Cancer stands as one of the major threats to human life.Ensuring the safety of drugs is paramount,and the impact of adverse reactions on patients’quality of life and prognosis should not be underestimated.Diarrhea is...Cancer stands as one of the major threats to human life.Ensuring the safety of drugs is paramount,and the impact of adverse reactions on patients’quality of life and prognosis should not be underestimated.Diarrhea is a common clinical adverse event,and despite the absence of specific anti-diarrhea drugs,there is a pressing need for improvement.This article aims to provide a valuable reference for researchers in clinical drug use and scientific tumor treatment.It summarizes recent advancements in drug mechanisms and adverse reactions,whether in preclinical research or clinical diagnosis and therapy.展开更多
Recently microwave-induced chemical synthesis of curcumin-metformin adduct to enhance the efficacy of metformin in preventing the formation of Advanced Glycation End Products (AGEs) has been reported from authors' ...Recently microwave-induced chemical synthesis of curcumin-metformin adduct to enhance the efficacy of metformin in preventing the formation of Advanced Glycation End Products (AGEs) has been reported from authors' laboratory. The present studies describe microwave-induced chemical synthesis and mass spectral characterization of curcumin-phenformin adducts using LC-MS/MS. The mechanism of formation and its analytical data via Thin-Layer Chromatography (TLC) combined with MS/MS fragmentation revealed a major six membered ring adduct and a minor eight membered ring isomer. A facile chemical synthesis and identification of major and minor isomers presented in this study may offer novel therapeutic strategies for inhibiting AGEs as well as anti-cancer treatments.展开更多
This review starts with a brief history of drug discovery & development, and the place of Asia in this worldwide effort discussed. The conditions and constraints of a successful translational R&D involving aca...This review starts with a brief history of drug discovery & development, and the place of Asia in this worldwide effort discussed. The conditions and constraints of a successful translational R&D involving academic basic research and clinical research are discussed and the Singapore model for pursuit of open R&D described. The importance of well-characterized, validated drug targets for the search for novel targeted anti-cancer agents is emphasized, as well as a structured, high quality translational R&D. Furthermore, the characteristics of an attractive preclinical development drug candidate are discussed laying the foundation of a successful preclinical development. The most frequent sources of failures are described and risk management at every stage is highly recommended. Organizational factors are also considered to play an important role. The factors to consider before starting a new drug discovery & development project are described, and an example is given of a successful clinical project that has had its roots in local universities and was carried through preclinical development into phase I clinical trials.展开更多
Acetylated N-xyloside of 1-naphthylamine(K8A)has been shown to be more potent than 2-deoxy-D-glucose in lung cancer cells and has therapeutic potential for further drug development.In this paper we evaluate and report...Acetylated N-xyloside of 1-naphthylamine(K8A)has been shown to be more potent than 2-deoxy-D-glucose in lung cancer cells and has therapeutic potential for further drug development.In this paper we evaluate and report cytotoxicity,pharmacokinetic,physicochemical and medicinal properties of this D-Xylose derivative(K8A)as a lead anticancer agent with greater therapeutic potential than 2-deoxy-D-glucose(2-DG).2-DG has been in clinical trials for treatment of solid tumors and other types of cancer.We demonstrate using virtual tools that K8A has better“drug-likeness”than 2-DG and does not violate any Lipinski,Ghose,Veber,Egan or Muegge rules.On the other hand,2-DG violates Ghose and Muegge rules.A“BOILEDegg evaluation”,predicts that K8A has higher gastrointestinal absorption(HIA)than 2-DG and is not effluxed by P-glycoprotein(P-gp).Additionally,K8A does not penetrate the blood brain barrier(BBB)and is not a substrate of most Cytochrome P450(CYP)enzymes.Importantly,K8A did not show false positive alert from PAINS screening enabling us to narrow down and rule out false targets.Importantly,K8A is more potent than 2-DG in H1299 and A549 lung cancer cells.展开更多
Rhodiola rosea,a perennial herb of the genus Rhodiola in the Crassulaceae family,is commonly used to treat depression,fatigue,cancer and cardiovascular diseases.Herbacetin is a natural flavonol compound extracted from...Rhodiola rosea,a perennial herb of the genus Rhodiola in the Crassulaceae family,is commonly used to treat depression,fatigue,cancer and cardiovascular diseases.Herbacetin is a natural flavonol compound extracted from R.rosea plant,with many pharmacological effects such as anti-cancer effect,anti-oxidant effect and anti-inflammatory effect.In this paper,the pharmacological effects and molecular mechanisms of herbacetin were summarized by consulting domestic and foreign literature,in order to provide a theoretical basis for the development and utilization of herbacetin.展开更多
