作者: Burattini, Sabrina ; Fimognari, Carmela ; Sestili, Piero ; Sissi, Claudia ; Turrini, Eleonora ; Diederich, Marc ; Milelli, Andrea ; Calcabrini, Cinzia ; Maffei, Francesca ; Guardigni, Melissa ; Greco, Giulia ; Schnekenburger, Michael ; Catanzaro, Elena

In search of semisynthetic derivatives with increased antitumor activity, we condensed sulforaphane (SFR) with rhodol, a fluorophore platform capable of modifying the intracellular trafficking and pharmacokinetics of the linked molecules. The two tested derivatives, namely MG28 and MG46, showed a far higher, as compared to SFR, cytotoxicity toward cancer cells. Apoptotic cell death was preceded by the extensive generation of DNA lesions, which were repaired relatively slowly and caused formation of micronuclei. Unlike SFR, rhodol-SFR conjugates' DNA lesions resulted from direct interactions with nuclear DNA. Overall, MG28 and MG46 exhibit a remarkable cytotoxic effect, which is the likely consequence of their direct and intense DNA damaging activity, i.e., a novel and peculiar mechanism arising from the conjugation of the parental rhodol and SFR. Considering that a wide number of clinically used drugs kill cancer cells by inducing DNA damage, MG could represent a new and promising chance in antitumor chemotherapy.

1986-03-01·Canadian Journal of Physiology and Pharmacology4区 · 医学

A comparison of the inhibitory effects of somatostatin-14, -25, and -28 on motility of the guinea pig ileum

4区 · 医学

Article

作者: Kwok, Yin Nam ; Brown, John C. ; Bakich, Victoria ; McIntosh, Christopher H. S.

A number of studies have suggested that somatostatin-14 (SS-14) and somatostatin-28 (SS-28) exhibit a similar spectrum of biological activities but have different potencies. In the present study the effects of SS-14, SS-28, and somatostatin-25 on electrically induced contractions of the guinea pig ileum have been compared. All three peptides exhibited equipotent inhibitory effects. Inhibition was obtained at a threshold concentration less than 10−10 M, with maximal inhibition at 10−7 M and IC50 values of 6.0–6.5 × 10−10 M. The N-terminal 14 amino acid fragment of SS-28 had no effect either on motility, when added alone, or on the actions of SS-28, suggesting that this region of the molecule is not critical for biological activity.

1968-08-30·Nuclear-Medizin

Experimentelle 28-Mg-Verteilungsstudien im Ganzkörperzähler.

Article

作者: Choné, B ; Jahns, E ; Misri, H T

100 项与 MG-28 相关的药物交易

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