastroenterology 2017年第23期23卷 4311-4316页

作者： Ji-Lai Bian Mei-Mei Wang En-Juan Tong Jing Sun Ming Li Zhi-Bo Miao Yan-Lin Li Bai-Hong Zhu Jia-Jia Xu Department of Medical Oncology The Fifth People's Hospital of Dalian Origimed Inc Institute of Precision Medicine 3D Medicines Inc

Intrahepatic cholangiocarcinoma(ICC) is a relatively rare form of liver cancer with a poor prognosis. The therapeutic options for patients with advanced ICC are limited and usually ineffective. There is currently no approved targeted therapy for ICC, although accumulating evidence supports inhibition of the PI3K/Akt/m TOR signaling pathway as a promising therapeutic strategy in the treatment of ICC. Here, we report a patient with stage IV ICC harboring a PIK3 CA mutation who responded well to the m TOR inhibitor everolimus. Computed tomography and magnetic resonance imaging demonstrated shrinkage of the tumor and maintenance of a partial response for 6.5 mo after everolimus treatment as the best response. To the best of our knowledge, this is the first clinical case report in the literature of clinical benefit from everolimus treatment in an ICC patient with PIK3 CA mutation.

关键词： everolimus 定序的下一代 PIK3CA Intrahepatic cholangiocarcinoma

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Safety and performance of the EverProTM everolimus-eluting coronary stent system with biodegradable polymer in a real-world scenario

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World Journal of Cardiology 2020年第12期12卷 615-625页

作者： Rahul Trimukhe Preeti Vani Arvind Patel Vikas Salgotra Department of Cardiology Atma Malik HospitalAhmednagar 423601MaharashtraIndia SLTL Medical Division SLTL(Sahajanand Laser Technology Ltd.)Gandhinagar 382016GujaratIndia SLTL Group SLTL(Sahajanand Laser Technology Ltd.)Gandhinagar 382016GujaratIndia

BACKGROUND The EverProTM(Sahajanand Laser Technology Ltd.,India)everolimus-eluting coronary stent system(EES)is a second-generation drug-eluting stent with a biodegradable *** To determine the safety and performance of the EverProTM EES in patients with coronary artery disease(CAD)during a 1-year clinical *** This observational,retrospective,single-center study enrolled patients who had been implanted with the EverProTM stent between June 1,2018 and January 31,2019,and had completed a 1-year follow-up period after the index *** primary clinical endpoint was major adverse cardiac events(MACE)at 6 mo defined as the composite of cardiac death,myocardial infarction(MI),and target lesion revascularization(TLR).Secondary endpoints were the incidence of TLR at 1,6 and 12 mo follow-up,MACE at 1 and 12 mo follow-up,and stent thrombosis up to 1 year after the index *** The study population comprised 77 patients(98 lesions).A total of 37(48.1%)patients had comorbid *** total,26(33.8%)patients presented with ST segment elevation MI and 10.4%patients with non-ST segment elevation *** lesions were located mainly in the left anterior descending artery(49%)followed by the right coronary artery(29.6%),left circumflex(12.2%)and obtuse marginal(9.2%)*** majority of patients were with single-vessel disease(79%),22.2%of lesions had a mild to severe thrombus load,and 94.9%were American College of Cardiology/American Heart Association type B or *** novo stenting was performed in 96.9%of patients and 3%were treated for in-stent *** success was attained in all ***-hospital or followup MACE and stent thrombosis were not reported during the 1-year follow-up *** These findings suggest that the EverProTM EES is a safe and effective treatment option with no MACE or stent thrombosis reported during the 1-year study period in patients with CAD.

关键词： Coronary artery disease everolimus Major adverse cardiac event Retrospective,EverPro^(TM),Myocardial infarction

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everolimus Associated with Activated Vitamin D for Post-Transplant Increase Epstein-Barr-Virus Load Treatment. Two Case Reports

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International Journal of Clinical Medicine 2012年第7期3卷 669-672页

作者： Luciano Moscarelli Giulia Antognoli Renal Unit Careggi University Hospital Florence Italy.

Post-transplant lymphoproliferative disease (PTLD) is an uncommon but life-threatening complication of solid-organ and blood stem-cell transplants. It is caused by an uncontrolled expansion of B lymphocytes infected with Epstein-Barr virus (EBV). It responds poorly to therapy, including reduction of immunosuppression, interferon, antivirals or chemotherapy. Therefore the optimal strategy for management is currently focused on prevention. Some centers have already introduced chemoprophylaxis and/or preemptive strategies using EBV viral load as a surveillance. Some experimental studies suggest that mTOR inhibitors inhibits growth of human EBV-transformed B lymphocytes and vitamin D had an immune response to EBV. We report two cases of an increased of blood BKV viral load after renal transplantation that were successfully treated with everolimus in association with calcitriol. This report suggests that everolimus associated with calcitriol could be an effective and safe treatment for the prevention of PTLD in transplant recipients.

