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Guaianolide sesquiterpene lactones, a source to discover agents that selectively inhibit acute myelogenous leukemia stem and progenitor cells.

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Small molecules that can selectively target cancer stem cells (CSCs) remain rare currently and exhibit no common structural features. Here we report a series of guaianolide sesquiterpene lactones (GSLs) and their derivatives that can selectively eradicate acute myelogenous leukemia (AML) stem or

The application of Heck reaction in the synthesis of guaianolide sesquiterpene lactones derivatives selectively inhibiting resistant acute leukemic cells.

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A series of guaianolide-type sesquiterpene lactones derivatives with arylation of α-methylene-γ-lactone moiety was synthesized using Heck reactions, and was evaluated for their activities against acute myelogenous leukemia (AML) cell line HL-60 and doxorubicin-resistant cell line HL-60/A. Although

Antineoplastic effects and mechanisms of micheliolide in acute myelogenous leukemia stem cells.

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Leukemic stem cells (LSCs) greatly contribute to the initiation, relapse, and multidrug resistance of leukemia. Current therapies targeting the cell cycle and rapidly growing leukemic cells, including conventional chemotherapy, have little effect due to the self-renewal and differentiated malignant

Carpedilactones A-D, four new isomeric sesquiterpene lactone dimers with potent cytotoxicity from Carpesium faberi.

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Four new isomeric sesquiterpene lactone dimers, carpedilactones A-D (1-4), were isolated from the acetonic extract of Carpesium faberi. Among them, 1-3 are the first three 2,4-linked exo-Diels-Alder adducts between a eudesmanolide dienophile and a guaianolide diene. The absolute configurations of

NF-κB dependent anti-inflammatory activity of chlorojanerin isolated from Saussurea heteromalla.

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Medicinal plants have shown great promise as a source of novel drug compounds for the treatment of inflammatory disorders. In our search for new entities with anti-inflammatory potential, the extracts of the whole plant of Saussurea heteromalla (family-Asteraceae), collected from Himalayas, were

Bioactivity-guided isolation of cytotoxic sesquiterpene lactones of Gochnatia polymorpha ssp. floccosa.

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Phytochemical study of Gochnatia polymorpha (Less) Cabr. ssp. floccosa Cabr. trunk bark, guided by antiproliferative assays on 10 human cancer cell lines and the VERO cell line, yielded six known compounds identified as the triterpene bauerenyl acetate, the guaianolide 11α,13-dihydrozaluzanin C and

Synthesis and biological evaluation of amino analogs of Ludartin: potent and selective cytotoxic agents.

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Diverse amino analogs of Ludartin, a cytotoxic guaianolide and a position isomer of an anticancer drug, Arglabin were prepared through Michael type addition at its highly active α-methylene-γ-lactone motif. The semisynthetic derivatives were subjected to sulphorhodamine B cytotoxicity assay against

Dynamin-related protein 1 is involved in micheliolide-induced breast cancer cell death.

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Dynamin-related protein 1 (Drp1) is a newly discovered therapeutic target for tumor initiation, migration, proliferation, and chemosensitivity. Thus, therapeutic strategies that focus on targeting Drp1 and its related signaling pathway pave a new way to address the ineffectiveness of traditional

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