Results 121 to 130 of about 1,175 (153)
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Mechanism of eukaryotic protein synthesis inhibition by brusatol
Nucleic Acids and Protein Synthesis, 1981The mechanism by which brusatol inhibits protein synthesis in rabbit reticulocytes has been investigated. When added to reticulocyte lysates, brusatol inhibits endogenous protein synthesis only after a lag of 2-4 min at 30 degrees C. During this period 80 S ribosomes accumulate.
Stephen G Chaney +2 more
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Identification of a 3-β-homoalanine conjugate of brusatol with reduced toxicity in mice
Bioorganic and Medicinal Chemistry Letters, 2020 Brusatol, a quassinoid natural product, is effective against multiple diseases including hematologic malignancies, as we reported recently by targeting the PI3Kγ isoform, but toxicity limits its further development. Herein, we report the synthesis of a series of conjugates of brusatol with amino acids and short peptides at its enolic hydroxyl at C-3. A
Yonggang Pei +2 more
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Brusatol suppresses the growth of intrahepatic cholangiocarcinoma by PI3K/Akt pathway
Phytomedicine, 2022Intrahepatic cholangiocarcinoma (ICC) is a malignancy with a hidden onset, high metastasis recurrence rate, and poor prognosis. Research on effective drugs for ICC is important for improving the prognosis of patients in the clinic. Brusatol is a quassinoid extracted from the seeds of Brucea sumatrana and has been shown to have the potential to inhibit ...
Ziyan Chen +9 more
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In vitro antimalarial and cytotoxic activities of semisynthetic derivatives of brusatol
European Journal of Medicinal Chemistry, 1993Brusatol 2a was converted to the amide 2d, then the hydroxyl function on ring A of both compounds was acylated by a lipidic alpha-amino acid to give compounds 2b and 2e. To assess the effect of the size of the alkyl side chain on the biological activity the acetate 2c was also produced.
István Tóth
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Pharmacokinetic, metabolic profiling and elimination of brusatol in rats
Biomedical Chromatography, 2018AbstractBrusatol, a quassinoid isolated from the traditional Chinese medicine Brucea javanica, has been reported to be an inhibitor of Nrf2 pathway and has great potential to be developed into a novel chemotherapeutic adjuvant. However, the in vivo process of brusatol has not been comprehensively explained yet.
Nan Guo, Xin Xu, Guiyan Yuan
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Journal of Natural Products, 1987
The quassinoids bruceoside-A [1], brusatol [2], and bruceolide [3] were tested for antimalarial activity in vitro against the chloroquine-resistant (Smith) isolates of Plasmodium falciparum. Compound 2 was quite active, 1 was not active, and 3 showed only a trace of activity.
K H, Lee, S, Tani, Y, Imakura
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The quassinoids bruceoside-A [1], brusatol [2], and bruceolide [3] were tested for antimalarial activity in vitro against the chloroquine-resistant (Smith) isolates of Plasmodium falciparum. Compound 2 was quite active, 1 was not active, and 3 showed only a trace of activity.
K H, Lee, S, Tani, Y, Imakura
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Spectroscopic Studies of Brusatol
Journal of Natural Products, 1989An approach to the absolute stereochemistry of brusatol, an antitumor quassinoid isolated from Brucea javanica, by a combination of high-resolution mmr and cd spectroscopic ...
Yoshihiro Harigaya +7 more
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Brusatol inhibits the response of cultured beta-cells to pro-inflammatory cytokines in vitro
Biochemical and Biophysical Research Communications, 2015 Brusatol is a natural terpenoid that is capable of inducing a variety of biological effects. We presently report that this substance dramatically improves beta-cell survival when exposed to pro-inflammatory cytokines (IL-1β and IFNγ) in vitro. This was observed in insulin producing rat (RIN-5AH), mouse (βTC6) and human (EndoC-βH1) beta-cell lines ...
Nils Welsh
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A structure–activity relationship study of brusatol, an antitumor quassinoid
Tetrahedron, 2006Abstract Analogues of brusatol ( 2 ) were prepared and examined for their cytotoxic activity by using P-388 murine leukemia cells. The following structure–activity relationships were noted: (i) an enone carbonyl oxygen or an enolic oxygen at C-2 is essential, but an oxygen at C-3 not essential for the activity; (ii) the C-11 β-hydroxyl group is ...
Yukio Hitotsuyanagi +4 more
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Brusatol hinders the progression of bladder cancer by Chac1/Nrf2/SLC7A11 pathway
Experimental Cell ResearchBladder cancer is a common tumor that impacts the urinary system and marked by a significant fatality rate and an unfavorable prognosis. Promising antineoplastic properties are exhibited by brusatol, which is obtained from the dried ripe fruit of Brucea javanica.
Ziqi He, Qinghua Wang, Shuai Ke
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