Piceatannol 3'-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide (NO) synthase through inhibition of arginase activity with IC50s of 11.22 µM and 11.06 µM against arginase I and arginase II, respectively.
Isovaleramide is an active principle on central nervous system from Valeriana pavonii, as an anticonvulsant.Target：in vitro: Isovaleramide (300 μM) exhibits a 42% of inhibition of the binding of 3H-FNZ to its sites.in vivo: Isovaleramide at 100 mg/Kg, p.o, evidences a 90% index protection against the maximal electroshock seizure in mice (MES).
3-Hydroxyhippuric acid is an acyl glycine. Acyl glycines are normally minor metabolites of fatty acids.
Geniposide is an iridoid glucoside extracted from Gardenia jasminoides Ellis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
Echinacoside is a natural polyphenolic compound, has various kinds of pharmacological activities, such as antioxidative, anti-inflammatory, neuroprotective, hepatoprotective, nitric oxide radical-scavenging and vasodilative ones.IC50 value:Target:in vitro: Echinacoside(ECH) dose dependently inhibited HEWL aggregation, and this inhibition occurred in different fiber-forming stages. ECH could also scavenge the DPPH and OH free radicals in a concentration-dependent manner. ECH could increase viability of rat pheochromocytoma PC12 cells injured by Aβ and suppress the increase in intracellular reactive oxygen species (ROS) triggered by Aβ [1]. Transient treatment with echinacoside inhibits cytochrome c release and caspase-3 activation caused by ensuing rotenone exposure via activating Trk-extracellular signal-regulated kinase (ERK) pathway in neuronal cells [2]. ECH caused a significant increase in cell proliferation, ALP activity, COL I contents, OCN levels and an enhancement of mineralization in osteoblasts at the concentration range from 0.01 to 10nmol·L(-1) (p<0.05), suggesting that ECH has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis [4]. in vivo: In OVX rats, the increases of body weight, serum hydroxyproline (HOP) levels, and the decreases of uterus wet weight and BMD were significantly reversed by ECH treatment [3]. Echinacoside (60 mg/kg) was given intraperitoneally to mice at 1 h prior to GalN/LPS exposure. Pretreatment with echinacoside remarkably improved the survival rate of GalN/LPS-treated mice and attenuated acute hepatotoxicity, as demonstrated by decreased ALT levels and improved histological signs. Echinacoside shows both anti-apoptotic and anti-inflammatory properties, characterized by a substantial inhibition of hepatocyte apoptosis and a significant reduction in the inflammatory markers, including myeloperoxidase, extracellular nucleosomes, high-mobility group box 1, and inflammatory cytokines in the plasma of mice, which may be important mechanisms related to its protective effect [5].
Alfuzosin hydrochloride is an α1 adrenergic receptor antagonist used to treat benign prostatic hyperplasia (BPH).Target: α1 adrenergic receptorAlfuzosin, a new quinazoline derivative, acts as a selective and competitive antagonist of alpha 1-adrenoceptor-mediated contraction of prostatic, prostatic capsule, bladder base and proximal urethral smooth muscle, thereby reducing the tone of these structures. Consequently, urethral pressure and resistance, bladder outlet resistance, bladder instability and symptoms associated with benign prostatic hyperplasia are reduced. A limited range of clinical studies have shown oral alfuzosin to be more effective than placebo (in studies of < or = 6 months duration), to have sustained effects on long term administration (< or = 30 months), and to be comparable with the alpha 1-adrenoceptor antagonist prazosin, in the symptomatic treatment of benign prostatic hyperplasia.Oral alfuzosin 7.5 to 10 mg/day in divided doses appears to be a promising first-line agent for symptomatic treatment of noncomplicated mild to moderate benign prostatic hyperplasia in patients with a high dynamic component to their obstruction. In addition, alfuzosin offers an alternative to prostatectomy (the current 'gold standard') in patients who require surgery but are unfit for this treatment, and in patients requiring symptomatic relief while awaiting surgery.
Perisesaccharide C is an oligosaccharide isolated from the root barks of Periploca sepium.
Hydrocortisone is a steroid hormone or glucocorticoid secreted by the adrenal cortex.
Terephthalic acid is one isomer of the three phthalic, a precursor to the polyester PET, used to make clothing and plastic bottles.
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
Anemarsaponin E is extracted from Anemarrhena asphodeloides Bunge and has anti-inflammatory activity.
NADP is nicotinamide adenine dinucleotide phosphate, acting as a key cofactor for electron transfer in the metabolism of all organisms, being alternately oxidized (NADP+) and reduced (NADPH).
Decanoic acid belongs to the class of organic compounds known as medium-chain fatty acids.
