Rosmarinic acid racemate is the racemate of Rosmarinic acid. Rosmarinic acid inhibits MAO-A, MAO-B and COMT enzymes with IC50s of 50.1, 184.6 and 26.7 μM, respectively.
L-5,6,7,8-Tetrahydrofolic acid, a folic acid derivative, which is a coenzyme in many reactions, especially in the metabolism of amino acids and nucleic acids.
Urocanic acid, produced in the upper layers of mammalian skin, is a major absorber of ultraviolet radiation (UVR).
Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.IC50 Value:Target:In vitro: The effects of Resibufogenin on the outward delayed rectifier potassium current (IK) and outward transient potassium current (IA) in rat hippocampal neurons was investigated, and it inhibited both IK and IA, at 1 μM concentration RBG could alter some channel kinetics and gating properties of IK, such as steady-state activation and inactivation curves, open probability and time constants [1].In vivo: Resibufogenin prevented evidence of oxidative stress in "preeclamptic" rats [2].
Bambuterol is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.IC50 value:Target: beta-adrenoceptor agonistBambuterol is contraindicated in pregnancy and in people with seriously impaired liver function. It can be used by people with renal impairment, but dose adjustments are necessary. The adverse effect profile of bambuterol is similar to that of salbutamol, and may include fatigue, nausea, palpitations, headache, dizziness and tremor.
5-Methylcytidine is a pyrimidine nucleoside detected in multiple biofluids.
Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1); an antioxidant dietary supplement.IC50 value:Target: Benfotiamine, the lipid-soluble thiamine derivative used as a treatment for diabetic neuropathy, can inhibit three major pathways(the hexosamine pathway, the advanced glycation end product (AGE) formation pathway and the diacylglycerol (DAG)?protein kinase C (PKC) pathway）of hyperglycemic damage and prevent experimental diabetic retinopathy. Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1) for treating sciatica and other painful nerve conditions. More effective at increasing thiamin levels in blood and tissues than water-soluble salts like the previous vitamin B1.
Cholestenone is the intermediate oxidation product of cholesterol.
Glycoursodeoxycholic acid, a acyl glycine and a bile acid-glycine conjugate, is a metabolite of ursodeoxycholic acid.In Vitro: The antioxidant compound glycoursodeoxycholic acid (GUDCA) fully abrogates UCB-induced cytochrome c oxidase inhibition and significantly prevents oxidative stress, metabolic alterations, and cell demise[1].GUDCA has shown therapeutic efficacy in neurodegenerative models and diseases. Increased cytosolic SOD1 inclusions were observed in 4 DIV NSC-34/hSOD1(G93A) cells together with decreased mitochondria viability, caspase-9 activation, and apoptosis[2]. Glycoursodeoxycholic acid shows preventive and restorative effects against unconjugated bilirubin -induced blood-brain barrier disruption and damage to human brain microvascular endothelial cells[3].
Thymine is one of the four nucleobases in the nucleic acid of DNA and can be a target for actions of 5-fluorouracil (5-FU) in cancer treatment, with a Km of 2.3 μM.
(R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.
