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• 470-17-7 isoalantolactone 

Relevant academic research and scientific papers

Structural investigation and biological activity of sesquiterpene lactones from the Traditional Chinese Herb Inula racemosa

Five new sesquiterpene lactones, racemosalactones A-E (1-5), along with 19 known sesquiterpene latones (6-24), were isolated from the roots of Inula racemosa. Their structures were elucidated by extensive spectroscopic analysis, and the absolute configuration of 2 was deduced from X-ray diffraction analysis. Compounds 1, 6, 8, 10, 12, 14, and 17 exhibited antiproliferative activities with IC50 values ranging from 0.38 to 4.19 μg/mL against human non-small-cell lung cancer A549, hepatocellular carcinoma HepG2, and human fibrosarcoma HT1080 cells. Compounds 6 and 8 exhibited antiproliferative activities against endothelial cells with IC50 values of 2.4 and 2.5 μg/mL, respectively. Furthermore, compounds 6 and 8 both inhibited endothelial cell tube formation at 1.0 μg/mL. A method for the rapid and straightforward preparative-scale isolation of compound 6 from alantolides is described.

Sesquiterpene lactone nitrogen methyl piperazine derivative and salt thereof, and application thereof in medicine preparation

The invention relates to sesquiterpene lactone nitrogen methyl piperazine derivatives and pharmaceutically acceptable salts thereof, and applications thereof in medicine preparation. The invention concretely relates to compounds represented by formulas (I), (II), (III) and (IV), and pharmaceutically acceptable salts thereof, as well as the applications of the compounds shown in formulas (I), (II), (III) and (IV) and pharmaceutically acceptable salts and compositions thereof for preparing anti-cancer or auxiliary anti-cancer drugs.

Isolation, Chemical Transformation, and Antifungal Potential of Sesquiterpene Lactones from Inula Racemosa

The present study reports the isolation of two eudesmanolide type sesquiterpenoid lactones, viz. alantolactone and isoalantolactone, from the roots of Inula racemosa Hook L. and their chemical transformations using various reagents. All the compounds isol

Synthetic Transformations of Sesquiterpene Lactones. 11.* Conjugates Based on Caffeine and Eudesmanolides with N-Containing Linkers

8-(Aminoalkylamino)caffeine or 8-(piperazinyl)caffeine were formed in high yields by reacting 8-bromo- or 8-chlorocaffeine with linear and cyclic diamines using microwave-assisted organic synthesis. These amines were highly reactive in Michael reactions with sesquiterpene lactones containing active methylene groups. Conjugates with caffeine and eudesmanolide moieties bonded by a N-containing linker were synthesized.

Isoalantolactone derivative, pharmaceutical composition and application thereof

The invention relates to an isoalantolactone derivative, a pharmaceutical composition and application thereof, especially use of the isoalantolactone derivative shown as formula (I) or a salt pharmaceutical compound thereof in preparation of adjuvant drugs treating cancer, a pharmaceutical composition containing a therapeutically effective amount of isoalantolactone derivative (I) or its salt anda pharmaceutically acceptable carrier or a composition with other anticancer drugs.

Synthesis and discovery of a drug candidate for treatment of idiopathic pulmonary fibrosis through inhibition of TGF-β1 pathway

In this study, anti-IPF lead compounds 42 and 44, derived from natural sesquiterpene lactones Isoalantolactone and alantolactone, were discovered by screening from a high-throughput TGF-β1 reporter luciferase assay. Notably, they could reduce the myofibroblast activation and extracellular matrix deposition both in vitro and in vivo. Additionally, compounds 42 and 44 could significantly attenuate bleomycin-induced pulmonary fibrosis in mice. Further validation of pharmacokinetics study and toxicity evaluation indicated that compound 44 might be a promising anti-IPF drug candidate.

Isoalantolactone derivative promotes glucose utilization in skeletal muscle cells and increases energy expenditure in db/db mice via activating AMPK-dependent signaling

