Anti-leukemic activity

The histone deacetylase inhibitor ITF2357 has anti-leukemic activity in vitro and in vivo and inhibits IL-6 and VEGF production by stromal cells. Leukemia,... 

Extracts of Amaryllidaceae alkaloids have long been used in traditional medicine for the treatment of a variety of illnesses. As early as the fourth century B.C., Hippocrates had reputedly advised the use of preparations of Amaryllidaceae plants to control uterine tumours [157]. More recently, a systematic bioassay of these alkaloids of different structural types has revealed a diversity of interesting biological properties. Thus, (+)-pretazettine (369) [158,159], and ungeremine (182) [160] show anti-leukemic activity. Cytotoxicity was observed for (-)-lycorine (245) [161], (-)-pseudolycorine (574) [162], 6-a-hydroxycrinamine (575) [163],... 

Jones RJ, Sharkis SJ, Miller CB, Rowin-sky EK, Burke PJ, May WS. 1990. Bryostatin 1, a unique biologic response modifier anti-leukemic activity in vitro. Blood 75 1319-23... 

Usnic acid (7.53)—a highly biologically active dibenzofuran—is a phenol oxidation product of an acylphlorogludnol. It is produced by numerous lichens, including several Usnea species. Apart from its antibiotic and anti-leukemic activity, it has insect anti-feedant activity. Its presence may account for the observation that many lichens are resistant to serious insect attack. 

Myers, D., Yanishevski, Y., Masson, E., Irvin, J., Evans, W., and Uckun, F. (1995) Favorable pharmacodynamic features and superior anti-leukemic activity of B43 (anti-CD19) immunotoxins containing two pokeweed antiviral protein molecules covalently linked to each monoclonal antibody molecule. Leuk. Lymphoma 18, 93-102. 

Table 8. Anti leukemic Activity of Bisbrusatolyl and Brusatolyl Esters and Related Compounds against P>388 Lymphocytic Leukemia Cell Growth in BDFl Mice...

See, for example, Andrivon, W., et ai. A new anthracycline with potent anti-leukemic activity overcomes P-glycoprotein multidrug resistance. Leuk. Res. 1998, 22, 719-725. 

Chakrapani, H., Goodblatt, M.M., Udupi, V., Malaviya, S., Shami, P.J., Keefer, L.K., and Saavedra, J.E. (2008). Synthesis and in vitro anti-leukemic activity of structural analogues of js-k, an anti-cancer lead compound. Bioorg. Med. Chem. Lett. 18, 950-953. 

A third activity, anti-leukemic activity, has only been demonstrated by the maytansinoids 61—63,150). An insufficient number of compounds has been reported for extensive conclusions to be drawn, but it does appear that an ester at C-3 and a carbinolamide at C-9 are both required for anti-leukemic activity. 

Furlong MT et al (2012) A validated LC-MS/MS assay for the simultaneous determination of the anti-leukemic agent dasatinib and two pharmacologically active metabolites in human plasma application to a clinical pharmacokinetic study. J Pharm Biomed Anal 58 ... 

Heyneanol A (684) was demonstrated to possess anti-tumor activity, which may be mediated by apoptosis caused by cytochrome c release and caspase activation in human leukemic U937 cells [476]. 

Baurain R, Masquelier M, Deprezedcampeneere D, et al. Amino acid and dipeptide derivatives of daunorubicin. 2. cellular pharmacology and anti-tumor activity on L1210 leukemic-cells in vitro and in vivo. J Med Chem 1980 23 1171-1174. 

PP2A impaired activity is a common event in acute myeloid leukemia and its activation by forskolin has a potent anti-leukemic effect. Leukemia 25 606-614... 

NR Ferringi, JL McLaughlin, RG Powel, CR Smith. Use of potato disk and brine shrimp bioassay to detect activity and isolate piceatanol as the anti-leukemic principle from the seeds of Euphobia lagascae. J Nat Prod Al 347-352, 1984. 

Moreover, a recent study also revealed that ROS generation led to the activation of caspase-2 during p-carotene-induced apoptosis in the human leukemic T cell line Molt 4. The apoptosis progressed by simultaneous activation of caspase-8 and caspase-9, and a cross talk between these initiator caspases was mediated by the pro-apoptotic protein Bid. Inhibition of caspases 2, 8, 9, and 3 independently suppressed the caspase cascade. The cleavage of the anti-apoptotic protein BclXL was found to be another important event during P-carotene-induced apoptosis, suggesting the presence of an extensive feedback amplification loop in P-carotene-induced apoptosis (Prasad et al., 2006). 

A variety of biological activities have been associated with labdane diterpenes including antibacterial, antifungal, antiprotozoal, enzyme induction, anti-inflammatory modulation of immune cell functions, as well as cytotoxic and cytostatic effects against human leukemic cell lines. 

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