Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.IC50 value:Target: in vitro: Schisanhenol exhibited strong inhibition toward UGT2B7, with the residual activity to be 7.9% of control activity [1]. The BAECs were cultured with ox-LDL (200 microg/ml) in the presence and absence of Sal (10 and 50 micromol L(- 1)) for 24 h. The cytotoxicity of ox-LDL was evaluated by LDH leakage, cell viability and morphological change. Cell apoptosis was estimated by DNA ladder, chromatin condensation, and flow cytometry assay. The intracellular ROS production was detected by using DCF, a ROS probe, with laser confocal microscopy and flow cytometry. Sal was shown to reduce LDH leakage and increase cell viability. Sal also attenuated ox-LDL-induced BAECs apoptosis as indicated in typical internucleosomal DNA degradation (DNA ladder), condensed chromatin, and the sub-G1 peak appearance in flow cytometry assay [2].in vivo: Sal significantly impeded production of MDA and loss of ATPase activity induced by reoxygenation following anoxia. Oral administration of Sal induced increase of cytosol glutathione-peroxidase of brain in mice under the condition of reoxygenation following anoxia [4].
H-Tyr(3-I)-OH is an effective tyrosine hydroxylase inhibitor.
Luteolin-7-rutinoside has both anti-arthritic and antifungal activities, can result in a combination therapy for the treatment of fungal arthritis due to C. albicans infection.
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
Schisantherin E is a natural compound isolated from the active fraction of the fruits of Schisandra sphenanthera Rehd. et Wils.
Angiotensin II is a Vasoconstrictor that plays an endocrine role in the regulation of blood pressure, fluid and electrolyte homeostasis.
Fisetin is a natural flavonol found in many fruits and vegetables with various benefits, such as antioxidant, anticancer, neuroprotection effects.
Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist.IC50 value:Target: Adrenergic receptor; H1 receptorFenspiride hydrochloride is a bronchodilator with anti-inflammatory properties. Fenspiride hydrochloride inhibits mucus secretion and reduces the release of tachykinins at a prejunctional level. Fenspiride hydrochloride also may be an antagonist at α adrenergic and H1 histamine receptors.
14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide that can be isolated from A. paniculata. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
Rapamycin (Sirolimus) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM.
Etimizol(Ethymisole; Antiffine; Ethylnorantifein) was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain). IC50 Value: Target: Etimizol has a catalytic effect on the respiratory center and belongs to the group of respiratory analeptics, however, it activates adrenokortikotropnuyu pituitary function, which leads to increased levels of glucocorticosteroids in the blood. There is also evidence that short etimizol improves memory and increases mental performance.in vitro:in vivo: The time interval between administration ofetimizol (3 mg/kg) and the onset of learning varied between 0.5 and 3 h in the several series. Etimizol did not facilitate the learning in rats whatever the time of administration and biological modality of reinforcement [1]. After administration of etimizol at doses of 10 or 1 mg/loop mean residence time of etimizol in the loop was 20.1 and 7.6 min, respectively, with mean standard deviation being 3.1 and 0.8, respectively [2]. Extracellular application of 5--10 mM/L etimizol exerted a specific effect on the giant neurons of the Coretus corneus isolated nervous system: action potential duration increased significantly, speed of development of its descending phase decreased, as well as the trace hyperpolarization amplitude [3].
Coenzyme Q9, a nine isoprenyl group-containing member of the ubiquinone family, is a normal constituent of human plasma.
Toxicarol isoflavone is an isoflavone extracted from Millettia brandisiana.
Dihydrodaidzein is one of the most prominent dietary phytoestrogens.
Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins.Target: Alpha-1A adrenergic receptorNicergoline acts by inhibiting the postsynaptic alpha(1)-adrenoceptors on vascular smooth muscle. This inhibits the vasoconstrictor effect of circulating and locally released catecholamines (epinephrine and norepinephrine), resulting in peripheral vasodilation. Nicergoline displaced [3H]-prazosin bound to rat forebrain membranes pretreated with chloroethylclonidine (pKi = 9.9 +/- 0.2) at concentrations 60-fold lower than in rat liver membranes (pKi = 8.1 +/- 0.2). Finally, of the nicergoline metabolites studied, lumilysergol acted as a modest alpha 1 antagonist (bromonicotinic acid was devoid of alpha 1 antagonist activity). In conclusion, nicergoline is a potent and selective alpha 1A-adrenoceptor subtype antagonist, an alpha 1-adrenoceptor subtype which is mainly represented in resistance arteries [1].
Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
Mecarbinate is an anti-hepatitis C virus (HCV) agent.
Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.
Glycylglycine is the simplest of all peptides and could function as a gamma-glutamyl acceptor.
Curcumol is a sesquiterpene originally isolated from curcuma rhizomes; shows anticancer activities both in vitro and in vivo.IC50 value:Target: Anticancer natural compoundin vitro: Curcumol exhibited time- and concentration-dependent anti-proliferative effects in SPC-A-1 human lung adenocarcinoma cells with cell cycle arrest in the G0/G1 phase while apoptosis-induction was also confirmed with flow cytometry and morphological analyses [1]. Curcumol-induced growth inhibition correlated with apoptosis induction as evidenced by Annexin V staining, and cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP) in HSC-T6. Suppression of the NF-κB translocation via inhibition of IκB-α phosphorylation by the curcumol led to the inhibition of expression of NF-κB-regulated gene, e.g. Bcl-xL and Bcl-2, in a PI3K-dependent manner, which is upstream of NF-κB activation [2]. Curcumol exhibits an inhibitory effect on receptor activator of nuclear factor kappaB ligand (RANKL)-induced osteoclast differentiation with both bone marrow-derived macrophages and RAW264.7 cells in a dose-dependent manner [3].in vivo: Anti-neoplastic effects of curcumol were also confirmed in tumor bearing mice. Curcumol (60 mg/kg daily) significantly reduced tumor size without causing notable toxicity [1].
Oxaceprol is an anti-inflammatory drug used in the treatment of osteoarthritis. Oxaceprol markedly inhibited inflammatory cell infiltration and bone damage in the adjuvant-injected paw. oxaceprol was effective at inhibiting periarticular soft tissue inflammation.[1] IV Injection: 50mg/kg.[2]
Maltohexaose is a natural saccharide, and can be produced from amylose, amylopectin and whole starch.
Lycorine (hydrochloride) is VE-cadherin inhibitor,and has IC50 of 1.2μM in Hey1B cell.IC50: 1.2μM (Hey1B cell)[2]In vitro:Lycorine (hydrochloride) executed an anti-melanoma vasculogenic effect by inhibiting VE-cadherin gene expression in C8161 cells and caused a decrease in cell surface exposure of VE-cadherin protein. Consistently, LH significantly suppressed VE-cadherin gene promoter activity. [1]Lycorine (hydrochloride) effectively inhibited mitotic proliferation of Hey1B cells (half maximal inhibitory concentration = 1.2 μM) with very low toxicity, resulting in cell cycle arrest at the G2/M transition through enhanced expression of the cell cycle inhibitor p21 and marked down-regulation of cyclin D3 expression. Moreover, LH suppressed both the formation of capillary-like tubes by Hey1B cells cultured in vitro.[2]In vivo: Lycorine effectively suppressed C8161 cell-dominant tumor formation and generation of tumor blood vessels in vivo with low toxicity.[1]Lycorine (hydrochloride) suppressed the formation of the ovarian cancer cell-dominant neovascularization in vivo when administered to Hey1B-xenotransplanted mice, suggest that LH selectively inhibits ovarian cancer cell proliferation and neovascularization and is a potential drug candidate for anti-ovarian cancer therapy.[2]
Cynaroside is a flavone, a flavonoid-like chemical compound. It is a 7-O-glucoside of luteolin.
pleuromutilin inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit of bacteria.
L-SelenoMethionine is a major natural food-form of selenium.Target：The median lethal dose (LD50) of L-SelenoMethionine in rats given an intraperitoneal injection was determined to 4.25 mg Se/kg body and thus is comparable to that of selenite or selenate. In mice, the LD50 of L-SelenoMethionine was 8.8 ± 1.37 mg Se/kg, and the minimal lethal dose, 4.0 mg Se/kg, after intravenous injection.
Moxifloxacin is a synthetic fluoroquinolone antibiotic agent.Target: AntibacterialMoxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3]. Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infectionToxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.
meso-Erythritol is a sugar alcohol derived from fermenting the glucose of cornstarch, resulting in fewer calories and a less sweeter taste than regular sugar.
5-Hydroxymethyl-2-furancarboxylic acid is the main metabolite of 5-hydroxymethyl-2-furfural (HMF) in the body and eliminated renally.
Wilforine is a sesquiterpene pyridine alkaloid; importantbioactive compound in T. wilfordii plants, and is effective intreating idiopathic pulmonary fibrosis.