Acetyl-11-Keto-β-Boswellic Acid (AKBA) is an active triterpenoid compound from the extract of Boswellia serrate; a novel Nrf2 activator.IC50 value:Target: Nrf2 activatorin vitro: AKBA significantly reduced infarct volumes and apoptotic cells, and also increased neurologic scores by elevating the Nrf2 and HO-1 expression in brain tissues in middle cerebral artery occlusion (MCAO) rats at 48 hours post reperfusion. In primary cultured neurons, AKBA increased the Nrf2 and HO-1 expression, which provided protection against OGD-induced oxidative insult. Additionally, AKBA treatment increased Nrf2 binding activity to antioxidant-response elements (ARE) [1]. AKBA significantly inhibited human colon adenocarcinoma growth, showing arrest of the cell cycle in G1-phase and induction of apoptosis[3]. AKBA triggered significant lipolysis in 3T3-L1 adipocytes as shown by reduced neutral lipids in cytosol and increased free fatty acids in culture medium. Increased lipolysis by AKBA was accompanied by up-regulation of lipolytic enzymes, adipocyte triglyceride lipase (ATGL) and hormone sensitive lipase (HSL), and a decreased expression of lipid droplet stability regulator perilipin. In addition, AKBA treatment reduced phenotypic markers of mature adipocyte aP2, adiponectin and glut-4 in mature adipocytes [5].in vivo: AKBA significantly prevented the formation of intestinal adenomatous polyps without toxicity to mice. AKBA's activity both in the prevention of small intestinal and colonic polyps was more potently than aspirin. Histopathologic examination revealed that AKBA's effect, that is the reduction of polyp size and degree of dysplasia, was more prominent in larger sized polyps, especially those originating in colon [2]. AKBA administration in mice effectively delayed the growth of HT-29 xenografts without signs of toxicity. The activity of AKBA was more potent than that of aspirin [3]. AKBA exhibited anti-cancer activity in vitro and in vivo. With oral application in mice, AKBA significantly inhibited SGC-7901 and MKN-45 xenografts without toxicity [4].
Cimiside B, a glycoside alkaloid, isolated from the rhizome of Cimicifuga dahurica.
4-Hydroxycyclohexanecarboxylic acid belongs to the class of organic compounds known as cyclohexanols.
1-Methyluric acid acts on the urinary bladder mucosa and increases the blood glucose, insulin, triglyceride, and cholesterol levels.
3-Methylbutanoic acid is a natural fatty acid and known to effect on neonatal death and possible Jamaican vomiting sickness in human.
Synephrine Hcl(Oxedrine) is an alkaloid; synephrine produces most of its biological effects by acting as an agonist at adrenergic receptors.IC50 value:Target: adrenergic receptor agonistThere is some evidence that synephrine also has weak activity at 5-HT receptors, and that it interacts with TAAR1 (trace adrenergic amine receptors). d-synephrine inhibited the uptake of [3H]-norepinephrine with an IC50 = 5.8 μM; l-synephrine was less potent (IC50 = 13.5 μM). d-Synephrine also competitively inhibited the binding of nisoxetine[m] to rat brain cortical slices, with a Ki = 4.5 μM; l-synephrine was less potent (Ki = 8.2 μM). In experiments on the release of [3H]-norepinephrine from rat brain cortical slices, however, the l-isomer of synephrine was a more potent enhancer of the release (EC50 = 8.2 μM) than the d-isomer (EC50 = 12.3 μM). This enhanced release by l-synephrine was blocked by nisoxetine.
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.
L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer.
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.
Resveratrol (SRT 501), a natural polyphenol that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. It has a wide spectrum of targets including mTOR, JAK, β-amyloid.
Raspberry ketone is a major aromatic compound of red raspberry, widely used as a fragrance in cosmetics and as a flavoring agent in foodstuff; also shows PPAR-α agonistic activity.
2-Phenylethanamine is believed to function as a neuromodulator or neurotransmitter.
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].
5,15-Diacetyl-3-benzoyllathyrol is one of the lathyrane diterpenoids, that has anti-cancer activity.
1) Natural acacetin was a 4.0-fold and 5.5-fold more potent inhibitor of BACE-1 than oleanolic acid and maslinic acid, respectively.[1]2) Acacetin significantly suppressed the photoreceptor collapse. [1]3) Acacetin significantly reduces the Aβ levels by interfering with human APP proteolytic processing and BACE-1 expression. [1]4) Acacetin inhibited the generation of the APP-CTF by affecting APP cleavage. [1]5) Acacetin prolongs lifespan of significantly in the dose dependent manner. Acacetin(25 uM) had the greatest effect on longevity, extending mean lifespan significantly by 27.31% at 25 uM concentration