xiap

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an O-methylated flavone found in various plants, exhibiting antinociceptive, anti-inflammatory, and antioxidant activities in different research models.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).

Neoandrographolide (Neoandrographiside) has potent hypolipidemic effect and protects the cardiovascular without significant liver damage.Neoandrographolide has anti-inflammatory effect, might result from inhibition of iNOS and COX-2 expression through inhibiting p38 MAPKs activation.Neoandrographolide as chemosensitizer in S-Jurkat and X chromosome-linked inhibitor of apoptosis protein (XIAP)-overexpressing Jurkat cells, a model for chemoresistance.

Alpinetin ((-)-alpinetin) has antibacterial activity.Alpinetin has anti-inflammatory activity.Alpinetin can enhance the sensitivity of HepG2 hepatoma cells to the chemotherapeutic agent CDDP. Alpinetin has strong anti-hepatoma and pancreatic cancer cells effects, by inhibiting proliferation , regulating of the Bcl-2 family and XIAP expression, releasing of cytochrome c and activating caspases.

Sanggenon G, a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP), specifically binds to the XIAP BIR3 domain with a binding affinity of 34.26 μM, thereby enhancing caspase activation [1].

β-Carotene-15,15ʹ-epoxide acts as an XIAP antagonist with pro-apoptotic (Apoptosis) and anti-tumor properties, found in the leaves of Spondias mombin. In rat models of DMBA-induced breast cancer, it induces tumor cell apoptosis by binding to the BIR3 domain of the XIAP protein, thereby inhibiting its interaction with caspase-9. Additionally, β-carotene-15,15ʹ-epoxide significantly reduces BCL-2, COX-2, and TNF-α expression in tumor tissue, decreases MDA levels, enhances catalase activity, and modulates biochemical markers in serum such as LDH, ALP, and ALT, indicating its antioxidant, anti-inflammatory, and metabolic protective effects. This compound is useful for researching inflammation-related diseases and tumors such as breast cancer.

Hellebrigenin, as a selective inhibitor of MAPK signaling pathways (ERK, p38, JNK) and XIAP, effectively suppresses Akt expression and phosphorylation. This compound activates endogenous apoptosis pathways (including mitochondrial membrane potential disruption, Caspase family activation, and PARP cleavage) while modulating apoptosis-related protein expression. Hellebrigenin also induces DNA double-strand breaks to activate the ATM pathway, inhibiting tumor cell proliferation and clonogenesis, primarily applied in research of oral squamous cell carcinoma and liver cancer.