antagonistic

Voacamine (Voacanginine) is an indole alkaloid. Voacamine exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.Voacanginine may have rhythmic effects.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

Xanthotoxol (Psoralen) is a biologically active linear furocoumarin, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects.

Benzoylmesaconine (Mesaconine 14-benzoate) is the most abundant component of Wutou decoction, which is widely used in China because of its therapeutic effect on rheumatoid arthritis. Benzoylmesconine has analgesic activity. Benzoylmesconine may improve the resistance of T6S-mice (or thermally injured mice) to the infection of HSV-1, through the induction of antagonistic CD4+ T cells against burn-associated type-2 T cells.

Estetrol(Donesta) is an orally available, selective modulator of the estrogen receptor, a naturally occurring estrogen synthesized by the human fetal liver during pregnancy.Estetrol has effects on the endometrium or central nervous system, but is antagonistic to the breast.Estetrol may help to reduce thrombosis at low concentrations. Estetrol may be used to relieve menopausal symptoms.

Bimatoprost acid (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% compared to PGF2α for binding to the FP receptor on ovine luteal cells.

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

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)

1. Rhynchophylline (Mitrinermine) can protect against ischemic damage, probably via regulating the Akt mTOR pathway. 2. Rhynchophylline can protect against glutamate-induced neuronal death, can inhibit MA impairment in cultured neurons in vitro. 3. Rhynchophylline and isorhynchophylline have a non-competitive antagonistic effect on the NMDA-type ionotropic glutamate receptors, suggest that these alkaloids exert their protective action against ischemia-induced neuronal damage by preventing NMDA, muscarinic M1, and 5-HT2 receptors-mediated neurotoxicity during ischemia.

Gymnestrogenin has a dual LXRα± α2 antagonistic profile.

Kadsulignan L shows in vitro antiviral effects on hepatitis B virus. It also shows moderate platelet-activating factor (PAF) antagonistic activities with the IC50 value of 2.6 x 10(-5) M.

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.

Isopimaric acid is active against MDR and MRSA strains of S. aureus which are becoming increasingly resistant to antibiotics, the minimum inhibitory concentrations (MIC) are 32-64 microg mL . Isopimaric acid is also possible that an antagonistic interacti

Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca

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

Microgrewiapine A is a selective cytotoxic agent for colon cancer cells over normal colon cells and to exhibit nicotinic receptor antagonistic activity for both the hα3β4 and hα4β2 receptor subtypes.

Cyclo(Tyr-Pro) shows antibacterial activity towards several marine bacterial species, it also shows weak antagonistic activity against VEGFR2 -CD. Cyclo(Tyr-Pro) and cyclo(Pro-Val) are toxic to both suspension cells and seedlings of Pinus thunbergii, whic

Cyclo(Phe-Gly) shows weak antagonistic activity against VEGFR2 -CD, it also shows strong inhibitory activity against human cancer cells(KB,KBv200) with LD50 at 6.5 and 11.2 umol/L,respectively.

Kadsurenin C (compound 1), a neolignan isolated from the aerial parts of Piper kadsura, exhibits anti-inflammatory properties and significant PAF (Platelet Activating Factor) antagonistic activity, with an IC50 value of 5.1 μM [1].