Uses
Bryostatin 1 has been used to study its effects on spontaneous Crohn′s disease (CD) like colitis in?mice. It has also been used to study its effects as an anthelmintic drug on adult
Syphacia muris infection in rats.
Definition
ChEBI: A member of the class of bryostatins that is (17E)-2-oxooxacyclohexacos-17-ene which is substituted by hydroxy groups at positions 4, 10, and 20; an acetoxy group at position 8; methyl groups at positions 9, 9, 18, and 19; 2-methoxy-2-oxoe
hylidene groups at positions 14 and 24; an (E,E)-octa-2,4-dienoyloxy group at position 21; and with oxygen bridges linking positions 6 to 10, 12 to 16, and 20 to 24. It is one of the most abundant member of the class of br
ostatins.
Biological Activity
Protein kinase C (PKC) activator that binds with high affinity (K i = 1.35 nM). Initially activates and subsequently induces downregulation of PKC isozymes. Sensitizes tumor cells to cytotoxic effects of anticancer agents.
Biochem/physiol Actions
Bryostatin 1 (Bry1) is a macrocyclic lactone. This synaptogenic compound is obtained from the marine bryozoan?Bugula neritina. Bry1 is capable of reversing synaptic loss. It can enable synaptic maturation in animal models with several neurological disorders. It possesses antidepressant activity, when administered intracebroventricularly. Bry1 is known to participate in protecting cell tight junctions (TJs), anti-inflammatory functions and immune regulation.
References
[1]. gschwendt m, fürstenberger g, rose-john s, et al. bryostatin 1, an activator of protein kinase c, mimics as well as inhibits biological effects of the phorbol ester tpa in vivo and in vitro. carcinogenesis, 1988, 9(4): 555-562.
[2]. stone rm, sariban e, pettit gr, et al. bryostatin 1 activates protein kinase c and induces monocytic differentiation of hl-60 cells. blood, 1988, 72(1): 208-213.
[3]. schuchter lm, esa ah, may s, et al. successful treatment of murine melanoma with bryostatin 1. cancer res, 1991, 51(2): 682-687.