未来6G网络将内生支持通信和AI一体化服务,赋能丰富多彩的新业务,支撑社会高效可持续发展。为此,借鉴了IT行业AI Agent的应用范式,基于电信应用场景创新地提出了6G AI Agent技术框架的三大设计理念,包括多模型融合、定制化Agent和插件...未来6G网络将内生支持通信和AI一体化服务,赋能丰富多彩的新业务,支撑社会高效可持续发展。为此,借鉴了IT行业AI Agent的应用范式,基于电信应用场景创新地提出了6G AI Agent技术框架的三大设计理念,包括多模型融合、定制化Agent和插件式环境交互,并基于该理念构建了6G AI Agent技术框架。通过环境交互层、Agent引擎层、模型调度层、模型基座层交互协同,实现了自主环境感知、自主任务生成和自主执行任务的能力。此外,以移动网络的智能感知任务为例,探索了AI Agent的使用场景及价值,为AI新技术在电信领域发展提供了新的思路和技术支撑。展开更多
Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangusto...Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangustone A(IAA) from licorice(Glycyrrhiza uralensis), which induces apoptosis in colorectal cancer cells by disrupting mitochondrial functions. In the present study, we compared a group of flavonoids from licorice with IAA for their anti-proliferation activities and effects on intracellular signaling. The results indicated that the isoprenyl groups on the A and B rings, the hydroxyl groups at the ortho position of isoprenyl on A ring and the conjugated plane of C ring might contribute to the anti-cancer activity of prenylated flavonoids. Based on the above structure-activity relationship, we further identified four prenylated flavonoids with similar anti-cancer activities from licorice. Taken together, our present study established a preliminary structure-activity relationship of anti-cancer prenylated flavonoids, and our data provided important leading compounds from licorice, which deserved further research and development.展开更多
While newer,more efficient Lithium-ion batteries(LIBs)and extinguishing agents have been developed to reduce the occurrence of thermal runaway accidents,there is still a scarcity of research focused on the application...While newer,more efficient Lithium-ion batteries(LIBs)and extinguishing agents have been developed to reduce the occurrence of thermal runaway accidents,there is still a scarcity of research focused on the application of surfactants in different LIBs extinguishing agents,particularly in terms of patented technologies.The aim of this review paper is to provide an overview of the technological progress of LIBs and LIBs extinguishing agents in terms of patents in Korea,Japan,Europe,the United States,China,etc.The initial part of this review paper is sort out LIBs technology development in different regions.In addition,to compare LIBs extinguishing agent progress and challenges of liquid,solid,combination of multiple,and microencapsulated.The subsequent section of this review focuses on an in-depth analysis dedicated to the efficiency and challenges faced by the surfactants corresponding design principles of LIBs extinguishing agents,such as nonionic and anionic surfactants.A total of 451,760 LIBs-related patent and 20 LIBs-fire-extinguishing agent-related patent were included in the analyses.The extinguishing effect,cooling performance,and anti-recombustion on different agents have been highlighted.After a comprehensive comparison of these agents,this review suggests that temperature-sensitive hydrogel extinguishing agent is ideal for the effective control of LIBs fire.The progress and challenges of surfactants have been extensively examined,focusing on key factors such as surface activity,thermal stability,foaming properties,environmental friendliness,and electrical conductivity.Moreover,it is crucial to emphasize that the selection of a suitable surfactant must align with the extinguishing strategy of the extinguishing agent for optimal firefighting effectiveness.展开更多
Pterostilbene is a natural compound that can be found in various food plants such as blueberries,grapes,and peanuts.It has also been reported to be extracted from Pterocarpus indicus,a tree species native to India and...Pterostilbene is a natural compound that can be found in various food plants such as blueberries,grapes,and peanuts.It has also been reported to be extracted from Pterocarpus indicus,a tree species native to India and Southeast Asia.Pterostilbene exhibits various pharmacological activities such as antioxidants,anti-proliferation,anti-microbial,and anti-inflammatory activities with favorable pharmacokinetic properties,such as high oral bioavailability and longer half-life.The anti-inflammatory effect of pterostilbene has been reported to contribute to its therapeutic effects in many chronic inflammatory diseases.Besides,pterostilbene has anti-cancer activity on various types of cancers due to its ability to induce cell cycle arrest and apoptosis.Hence,in this review,we discuss the anti-inflammatory and anti-cancer activities of pterostilbene in preclinical studies.展开更多
文摘Cancer stands as one of the major threats to human life.Ensuring the safety of drugs is paramount,and the impact of adverse reactions on patients’quality of life and prognosis should not be underestimated.Diarrhea is a common clinical adverse event,and despite the absence of specific anti-diarrhea drugs,there is a pressing need for improvement.This article aims to provide a valuable reference for researchers in clinical drug use and scientific tumor treatment.It summarizes recent advancements in drug mechanisms and adverse reactions,whether in preclinical research or clinical diagnosis and therapy.