关键词： Calcitriol everolimus Post-Transplant Lymphoproliferative Disease Renal Transplant

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Introduction of everolimus in kidney transplant recipients at a late posttransplant stage

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World Journal of Transplantation 2018年第5期8卷 150-155页

作者： Junji Uchida Tomoaki Iwai Tatsuya Nakatani Department of Urology Osaka City University Graduate School of Medicine

This minireview focuses on the current knowledge about the introduction of everolimus(EVL),a mammalian target of rapamycin inhibitor,with calcineurin inhibitor(CNI)elimination or minimization in kidney transplant recipients at a late posttransplant ***,we have summarized two major clinical trials,ASCERTAIN and APOLLO,and seven other retrospective or nonrandomized *** the open-label multicenter ASCERTAIN study,the estimated glomerular filtration rate(eGFR)at 24 mo after conversion was not significantly different between three groups-EVL with CNI elimination,CNI minimization and continued CNI unchanged-at a mean of 5.4 years after ***,recipients with baseline creatinine clearance higher than 50 mL/min had a greater increase in measured GFR after CNI *** the open-label multicenter APOLLO study,adjusted e GFR within the on-treatment population was significantly higher in the EVL continuation group than in the CNI continuation group at 12 mo after conversion at a mean of 7 years *** studies on recipients without adverse events and already having satisfactory renal function showed favorable graft function by EVL late-induction with CNI elimination or *** studies showed that chronic allograft nephropathy,CNI nephrotoxicity,CNI arteriolopathy,cancer and viral infection(especially cytomegalovirus infection)may be good indications for late conversion to EVL.

关键词： Kidney transplantation everolimus mTOR inhibitor Late conversion Calcineurine inhibitor

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Use of everolimus in liver transplantation

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World Journal of Hepatology 2017年第23期9卷 990-1000页

作者： Mei-Ling Yee Hui-Hui Tan Department of Pharmacy Singapore General Hospital Department of Gastroenterology and Hepatology Singapore General Hospital

In recent years, the use of mammalian target of rapamycin inhibitors has gained traction in their use as alternative or adjunct immunosuppressants in the post-liver transplantation(LT) setting. The efficacy of everolimus(EVR) in de novo LT is established and a reasonable time to initiate EVR is 30d from LT surgery. Initiating EVR early post-LT allows for calcineurin inhibitor(CNI) reduction, thus reducing nephrotoxicity in LT recipients. However, data is inadequate on the appropriate timing for conversion from CNI to EVR maintenance in order to achieve optimal renoprotective effect without compromising drug efficacy. Adverse effects of proteinuria, hypercholesterolemia and hyperlipidemia are significantly higher as compared to standard CNI and long-term implications on graft and patient survival in LT is still unclear. Future research to explore strategies to minimise EVR adverse effects will be crucial for the success of EVR as an important alternative or adjunct immunosuppressive therapy in LT.

关键词： everolimus rapamycin 禁止者的哺乳动物的目标免疫力的抑制肝移植 Nephrotoxicity

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The Role of everolimus in the Treatment of Breast Cancer

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Journal of Cancer Therapy 2013年第7期4卷 1167-1176页

作者： José Pablo Leone Ricardo H. álvarez Department of Breast Medical Oncology Morgan Welch Inflammatory Breast Cancer Research Program and Clinic University of Texas M. D. Anderson Cancer Center Houston USA. University of Pittsburgh Cancer Institute Pittsburgh USA

The development of resistance to chemotherapy, endocrine therapy and anti HER2 agents in breast cancer is an important and common problem that impacts in the management of patients, particularly in the metastatic setting. This resistance has been explained in part by the activation of signal transduction pathways, including the PI3K/AKT/mTOR. The blockade with mTOR inhibitors such as everolimus is a new target agent for therapy that attempts to enhance treatment efficacy and restore tumor sensitivity. In this review article, we present the data about the use of everolimus for the treatment of breast cancer in all tumor phenotypes. Future studies that evaluate biomarkers for treatment response are needed to identify the specific populations that have the highest benefit of this new targeted therapy.

关键词： Advanced Breast Cancer everolimus mTOR Inhibitors

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