6-methylflavone is an activator of α1β2γ2L and α1β2 GABAA receptors.
Icaritin(Anhydroicaritin) is a component of Epimedium flavonoid isolated from Herba Epimedii; enhances osteoblastic differentiation of mesenchymal stem cells (MSCs) while it inhibits adipogenic differentiation of MSCs by inhibiting PPAR-g pathway.IC50 value:Target: in vitro: Icaritin was unable to promote proliferation, migration and tube like structure formation by human umbilical vein endothelial cells (HUVECs) in vitro [1]. Icaritin potently inhibited proliferation of K562 cells (IC50 was 8 μM) and primary CML cells (IC50 was 13.4 μM for CML-CP and 18 μM for CML-BC), induced CML cells apoptosis and promoted the erythroid differentiation of K562 cells with time-dependent manner. Furthermore, Icaritin was able to suppress the growth of primary CD34+ leukemia cells (CML) and Imatinib-resistant cells, and to induce apoptosis [2]. icaritin strongly inhibited the growth of breast cancer MDA-MB-453 and MCF7 cells. At concentrations of 2-3 μM, icaritin induced cell cycle arrest at the G(2)/M phase accompanied by a down-regulation of the expression levels of the G(2)/M regulatory proteins such as cyclinB, cdc2 and cdc25C. Icaritin at concentrations of 4-5 μM, however, induced apoptotic cell death characterized by the accumulation of the annexin V- and propidium iodide-positive cells, cleavage of poly ADP-ribose polymerase (PARP) and down-regulation of the Bcl-2 expression [3].in vivo: In mouse leukemia model, Icaritin could prolong lifespan of NOD-SCID nude mice inoculated with K562 cells as effective as Imatinib without suppression of bone marrow. Icaritin could up-regulate phospho-JNK or phospho-C-Jun and down-regulate phospho-ERK, phospho-P-38, Jak-2, phospho-Stat3 and phospho-Akt expression with dose- or time-dependent manner [2].
L-Carnosine is a dipeptide of the amino acids beta-alanine and histidine and has the potential to suppress many of the biochemical changes that accompany aging.
Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay.
Octopamine Hydrochloride is an endogenous biogenic amine that is closely related to norepinephrine, and has effects on the adrenergic and dopaminergic systems.Target: Dopamine Receptor; Adrenergic ReceptorOctopamine is present in relatively high concentrations in neuronal as well as in non-neuronal tissues of most invertebrate species studied, and modulates almost every physiological process. Octopamine acts as neurohormone including desensitization of sensory inputs, influence on learning and memory, or regulation of the mood of the animal in the central nervous system. Octopamine is the only neuroactive non-peptide transmitter whose physiological role is restricted to invertebrates, and all octopamine receptors belong to the family of G-protein coupled receptors [1].Octopamine (10 μM) injected into the mushroom body (MB) calyces or the antennal lobe but not the lateral protocerebral lobe produces a lasting, pairing-specific enhancement of extension of the proboscis. Octopamine (10 μM) injected into the MB calyces results in an additional pairing-specific effect, because it does not lead to an acquisition but a consolidation after conditioning [2]. Octopamine treatment significantly elevates levels of octopamine in the brain and caused a significant dose-dependent increase in the number of new foragers. Octopamine treatment is effective only when given to bees old enough to forage, i.e., older than 4 days of age. Octopamine influences division of labor in honey bee colonies [3].
Ikarisoside F is a flavonol glycoside from Vancouveria hexandra; could bind to AdoHcy hydrolase.
Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced NF-κB activation and ERK phosphorylation in BMMs. [1] EA inhibit IL-1β-induced inflammation in chondrocytes. [2]In vivo: Echinocystic acid reduces reserpine-induced pain/depression dyad in mice. [3]
Ureidopropionic acid is an intermediate in the metabolism of uracil.
Foresaconitine(Vilmorrianine C) is a norditerpenoid alkaloid isolated from the processed tubers of Aconitum carmichaeli.
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
Aurothioglucose (Gold thioglucose) is a well known active-site inhibitor of TrxR1, inhibited TrxR1 activity in HeLa cell cytosol but had no effect on the viability of the cells.IC50 value:Target: TrxR1in vitro: Trx1 redox state and ROS generation were measured in cells exposed to the TrxR1 inhibitors aurothioglucose (ATG) and monomethylarsonous acid (MMA(III)) and in cells depleted of TrxR1 activity by siRNA knock down [1].in vivo: Adult mice received a single intratracheal dose of 0.375 μg/g lipopolysaccharide (LPS) 12 h before a single intraperitoneal injection of 25 mg/kg ATG. Control mice received intratracheal and/or intraperitoneal saline. ATG treatment significantly attenuated lung injury, increased lung GCLM expression and GSH levels, and decreased mortality. GSH depletion completely prevented the protective effects of ATG in LPS/hyperoxia-exposed mice [2].