文摘Recently microwave-induced chemical synthesis of curcumin-metformin adduct to enhance the efficacy of metformin in preventing the formation of Advanced Glycation End Products (AGEs) has been reported from authors' laboratory. The present studies describe microwave-induced chemical synthesis and mass spectral characterization of curcumin-phenformin adducts using LC-MS/MS. The mechanism of formation and its analytical data via Thin-Layer Chromatography (TLC) combined with MS/MS fragmentation revealed a major six membered ring adduct and a minor eight membered ring isomer. A facile chemical synthesis and identification of major and minor isomers presented in this study may offer novel therapeutic strategies for inhibiting AGEs as well as anti-cancer treatments.
文摘This review starts with a brief history of drug discovery & development, and the place of Asia in this worldwide effort discussed. The conditions and constraints of a successful translational R&D involving academic basic research and clinical research are discussed and the Singapore model for pursuit of open R&D described. The importance of well-characterized, validated drug targets for the search for novel targeted anti-cancer agents is emphasized, as well as a structured, high quality translational R&D. Furthermore, the characteristics of an attractive preclinical development drug candidate are discussed laying the foundation of a successful preclinical development. The most frequent sources of failures are described and risk management at every stage is highly recommended. Organizational factors are also considered to play an important role. The factors to consider before starting a new drug discovery & development project are described, and an example is given of a successful clinical project that has had its roots in local universities and was carried through preclinical development into phase I clinical trials.
文摘Acetylated N-xyloside of 1-naphthylamine(K8A)has been shown to be more potent than 2-deoxy-D-glucose in lung cancer cells and has therapeutic potential for further drug development.In this paper we evaluate and report cytotoxicity,pharmacokinetic,physicochemical and medicinal properties of this D-Xylose derivative(K8A)as a lead anticancer agent with greater therapeutic potential than 2-deoxy-D-glucose(2-DG).2-DG has been in clinical trials for treatment of solid tumors and other types of cancer.We demonstrate using virtual tools that K8A has better“drug-likeness”than 2-DG and does not violate any Lipinski,Ghose,Veber,Egan or Muegge rules.On the other hand,2-DG violates Ghose and Muegge rules.A“BOILEDegg evaluation”,predicts that K8A has higher gastrointestinal absorption(HIA)than 2-DG and is not effluxed by P-glycoprotein(P-gp).Additionally,K8A does not penetrate the blood brain barrier(BBB)and is not a substrate of most Cytochrome P450(CYP)enzymes.Importantly,K8A did not show false positive alert from PAINS screening enabling us to narrow down and rule out false targets.Importantly,K8A is more potent than 2-DG in H1299 and A549 lung cancer cells.
基金Supported by Talent Training Project of Central Support for the Reform and Development Fund of Local Colleges and Universities(2020GSP16)Heilongjiang Provincial Key R&D Plan Guidance Project(GZ20220039)Daqing Guiding Science and Technology Project(zdy-2024-91).
文摘Rhodiola rosea,a perennial herb of the genus Rhodiola in the Crassulaceae family,is commonly used to treat depression,fatigue,cancer and cardiovascular diseases.Herbacetin is a natural flavonol compound extracted from R.rosea plant,with many pharmacological effects such as anti-cancer effect,anti-oxidant effect and anti-inflammatory effect.In this paper,the pharmacological effects and molecular mechanisms of herbacetin were summarized by consulting domestic and foreign literature,in order to provide a theoretical basis for the development and utilization of herbacetin.