Augmenting glucose utilization and energy expenditure in skeletal muscle via AMP-activated protein kinase (AMPK) is an imperative mechanism for the management of type 2 diabetes. Chemical derivatives (2a-2h, 3, 4a-4d, 5) of the isoalantolactone (K007), a bioactive molecule from roots of Inula racemosa were synthesized to optimize the bioactivity profile to stimulate glucose utilization in skeletal muscle cells. Interestingly, 4a augmented glucose uptake, driven by enhanced translocation of glucose transporter 4 (GLUT4) to cell periphery in L6 rat skeletal muscle cells. The effect of 4a was independent to phosphatidylinositide-3-kinase (PI-3-K)/Akt pathway, but mediated through Liver kinase B1 (LKB1)/AMPK-dependent signaling, leading to activation of downstream targets acetyl coenzyme A carboxylase (ACC) and sterol regulatory element binding protein 1c (SREBP-1c). In db/db mice, 4a administration decreased blood glucose level and improved body mass index, lipid parameters and glucose tolerance associated with elevation of GLUT4 expression in skeletal muscle. Moreover, 4a increased energy expenditure via activating substrate utilization and upregulated the expression of thermogenic transcription factors and mitochondrial proteins in skeletal muscle, suggesting the regulation of energy balance. These findings suggest the potential implication of isoalantolactone derivatives for the management of diabetes.

Isoalantolactone derivative and application of salt of isoalantolactone derivative in preparation of medicine for treating thyroiditis

The invention discloses an isoalantolactone derivative and application of salt of the isoalantolactone derivative in preparation of a medicine for treating thyroiditis, and provides an isoalantolactone derivative as shown in formula (I); salifying acid is inorganic acid or organic acid; the inorganic acid is selected from hydrofluoric acid, hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, phosphoric acid, carbonic acid, boric acid, seleninic acid, phosphomolybdic acid, phosphorous acid and sulphurous acid; the organic acid is selected from citric acid, maleic acid, D-malic acid, L-malic acid, DL-malic acid, L-lactic acid, D-lactic acid, DL-acid, oxalic acid, methanesulfonic acid, valeric acid, oleic acid, lauric acid, p-toluene sulfonic acid, 1-naphthalenesulfonic acid, 2-naphthalene sulfonic acid, phthalic acid, tartaric acid, malonic acid, succinic acid, fumaric acid, glycollic acid, mercaptan acid, glycine, sarcosine, sulfonic acid, nicotinic acid, methyl pyridine acid, isonicotinic acid, benzoic acid or substituted benzoic acid.

Isoalantolactone derivatives and their application in preparation of drugs for treating inflammatory bowel diseases

Isoalantolactone derivatives and their application in preparation of drugs for treating inflammatory bowel diseases are provided, and an isoalantolactone derivative shown as in formula (I) is provided; a salt-forming acid is an inorganic acid or organic acid, the inorganic acid is selected from hydrofluoric acid, hydrochloric acid, hydrobromic acid, hydroiodic acid, sulfuric acid, nitric acid, phosphoric acid, carbonic acid, bromic acid, seleninic acid, phosphomolybdic acid, phosphorus acid and sulfurous acid, and the organic acid is selected from citric acid, maleic acid, D-malic acid, L-malic acid, DL-malic acid, L-lactic acid, D-lactic acid, DL-acid, oxalic acid, methylsulfonic acid, pentanoic acid, oleic acid, lauric acid, p-methylbenzene sulfonic acid, 1-naphthalene sulfonic acid, 2-naphthalene sulfonic acid, phthalic acid, tartaric acid, malonic acid, succinic acid, fumaric acid, glycolic acid, mercapturic acid, glycine, creatine, sulfonic acid, nicotinic acid, picolimic acid, isonicotinic acid, and benzoic acid or substituted benzoic acid.

Different elecampane lactone derivatives and salts thereof in the preparation of medicine for treating pulmonary fibrosis in the application of the (by machine translation)

Different elecampane lactone derivatives and salts thereof in the preparation of medicine for treating pulmonary fibrosis in the application, provides such as a kind of formula (I) indicated by the different elecampane lactone derivatives; to form the salt of the acid is an inorganic acid or organic acid, the inorganic acid is selected from hydrofluoric acid, hydrochloric acid, hydrobromic, hydroiodic, sulfuric acid, nitric acid, phosphoric acid, carbonic acid, boric acid, selenious acid, phosphomolybdic acid, phosphorous acid, sulfurous acid, the organic acid is selected from citric acid, maleic acid, malic acid D -, L - malic acid, DL - malic acid, L - lactic acid, D - lactic acid, DL - acid, oxalic acid, methanesulfonic acid, valeric acid, oleic acid, lauric acid, toluenesulfonates, 1 - naphthalene sulfonic acid, 2 - naphthalenesulfonic acid, phthalic, tartaric acid, malonic acid, succinic acid, fumaric acid, glycolic acid, sulfur hydroxy-acid, glycine, sarcosine, sulfonic acid, nicotinic acid, methyl pyridine acid, isonicotinic acid, benzoic acid or substituted benzoic acid. (by machine translation)