pafr

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

3'-Methoxydaidzein is a dual isoflavone and Sodium Channel inhibitor. 3'-Methoxydaidzein inhibited NaV1.7, NaV1.8 and NaV1.3 with IC50 of 181 nM, 397 nM and 505 nM, respectively. 3'-Methoxydaidzein was specific for collagen-induced platelet aggregation with IC50 values of 12.3 and 61.5µM, respectively. 3'-Methoxydaidzein acts as an analgesic by inhibiting voltage-gated sodium channels. 3'-Methoxydaidzein showed antioxidant activity and antiplatelet aggregation activity.

1-Cinnamoylpyrrolidine, a natural product prepared from Piper caninum, can be used as a DNA strand breaking agent, inducing the relaxation of the plasmid pBR322 DNA superhelix in the presence of Cu2+. 1-Cinnamoylpyrrolidine inhibits PAF-induced platelet aggregation with an IC50 value of 37.3 μM. value was 37.3 μM.

Ginkgolide B (BN-52021) is a PAFR antagonist(IC50=3.6 μM) isolated from Ginkgo biloba.

Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is extracted from Siam weeds and demonstrates anti-inflammatory activity via the NF-κB pathway.

Pregomisin shows platelet-activating factor (PAF) antagonistic activity and the IC 50 value is 4.8x10(-5) M.

Kadsurin A has anti-platelet activating factor activities.

(+)-Acuminatin exerts hepatoprotective activities, perhaps by serving as a potent antioxidant. (+)-trans-Acuminatin, and (+)-cis-acuminatin show weak activity against platelet aggregation with IC50 values of 108.5 and 90.02 uM, respectively. (+)-Acuminatin, and machilin G show dose-dependent potent inhibitory activities against PLCgamma1 in vitro with IC50 values ranging from 8.8 to 26.0 microM, the inhibition of PLCgamma1 may be an important mechanism for an antiproliferative effect on the human cancer cells, therefore, these inhibitors may be utilized as cancer chemotherapeutic and chemopreventive agents.

Cyclocommunol exhibits cytotoxicity against hepatocellular carcinoma (SMMC-7721) and gastric carcinoma (BGC-823 and SGC-7901) cell lines. It also shows strong inhibition of arachidonic acid (AA)- and collagen-induced platelet aggregation.

Epiyangambin is a phytotoxic lignan, it shows inhibition of seed germination of Agrostis stolonifera cv. penncross (Poaceae) and inhibition of development of Lactuca sativa L. (Asteraceae) seedlings in a microassay using 24-well plates. Epiyangambin exhibits significant inhibition of the transformation of murine epidermal JB6 cells, with the IC50 value of 0.15 microg mL. (+)-Epiyangambin also has anti-platelet aggregation activity.

Bisdethiobis(methylthio)gliotoxin is a platelet activating factor (PAF) antagonist.

Zingiberen newsaponin is a steroidal saponin from Dioscorea zingiberensis.

Spiradine F can significantly inhibit platelet-activating factor(PAF)-induced platelet aggregation in a concentration-dependent manner.

Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.

6-Deoxyjacareubin exhibits potent antioxidant and antifungal activities. 6-Deoxyjacareubin inhibits platelet activating factor (PAF) receptor with an IC50 of 29.0 microM and can be used in studies about natural PAF receptor antagonists.

(-)-Denudatin B (Denudatin B) is derived from Magnolia fargesii. (-)-Denudatin B has nonspecific antiplatelet action at high concentration by inhibiting phosphoinositides breakdown induced by collagen and thrombin.

1-Methoxyphaseollidin exhibits anti-Helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains. 1-Methoxyphaseollidin may show moderate cytotoxic activity against KB and L1210 cells. 1-Methoxyphaseollidin also shows inhibition of lysoPAF acetyltransferase activity.

Piperolactam C possesses anti-platelet aggregation activity in vitro. It can inhibit the growth of the fungi Cladosporium sphaerospermum and C. cladosporioides.

Cryptomeridiol is a potential skin-whitening agent, exhibits melanogenesis inhibitory activity on α-MSH-stimulated B16 melanoma cells. Cryptomeridiol has low activity against A. niger, T. mentagrophytes, and C. albicans. (-)-Cryptomeridiol also exhibits a significant and concentration-dependent inhibitory effect on PAF receptor binding, with inhibitory concentration (IC)(50) values of 17.5 uM.

Futoenone and a series of its derivatives have shown inhibitory activities against matrix metalloproteinases, the molecular modelings of these compounds indicate the preferred binding of the P2' site of the enzymes. Neolignan derivative compounds of the 2,4-diaryl-1,3-dithiolane and futoenone variety exhibit both platelet activating factor receptor(PAF)and 5-lipoxygenase antagonist activity.

Aristolactam AII has cytotoxic activity, it also shows platelet aggregation inhibitory activity.

6-Acetyl-2,2-dimethylchroman-4-one and vanillin exhibit anti-platelet aggregation activity induced by arachidonic acid in vitro.

2-Hydroxy-3-methoxybenzoic acid glucose ester shows a potent antagonistic activity against platelet activating factor (PAF), it can prevent the mice from the PAF-induced death at a dose of 300 micrograms mouse.