文摘未来6G网络将内生支持通信和AI一体化服务,赋能丰富多彩的新业务,支撑社会高效可持续发展。为此,借鉴了IT行业AI Agent的应用范式,基于电信应用场景创新地提出了6G AI Agent技术框架的三大设计理念,包括多模型融合、定制化Agent和插件式环境交互,并基于该理念构建了6G AI Agent技术框架。通过环境交互层、Agent引擎层、模型调度层、模型基座层交互协同,实现了自主环境感知、自主任务生成和自主执行任务的能力。此外,以移动网络的智能感知任务为例,探索了AI Agent的使用场景及价值,为AI新技术在电信领域发展提供了新的思路和技术支撑。
基金National Natural Science Foundation of China(Grant No.81472657 and 81272468)
文摘Prenylated flavonoids are mainly distributed in Leguminosae and Moraceae plants, and they have been reported to possess various biological activities. Previously, we have reported a prenylated isoflavonoid, isoangustone A(IAA) from licorice(Glycyrrhiza uralensis), which induces apoptosis in colorectal cancer cells by disrupting mitochondrial functions. In the present study, we compared a group of flavonoids from licorice with IAA for their anti-proliferation activities and effects on intracellular signaling. The results indicated that the isoprenyl groups on the A and B rings, the hydroxyl groups at the ortho position of isoprenyl on A ring and the conjugated plane of C ring might contribute to the anti-cancer activity of prenylated flavonoids. Based on the above structure-activity relationship, we further identified four prenylated flavonoids with similar anti-cancer activities from licorice. Taken together, our present study established a preliminary structure-activity relationship of anti-cancer prenylated flavonoids, and our data provided important leading compounds from licorice, which deserved further research and development.
基金supported by the National Key Research and Development Program of China (No.2017YFC0804700)the Opening Project of State Key Laboratory of Explosion Science and Technology,Beijing Institute of Technology (No.KFJJ23-23M)。
文摘While newer,more efficient Lithium-ion batteries(LIBs)and extinguishing agents have been developed to reduce the occurrence of thermal runaway accidents,there is still a scarcity of research focused on the application of surfactants in different LIBs extinguishing agents,particularly in terms of patented technologies.The aim of this review paper is to provide an overview of the technological progress of LIBs and LIBs extinguishing agents in terms of patents in Korea,Japan,Europe,the United States,China,etc.The initial part of this review paper is sort out LIBs technology development in different regions.In addition,to compare LIBs extinguishing agent progress and challenges of liquid,solid,combination of multiple,and microencapsulated.The subsequent section of this review focuses on an in-depth analysis dedicated to the efficiency and challenges faced by the surfactants corresponding design principles of LIBs extinguishing agents,such as nonionic and anionic surfactants.A total of 451,760 LIBs-related patent and 20 LIBs-fire-extinguishing agent-related patent were included in the analyses.The extinguishing effect,cooling performance,and anti-recombustion on different agents have been highlighted.After a comprehensive comparison of these agents,this review suggests that temperature-sensitive hydrogel extinguishing agent is ideal for the effective control of LIBs fire.The progress and challenges of surfactants have been extensively examined,focusing on key factors such as surface activity,thermal stability,foaming properties,environmental friendliness,and electrical conductivity.Moreover,it is crucial to emphasize that the selection of a suitable surfactant must align with the extinguishing strategy of the extinguishing agent for optimal firefighting effectiveness.
基金the Ministry of Higher Education(MOHE)Malaysia through the Fundamental Research Grant Scheme(FRGS)with grant number:FRGS/1/2019/SKK10/UKM/01/1.
文摘Pterostilbene is a natural compound that can be found in various food plants such as blueberries,grapes,and peanuts.It has also been reported to be extracted from Pterocarpus indicus,a tree species native to India and Southeast Asia.Pterostilbene exhibits various pharmacological activities such as antioxidants,anti-proliferation,anti-microbial,and anti-inflammatory activities with favorable pharmacokinetic properties,such as high oral bioavailability and longer half-life.The anti-inflammatory effect of pterostilbene has been reported to contribute to its therapeutic effects in many chronic inflammatory diseases.Besides,pterostilbene has anti-cancer activity on various types of cancers due to its ability to induce cell cycle arrest and apoptosis.Hence,in this review,we discuss the anti-inflammatory and anti-cancer activities of pterostilbene in preclinical studies.