11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
23-hydroxybetulinic acid is one of the bioactive components responsible for its anticancer activity.In vitro: 23-hydroxybetulinic acid also shows different proliferation inhibitory activity against B16, HeLa, and HUVEC, with the IC50 value of 78.5, 80, and 94.8 uM, respectively. 23-hydroxybetulinic acid can promote cell cycle arrest at S phase and induce apoptosis via intrinsic pathway. 23-hydroxybetulinic acid disrupts mitochondrial membrane potential significantly (p<0.01) and selectively downregulates the levels of Bcl-2, survivin and upregulates Bax, cytochrome C, cleaved caspase-9 23-hydroxybetulinic acid can induce apoptosis in K562 cells. [1] 23-hydroxybetulinic acid enhances sensitivity of doxorubicin (DOX, ADR) on MCF-7/ADR cell lines, indicating its potential to be developed as a novel MDR modulator.[2] 23-HBA significantly improve the sensitivity of the tumor to doxorubicin. [3]
All-trans-retinal is a one of the major vitamin A metabolites in the retina. In physiological conditions, all-trans-RAL is regenerated to the visual chromophore, 11-cis-retinal.
Epimedin A1 is a flavonoid extracted from Herba Epimedii which is one of commonly used Chinese medicines.
Poliumoside is a natural compound which exhibit significant inhibition of advanced glycation end product formation with IC50 value of 4.6-25.7 μM.IC50 value: Target: Poliumoside exhibited greater inhibitory effects on rat lens aldose reductase with IC50 values of 0.85 μM, than those of the positive controls, 3,3-tetramethyleneglutaric acid (IC50=4.03 μM) and quercetin (IC50=7.2 μM).
Gambogic acid is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic acid inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
Pemetrexed disodium is a novel antifolate that inhibits the folatedependent enzymes thymidylate synthase, dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase with Kis of 1.3, 7.2, and 65 nM, respectively.
Rutin hydrate is a flavonol glycoside, able to cross the blood-brain barrier, and acts by inhibiting JNK and ERK1/2 activation and activating mTOR signalling.
1-Methyl-L-histidine is an objective indicator of meat ingestion and exogenous 3-methylhistidine (3MH) intake.
3'-Methoxypuerarin (3'-MOP) is an isoflavone extracted from radix puerariae that shows neuron protection activity.
Mesaconitine is the main active component of genus aconitum plants.IC50 value:Target: in vitro: In HUVECs, 30 microM mesaconitine increased the [Ca(2+)](i) level in the presence of extracellular CaCl(2) and NaCl, and the response was inhibited by KBR7943. Mesaconitine increased intracellular Na(+) concentration level in HUVECs. The [Ca(2+)](i) response by mesaconitine was inhibited by 100 microM D-tubocurarine [1]. Mesaconitine at 30 microM inhibited 3 microM phenylephrine-induced contraction in the endothelium-intact, but not endothelium-denuded, aortic rings [2]. MA promoted the alpha-MT-induced decrease in NE levels in hippocampus, medulla oblongata plus pons and spinal cord [3].
Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression.
5-Methylfurfural is a naturally occurring substance, found in cigarette smoke condensate, licorice essential oil, stored dehydrated orange powder, baked potato flour, volatile compounds of roast beef, aroma concentrate of sponge cake. bread and in coffee, tea and cocoa[1]. A flavoring agent.
Panaxadiol is a novel antitumor agent extracted from the Chinese medical herb Panax ginseng.
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
Hypericin is a photosensitive antiviral with anticancer and antidepressant agent derived from Hypericum perforatum. It can inhibit tyrosine kinases with IC50 of 7.5 μM. IC50: 7.5 uMIn vitro:The photosensitive of hypericin can induce both apoptosis and necrosis in a concentration and light dose-dependent fashion. PDT with hypericin results in the activation of multiple pathways that can either promote or counteract the cell death program. It can effect cytotoxic to tumor cells by visible light.
Ursolic acid, a naturally occurring triterpenoid, induces the apoptosis of human cancer cells through multiple signaling pathways. In vitro: Ursolic acid is important in the induction of apoptosis via AKT/NF-κB signaling suppression in T24 human bladder cancer cells and this occurs in a dose-dependent manner. Thus, Akt and NF-κB are potential targets for bladder cancer therapy and ursolic acid may serve as a naturally-occurring candidate drug for the prevention and treatment of bladder cancer.[1]Ursolic acid induce apoptosis via inhibition of NF-κB induced BCl-2 mediated anti-apoptotic pathway leading to activation of p53 induced and caspase-3 mediated pro-apoptotic pathways.[2]In vivo: UA significantly suppressed prostate tumor growth in nude mice without any significant decrease in body weight. The systemic bioavailability of UA in serum samples obtained from nude mice. UA was detected in all serum samples 24 h after last injection. Systemic bioavailability of UA was in nanogram range and metabolites of UA were not detected in the samples. These results indicate that UA is well absorbed in the mouse peritoneum and supports the role of UA as a potent compound for chemoprevention and therapy of prostate cancer. [3]