Search results for "IC50"
showing 10 items of 129 documents
Cytotoxic 14-Membered Macrolides from a Mangrove-Derived Endophytic Fungus, Pestalotiopsis microspora.
2016
Seven new 14-membered macrolides, pestalotioprolides C (2), D-H (4-8), and 7-O-methylnigrosporolide (3), together with four known analogues, pestalotioprolide B (1), seiricuprolide (9), nigrosporolide (10), and 4,7-dihydroxy-13-tetradeca-2,5,8-trienolide (11), were isolated from the mangrove-derived endophytic fungus Pestalotiopsis microspora. Their structures were elucidated by analysis of NMR and MS data and by comparison with literature data. Single-crystal X-ray diffraction analysis was used to confirm the absolute configurations of 1, 2, and 10, while Mosher's method and the TDDFT-ECD approach were applied to determine the absolute configurations of 5 and 6. Compounds 3-6 showed signif…
Furoquinolines and dihydrooxazole alkaloids with cytotoxic activity from the stem bark of Araliopsis soyauxii.
2018
Abstract Two new furoquinoline alkaloids, maculine B (1) and kokusaginine B (2) and one new dihydrooxazole alkaloid, veprisazole (3), along with four known compounds namely, N13-methyl-3-methoxyrutaecarpine (4), flindersiamine (5), skimmianine (6) and tilianin (7) were isolated from the methanol extract of the stem bark of Araliopsis soyauxii Engl. by various chromatographic methods. Their structures were determined using spectrometry and spectroscopic techniques including NMR and MS. The cytotoxicity of the new compounds compared to that of doxorubicin, the reference anticancer compound, was determined on a panel of nine cancer cell lines including sensitive and drug resistant phenotypes. …
Rotenoids, Flavonoids, and Chalcones from the Root Bark of Millettia usaramensis.
2015
Five new compounds, 4-O-geranylisoliquiritigenin (1), 12-dihydrousararotenoid B (2), 12-dihydrousararotenoid C (3), 4'-O-geranyl-7-hydroxyflavanone (4), and 4'-O-geranyl-7-hydroxydihydroflavanol (5), along with 12 known natural products (6-17) were isolated from the CH2Cl2/MeOH (1:1) extract of the root bark of Millettia usaramensis ssp. usaramensis by chromatographic separation. The purified metabolites were identified by NMR spectroscopic and mass spectrometric analyses, whereas their absolute configurations were established on the basis of chiroptical data and in some cases also by X-ray crystallography. The crude extract was moderately active (IC50 = 11.63 μg/mL) against the ER-negative…
Naphthalene Derivatives from the Roots of Pentas parvifolia and Pentas bussei
2016
The phytochemical investigation of the CH2Cl2/MeOH (1:1) extract of the roots of Pentas parvifolia led to the isolation of three new naphthalenes, parvinaphthols A (1), B (2), and C (3), two known anthraquinones, and five known naphthalene derivatives. Similar investigation of the roots of Pentas bussei afforded a new polycyclic naphthalene, busseihydroquinone E (4), a new 2,2'-binaphthralenyl-1,1'-dione, busseihydroquinone F (5), and five known naphthalenes. All purified metabolites were characterized by NMR and MS data analyses, whereas the absolute configurations of 3 and 4 were determined by single-crystal X-ray diffraction studies. The E-geometry of compound 5 was supported by DFT-base…
Molecular Search of New Active Drugs AgainstToxoplasma Gondii
1999
Molecular connectivity has been applied to the search of new compounds with activity against the protozoan Toxoplasma gondii, using a stepwise linear discriminant analysis (SLDA) which is able to classify a compound according its activity either as active or as inactive. Among the selected compounds, andrographolide and dibenzotiophene sulfone stand out, both with IC50 values lower than 1 microgram/ml, which are comparable to these of drugs such as sulfamethoxazole, pyrimethamine and trimethoprim, with IC50 values equal to 1.1, 0.04 and 2.31 micrograms/ml, respectively. These results confirm the usefulness of our topological approach for the selection and design of new-lead drugs active aga…
Receptor Binding Properties of the New and Specific Thromboxane Receptor Antagonist Bay U 3405
1992
Human platelet membranes were used to characterize the receptor binding properties of the specific thromboxane receptor antagonist 3H-SQ 29548 and the displacement of 3H-SQ 29548 from its binding site by the new thromboxane receptor antagonist Bay u 3405. The specific binding of 3H-SQ 29548 was saturable with an association rate constant of 1 x 10(-11) mol-1 min-1 and a dissociation rate constant of 0.032 min-1. Nonspecific binding of 3H-SQ 29548 was below 10%. When Scatchard plot analysis was performed on equilibrium saturation binding the kD was 69 nmol/l and the Bmax was calculated as 3.9 pmol/mg membrane protein. 3H-SQ 29548 was dose dependently displaced from its binding site by additi…
Interactive effects of zearalenone and its metabolites on cytotoxicity and metabolization in ovarian CHO-K1 cells.
