Journal ArticleDOI
Fluorescent Coumarin–Artemisinin Conjugates as Mitochondria-Targeting Theranostic Probes for Enhanced Anticancer Activities
Xu Zhang,Xu Zhang,Qian Ba,Zhanni Gu,Zhanni Gu,Diliang Guo,Diliang Guo,Yu Zhou,Yungen Xu,Hui Wang,Deju Ye,Hong Liu,Hong Liu +12 more
TLDR
The potential of using mitochondria-targeting fluorophores to selectively trigger and directly visualize subcellular drug delivery in living cells is highlighted.Abstract:
Mitochondria-targeting theranostic probes that enable the simultaneously reporting of and triggering of mitochondrial dysfunctions in cancer cells are highly attractive for cancer diagnosis and therapy. Three fluorescent mitochondria-targeting theranostic probes have been developed by linking a mitochondrial dye, coumarin-3-carboximide, with a widely used traditional Chinese medicine, artemisinin, to kill cancer cells. Fluorescence images showed that the designed coumarin-artemisinin conjugates localized mainly in mitochondria, leading to enhanced anticancer activities over artemisinin. High cytotoxicity against cancer cells correlated with the strong ability to accumulate in mitochondria, which could efficiently increase the intracellular reactive oxygen species level and induce cell apoptosis. This study highlights the potential of using mitochondria-targeting fluorophores to selectively trigger and directly visualize subcellular drug delivery in living cells.read more
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Artemisinin as an anticancer drug: Recent advances in target profiling and mechanisms of action
Yin Kwan Wong,Chengchao Xu,Karunakaran A. Kalesh,Yingke He,Qingsong Lin,W.S. Fred Wong,Han-Ming Shen,Jigang Wang +7 more
TL;DR: The mechanism of artemisinin activation in cancer, novel and significant findings with regards to art Artemisinin target proteins and pathways, new understandings in artemisInin‐induced cell death mechanisms, as well as the practical issues of repurposing artemis inin are discussed.
Journal ArticleDOI
Coumarin-containing hybrids and their anticancer activities.
Longfei Zhang,Zhi Xu +1 more
TL;DR: This review aims to summarize the recent advances made towards the development of coumarin-containing hybrids as potential anticancer agents, covering articles published between 2015 and 2019, and the structure-activity relationship together with mechanisms of action are also discussed.
Journal ArticleDOI
Artemisinin, the Magic Drug Discovered from Traditional Chinese Medicine
TL;DR: An overview of the story of artemisinin in terms of its past, present, and future is provided, and the importance of relating mechanistic studies to therapeutic outcomes is emphasized, both in malarial and non-malarial contexts.
Journal ArticleDOI
Selective Dual‐Channel Imaging on Cyanostyryl‐Modified Azulene Systems with Unimolecularly Tunable Visible–Near Infrared Luminescence
TL;DR: The integration of an azulene and a cyanostyryl moiety into one skeleton is carried out for the generation of in situ stimuli-responsive luminescent materials, with the aim to achieve tunable and effective emissions in distinct channels through smart molecular design on a single-molecular platform.
Journal ArticleDOI
Artemisinin-Luminol Chemiluminescence for Forensic Bloodstain Detection Using a Smart Phone as a Detector.
Wenyue Gao,Chao Wang,Chao Wang,Kateryna Muzyka,Kateryna Muzyka,Shimeles Addisu Kitte,Jianping Li,Wei Zhang,Guobao Xu +8 more
TL;DR: In the present study, artemisinin has been exploited for the forensic bloodstain chemiluminescence detection for the first time and shows excellent selectivity against many common species.
References
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Journal ArticleDOI
Mitochondria: more than just a powerhouse.
TL;DR: A recent review as mentioned in this paper highlights the emerging evidence that provides molecular definition to mitochondria as a central platform in the execution of diverse cellular events, including cell-cycle control, development, antiviral responses and cell death.
Journal ArticleDOI
High-level semi-synthetic production of the potent antimalarial artemisinin
Christopher J. Paddon,Patrick J. Westfall,Douglas J. Pitera,Kirsten R. Benjamin,Karl Fisher,Derek McPhee,Michael D. Leavell,Anna Tai,A. Main,Diana Eng,Devin R Polichuk,Keat H. Teoh,Darwin W. Reed,T. Treynor,Jacob R. Lenihan,Hanxiao Jiang,M. Fleck,S. Bajad,G. Dang,D. Dengrove,Don Diola,G. Dorin,Kenneth W. Ellens,Scott Fickes,J. Galazzo,Sara P. Gaucher,T. Geistlinger,Ronald Henry,M. Hepp,Tizita Horning,T. Iqbal,L. Kizer,B. Lieu,D. Melis,Nathan A. Moss,Rika Regentin,S. Secrest,H. Tsuruta,R. Vazquez,Lars F. Westblade,Lan Xu,M. Yu,Yansheng Zhang,Lishan Zhao,Jefferson C. Lievense,Patrick S. Covello,Jay D. Keasling,K. K. Reiling,N. S. Renninger,Jack D. Newman +49 more
TL;DR: The strains and processes described here form the basis of a viable industrial process for the production of semi-synthetic artemisinin to stabilize the supply of art Artemisinin for derivatization into active pharmaceutical ingredients (for example, artesunate) for incorporation into ACTs.
Journal ArticleDOI
Targeting mitochondria for cancer therapy
Simone Fulda,Lorenzo Galluzzi,Lorenzo Galluzzi,Lorenzo Galluzzi,Guido Kroemer,Guido Kroemer,Guido Kroemer +6 more
TL;DR: The mitochondrial metabolism of cancer cells is deregulated owing to the use of glycolytic intermediates, which are normally destined for oxidative phosphorylation, in anabolic reactions and activation of the cell death machinery by stimulating mitochondrial membrane permeabilization could therefore be promising therapeutic approaches.
Journal ArticleDOI
Targeting mitochondria metabolism for cancer therapy
TL;DR: Accumulating evidence now suggests that mitochondrial bioenergetics, biosynthesis and signaling are required for tumorigenesis, and emerging studies have begun to demonstrate that mitochondrial metabolism is potentially a fruitful arena for cancer therapy.
Journal ArticleDOI
Artemisinins target the SERCA of Plasmodium falciparum
Ursula Eckstein-Ludwig,Richard Webb,I. D. A. van Goethem,J M East,Anthony G. Lee,Masatsugu Kimura,Paul M. O'Neill,Patrick G. Bray,Stephen A. Ward,Sanjeev Krishna +9 more
TL;DR: It is shown that artemisinins, but not quinine or chloroquine, inhibit the SERCA orthologue (PfATP6) of Plasmodium falciparum in Xenopus oocytes with similar potency to thapsigargin (another sesquiterpene lactone and highly specific SERCA inhibitor).