Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
7,8-Dihydro-L-biopterin is an oxidation product of tetrahydrobiopterin.
Nanchangmycin, produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
3,4-Dihydroxybenzeneacetic acid is the main neuronal metabolite of dopamine.
Allopurinol riboside, a metabolite of allopurinol, shows potent activities against parasites.
3-Methyl-L-histidine is a biomarker for meat consumption, especially chicken. It is also a biomarker for the consumption of soy products.
Lasalocid is an antibacterial agent and a coccidiostat, used in the feed additives
Biotin sulfone is first isolated as a natural metabolite of biotin.
Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
Salvianolic acid C is a noncompetitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2), with Kis of 4.82 μM and 5.75 μM for CYP2C8 and CYP2J2, respectively.
Orotic acid (OA) is an intermediate in pyrimidine metabolism.IC50 Value: Target: Nucleoside antimetabolite/analogin vitro: OA increases cell proliferation and decreases apoptosis in serum-starved SK-Hep1 hepatocellular carcinoma cells, which may ascribe to the inhibition of AMP-activated protein kinase (AMPK) phosphorylation and thus activation of mammalian target of rapamycin complex 1 (mTORC1) [1].in vivo: male Fischer 344 rats (130-150 g) to two-thirds PH in the absence or in the presence of OA (a 300-mg tablet of OA methyl ester implanted intraperitoneally at the time of two-thirds PH). treatment with OA resulted in a near-100% inhibition of RNR induced by two-thirds PH in rat liver, as monitored by enzyme activity and protein level [2]. The increases of hepatic OA and betaine levels in OA feeding rats was also found when compared to the normal rats [3]. Feeding 1% OA with diet decreased the phosphorylation of AMPK and increased the maturation of SREBP-1 and the expression of SREBP-responsive genes in the rat liver. OA-induced lipid accumulation was also completely inhibited by rapamycin. Mouse hepatocytes and mice were resistant to OA-induced lipogenesis because of little if any response in AMPK and downstream effectors [4].
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity.
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.IC50 Value: 140 nM (α2δ subunit of calcium channel) [1]Target: Calcium Channelin vitro: Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release [2]. A large inhibition of calcium currents by gabapentin was observed in pyramidal neocortical cells (up to 34%). Significantly, the gabapentin-mediated inhibition of calcium currents saturated at particularly low concentrations (around 10 microM), at least in neocortical neurons (IC50 about 4 microM) [3].in vivo: Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-α, 316.0 ± 69.7 pg/mL vs 88.8 ± 24.4 pg/mL; IL-1β, 1,212.9 ± 104.5 vs 577.4 ± 97.1 pg/mL; IL-6, 254.0 ± 64.8 pg/mL vs 125.5 ± 44.1 pg/mL; IL-10, 532.1 ± 78.7 pg/mL vs 918.9 ± 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody [4].Toxicity: No new safety signals or adverse event trends relating to GEn exposure were identified [5].Clinical trial: N/A
Isosakuranetin is a flavanone flavonoid which can be found in the fruit of Citrus bergamia.
Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
Desmopressin(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin. IC50 Value:Target: Vasopressin ReceptorThe antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.
Cholestenone is the intermediate oxidation product of cholesterol.
L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer.
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.
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
Brassinolide is a predominant plant growth modulator that regulate plant cell elongation.
Isoastragaloside IV is a triterpene oligoglycoside isolated from Astragali Radix.
Squalene is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity.
24, 25-Dihydroxy VD3 is a compound which is closely related to 1,25-dihydroxyvitamin D3, the active form of vitamin D3, but like vitamin D3 itself and 25-hydroxyvitamin D3 is inactive as a hormone both in vitro and in vivo.
2''-O-Rhamnosylicariside II is a flavonoid glycoside compound and might be beneficial for improving postmenopausal osteoporosis.
L-cycloserine irreversibly inhibit GABA pyridoxal 5′-phosphate-dependent aminitransferase in E. coli, as well in the brains of various animals in a time-dependent manner, results in increased levels of gamma-aminobutyric acid (GABA), which is an inhibitory neurotransmitter in vivo.
Acetyl Perisesaccharide C is an oligosaccharide, which is isolated from the root barks of Periploca sepium.