Methyl protodioscin(NSC-698790) is a furostanol bisglycoside with antitumor properties; shows to reduce proliferation, cause cell cycle arrest.IC50 value:Target: in vitro: MPD showed growth inhibitory effects in A549 cells in a dose- and time-dependent manner. The significant G2/M cell cycle arrest and apoptotic effect were also seen in A549 cells treated with MPD. MPD-induced apoptosis was accompanied by a significant reduction of mitochondrial membrane potential, release of mitochondrial cytochrome c to cytosol, activation of caspase-3, downregulation of Bcl-2, p-Bad, and upregulation of Bax [1]. In THP-1 macrophages, MPD increases levels of ABCA1 mRNA and protein in dose- and time-dependent manners, and apoA-1-mediated cholesterol efflux. MPD also decreases the gene expressions of HMGCR, FAS and ACC for cholesterol and fatty acid synthesis [2].
Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
Herniarin is a natural coumarin occurs in some flowering plants, with antitumor effect.
Oxytetracycline is a tetracycline analog isolated from the actinomycete streptomyces rimosus and used in a wide variety of clinical conditions.Target: AntibacterialOxytetracycline was the second of the broad-spectrum tetracycline group of antibiotics to be discovered. Oxytetracycline works by interfering with the ability of bacteria to produce essential proteins. Without these proteins, the bacteria cannot grow, multiply and increase in numbers. Oxytetracycline therefore stops the spread of the infection and the remaining bacteria are killed by the immune system or eventually die.Oxytetracycline is a broad-spectrum antibiotic, active against a wide variety of bacteria. However, some strains of bacteria have developed resistance to this antibiotic, which has reduced its effectiveness for treating some types of infections [1, 2].
(S)-3,4-Dihydroxybutyric acid is a normal human urinary metabolite that is excreted in increased concentration in patients with succinic semialdehyde dehydrogenase (SSADH) deficiency.
2-Hydroxy-4-methoxybenzoic is a derivative of methoxybenzoic. 2-Hydroxy-4-methoxybenzoic is a potential biomarker.
Cotinine is an alkaloid found in tobacco and is also the predominant metabolite of nicotine, used as a biomarker for exposure to tobacco smoke.
2'-Deoxycytidine, a deoxyribonucleoside, could inhibit biological effects of Bromodeoxyuridine (Brdu).
Tylosin (Fradizine; Tylocine; Tylosin A) is a broad spectrum antibiotic against Gram-positive organisms and a limited range of Gram-negative organisms.
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities[1].
Phillygenin is an active ingredient from Forsythia with many medicinal properties, such as antioxidant, reducing blood lipid, inhibition of low density lipoprotein oxidation.In vitro : 1) Phillygenin shows a greater inhibition on mouse B16 melanoma cells potential than vincristine.2) phillygenin had notable scavenging activity against DPPH, ABTS radicals, as well as potent reducing power in FRAP assay.In vivo: The reference for rat is 5.6 mg/m l ( i.v).
Formononetin (Formononetol; Flavosil) is a bioactive component extracted from the red clover; inhibits the proliferation of DU-145/PC-3 cells in a dose-dependent manner.IC50 value:Target: anti-cancer in vitro: formononetin inhibited the proliferation of DU-145 cells in a dose-dependent manner. DU-145 cells treated with different concentrations of formononetin displayed obvious morphological changes of apoptosis under fluorescence microscopy. In addition, formononetin increased the proportion of early apoptotic DU-145 cells, down-regulated the protein levels of Bcl-2 and up-regulated those of RASD1 and Bax [1]. Formononetin significantly inhibited the cell growth of PC-3 in a dose-dependent manner, but no such effect was observed in RWPE1 cells. Formononetin treatment contributed to the reduced Bcl-2 protein level and the elevated Bax expression in PC-3 cells, thereby resulting in the increasing Bax/Bcl-2 ratios. Furthermore, the phosphorylated level of p38 in PC-3 cells was activated through the FN treatment, whereas the endogenous Akt phosphorylation was blocked [2]. Compared with the control, formononetin inhibited the proliferation of MCF-7 cells and effectively induced cell cycle arrest. The levels of p-IGF-1?R, p-Akt, cyclin D1 protein expression, and cyclin D1 mRNA expression were also downregulated [3].in vivo: formononetin also prevented the tumor growth of human breast cancer cells in nude mouse xenografts [3].
Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, reduces several effects of tetrahydrocannabinol (THC).
8-Dehydrocholesterol elevated concentration is one of the diagnostic biochemical hallmarks of classical Smith-Lemli-Opitz syndrome (SLOS).
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.IC50 value:Target:Peimine (0-25 mg/L) significantly inhibited tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-1β, and increased IL-10 production. Furthermore, peimine significantly inhibited the phosphorylation of p38, ERK and c-jun N-terminal kinase (JNK) as well as decreased p65 and IκB.
Siamenoside I is one of the mogrosides that has several kinds of bioactivities.