Hot Natural Products & Bioactive Compounds

PI 3-Kinase inhibitor (IC₅₀ values are 0.098, 0.183, 0.227 and 1.967 <span class='symbol'>&mu;</span>M for p110<span class='symbol'>&beta;</span>, p110<span class='symbol'>&alpha;</span>, p110<span class='symbol'>&delta;</span> and p110<span class='symbol'>&gamma;</span> respectively) that displays higher potency than LY 294002. Can be immobilized onto a solid phase.

1. Withaferin A(WFA) has anti-inflammatory, anti-oxidant, immune modulatory, cardioactive, antithrombotic and central nervous system effects.
2. Withaferin A is a potent breast cancer anti-metastatic agent and the anti-metastatic activity of WFA is, at least in part, mediated through its effects on vimentin and vimentin ser56 phosphorylation.
3. Withaferin A induces p53-dependent apoptosis by repression of HPV oncogenes and upregulation of tumor suppressor proteins in human cervical cancer cells, it can be exploited as a potent therapeutic agent for the treatment and prevention of cervical cancer without deleterious effects.
4. Withaferin A could act as an anti-fibrotic compound against fibroproliferative diseases, including, but not limited to, cardiac interstitial fibrosis.
5. Withaferin A sensitizes TRAIL-induced apoptosis through reactive oxygen species-mediated up-regulation of death receptor 5 and down-regulation of c-FLIP.
6. Withaferin A is a proteasomal inhibitor promotes healing after injury and exerts anabolic effect on osteoporotic bone.

Competitive, non-selective nicotinic acetylcholine receptor antagonist; causes skeletal muscle relaxation. Also a 5-HT₃ and GABA_A receptor antagonist.

1. 17Alpha-estradiol and 17beta-estradiol treatments are effective in lowering cerebral amyloid-beta levels in AbetaPPSWE transgenic mice, they may help to develop safe and effective therapeutics to treat Alzheimer disease.
2. 17Alpha-estradiol arrests cell cycle progression at G2/M and induces apoptotic cell death in human acute leukemia Jurkat T cells.
3. 17Alpha-estradiol is neuroprotective in male and female rats in a model of early brain injury.
4. 17Alpha-estradiol is a potent estrogen and carcinogen during development.
5. 17Alpha-estradiol induces aromatase activity in isolated human hair follicles, it may be used for topical treatment of androgenetic alopecia (AGA) in women.

Formyl peptide receptor (FPR) agonist that potently activates neutrophils in vitro (EC50 values are 42 and 630 nM for neutrophil chemotaxis and Ca2+ mobilization respectively).

Human ether-a-go-go (hERG) KV11.1 potassium channel activator. Displays no major effect on INa, ICa/L, IK1 and IKs currents. Causes resting membrane hyperpolarization and decreases action potential duration in rat myocytes in vitro.

Dual fatty acid amide hydrolase (FAAH) inhibitor/TRPV1 antagonist (IC₅₀ values are 5.6 <span class='symbol'>&mu;</span>M and 37 - 40 nM for FAAH and TRPV1 respectively). Inactive at cPLA₂, CB₁ or 5-HT receptors. Displays strong analgesic activity against both acute and chronic peripheral pain.

Non-competitive nicotinic acetylcholine receptor antagonist. Displays antidepressant-like effects in mice.