2014
Zearalenone (ZEA) is a non-steroidal estrogen mycotoxin with high binding affinity to estrogen receptors. ZEA is rapidly absorbed and metabolized in vivo to α-zearalenol (α-ZOL) and β-zearalenol (β-ZOL). So, mixtures of them may be present in biological systems and suppose a hazard to animals and human health. The aims of this study were to determine the cytotoxic effects of ZEA and its metabolites, alone and in combination in ovarian (CHO-K1) cells during 24, 48 and 72h by the MTT assay; and to investigate the metabolism of the CHO-K1 cells on ZEA, and its conversion into α-ZOL and β-ZOL by CHO-K1 cell after 24 and 48h of exposure. The IC50 value obtained for individual mycotoxins range fr…
Synthesis of 5H-pyrido[3,2-b]pyrrolizin-5-one tripentone analogs with antitumor activity
2018
Abstract Pyrrolizinones represent an interesting class of compounds with varied degrees of structural complexity and pharmacological activity. Among these, 9H-pyrido[2,3-b]pyrrolizin-9-one, tripentone analogs, recently reported by us, showed significant antiproliferative activity against human tumor cell lines, inducing apoptosis and not affecting viability of Caco-2 differentiated in normal intestinal-like cells. Considering their interesting biological activity, their 5H-pyrido[3,2-b]pyrrolizin-5-one analogs were efficiently synthesized in good to excellent yields (61–91%). All tripentone derivatives were tested to assess their cytotoxicity against two human tumor cell lines, HCT-116 (hum…
Vaccinum ģints ogu spiedpalieku ekstraktu efekti uz alfa glikozidāzes aktivitāti
2018
Alfa-glikozidāzes inhibitori ir orāli pretdiabēta līdzekļi, ko lieto 2. tipa cukura diabēta ārstēšanai, lai novērstu vai palēninātu ogļhidrātu (piemēram, cietes un cukura) gremošanu. Arī starp dabas vielām tiek meklēti alfa-glikozidāzes inhibitori. Darba mērķis: pētīt melleņu, krūmmelleņu, lielogu dzērveņu, dzērveņu un brūkleņu ogu spiedatlieku ekstraktu ietekmi uz alfa glikozidāzes aktivitāti in vitro. Pētījumā ogu sauso ekstraktu aktivitāte ir pētīta ūdens un metanola ekstraktu šķīdumiem. Rezultāti liecina, ka visiem šo ogu ekstraktiem ir alfa glikozidāzes inhibēšanas spēja, bet ekstraktu šķīdumiem ūdenī tā ir gandrīz 10 reizes vājāka kā metanola. No ekstraktu šķīdumiem metanolā vislielāk…
Zileņu izspiedu ekstrakta pretiekaisuma efekti in vitro
2020
Savvaļas ogu bioaktīvi fitoķīmiski savienojumi kopā spēj uzrādīt virkni bioloģisko aktivitāšu, ietekmējot cilvēku veselību. Veselību ietekmējošās bioloģiskās aktivitātes galvenokārt attiecināmas uz sastāvā esošajiem polifenoliem, kuriem piemīt antioksidantu, pretiekaisuma un pretmikrobu īpašības. Darba mērķis ir pētīt zileņu izspiedu ekstrakta pretiekaisuma efektus in vitro. Pētījumā tika pētīta zileņu izspiedu ekstrakta ietekme uz iekaisuma procesos iesaistīto enzīmu - ksantīnoksidāzes, lipoksigenāžu 5 un 15 (LOX-5 un LOX-15) un ciklooksigenāzes 1 (COX-1) aktivitāti, izmantojot fluorimetriskās un kolorimetriskās metodes. Rezultāti liecina, ka zileņu izspiedu ekstrakts inhibē COX-1, LOX-5 u…