Docetaxel is an antineoplastic drug by inhibiting microtubule depolymerization, and attenuating of the effects of bcl-2 and bcl-xL gene expression.
Epothilone A is a competitive inhibitor of the binding of [3H] paclitaxel to tubulin polymers, with a Ki of 0.6-1.4 μM.
Nicotinuric acid is an acyl glycine. Nicotinuric acid is a metabolite of nicotinic acid.
Dimenhydrinate is an anti-emetic and anti-histamine commonly available over-the-counter as a motion sickness remedy.
Caffeic acid phenethyl ester is a NF-κB inhibitor.
PCL 016 is a topical antiviral agent, which inhibits adenovirus replication in rabbit.
Emodin is a broad-spectrum anticancer agent. Emodin inhibits casein kinase II (CKII) activity with IC50 of 2 μM.
Epimedin B, a component extracted from Epimedii Folium, is reported to have antiosteoporotic activity.IC50 value:Target:In vitro:In vivo: Prednisolone-induced osteoporosis model using zebrafish was used to evaluate the antiosteoporotic activity of micro amount epimedin B. The result showed that 1 μmol·L- 1epimedin B groups were significantly increased when compared with model group; Epimedin B can prevent zebrafish osteoporosis induced by prednisolone [1].
Cholecalciferol(Vitamin D3) is a naturally occuring form of vitamin D; Reported that upon metabolic activation, Cholecalciferol induces cell differentiation and prevents proliferation of cancer cells. IC50 value:Target: Vitamin D acts through a receptor that is a member of the ligand-dependent transcription factor superfamily. Modulates the proliferation and differentiation of both normal and cancer cells. Has antiproliferative and antimetastatic effects on breast, colon, and prostate cancer cells. Activated vitamin D receptors in intestine and bone maintain calcium absorbance and homeostasis.
Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
Eicosapentaenoic acid (EPA) is an omega-3 fatty acid.
Anethole is a type of aromatic compound that occurs widely in nature, widely used as a flavoring substance.
Elaidic acid is the major trans fat found in hydrogenated vegetable oils and can be used as a pharmaceutical solvent.
O-Acetylserine (O-Acetyl-L-serine) is an intermediate in the biosynthesis of the amino acid cysteine in bacteria and plants.
Dibucaine Hydrochloride is a local anesthetic of the amide type now generally used for surface anesthesia.Target: Sodium ChannelDibucaine is an amide local anesthetic. Dibucaine reduced the degradation of BSA-gold complex in the reservosomes, which was not caused either by an inhibition of the whole proteolytic activity of the parasite or by a reduction on the expression levels of cruzipain [1].Dibucaine, a quaternary ammonium compound, inhibited SChE to a minimum within 2 min in a reversible manner. The inhibition was very potent. It had an IC(50) of 5.3 microM with BuTch or 3.8 microM with AcTch. The inhibition was competitive with respect to BuTch with a K(i) of 1.3 microM and a linear-mixed type (competitive/noncompetitive) with respect to AcTch with inhibition constants, K(i) and K(I) of 0.66 and 2.5 microM, respectively. Dibucaine possesses a butoxy side chain that is similar to the butryl group of BuTch and longer by an ethylene group from AcTch [2].
Daunorubicin is a topoisomerase II inhibitor.
Gynostemma Extract is a natural product.
Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.
N8-Acetylspermidine dihydrochloride is a polyamine.
Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
Octanoic acid is an oily liquid with a slightly unpleasant rancid taste and used commercially in the production of esters used in perfumery and also in the manufacture of dyes.
Epicatechin gallate inhibits cyclooxygenase-1 (COX-1) with an IC50 of 7.5 μM.
(+)-α-Tocopherol is a vitamin E derivative. vitamin E is a fat-soluble antioxidant.
Bruceantin(NSC165563) is first isolated from Brucea antidysenterica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.IC50 value:Target: anticancerCell differentiation was induced and c-MYC was down-regulated, suggesting a mechanistic correlation between c-MYC down-regulation and induction of cell differentiation or cell death. Treatment of HL-60 and RPMI 8226 cell lines induced apoptosis, and this involved the caspase and mitochondrial pathways. Moreover, an in vivo study using RPMI 8226 human-SCID xenografts demonstrated that bruceantin induced regression in early as well as advanced tumors, and these significant antitumor responses were facilitated in the absence of overt toxicity.
Argatroban is a direct, selective thrombin inhibitor.Target: ThrombinArgatroban may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of argatroban is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries [1]. Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban [2].
Epimedin A is a natural compound extracted from Herba Epimedii.
5-Aminovaleric acid is believed to act as a methylene homologue of gamma-aminobutyric acid (GABA) and functions as a weak GABA agonist.
3-Methyl-2-oxovaleric acid is a neurotoxin, an acidogen, and a metabotoxin, and also an abnormal metabolite that arises from the incomplete breakdown of branched-chain amino acids.
Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.IC50 value:Target:In vitro: Salvianolic acid B (SA-B) 1 and 10 micromol/L decrease the cell active TGF-beta1 secretion by 63.3 % and 15.6 % of the control, down-regulat pro-collgen alpha1(I) mRNA expression to 77.0% and 51.8% respectively (P<0.05). SA-B 1 and 10 micromol/L also inhibit MAPK activity by 1 to 2 fold respectively [3].In vivo: Salvianolic acid B (SalB) (5 mg · kg-1 · h-1) significantly attenuates LPS-induced pulmonary microcirculatory disturbance, including the increase in leukocyte adhesion and albumin leakage. In addition, LPS increases pulmonary tissue wet-to-dry weight ratio and tumor necrosis factor [alpha] and interleukin 8 levels in plasma and bronchoalveolar lavage fluid enhances the expression of E-selectin, intercellular adhesion molecule 1, myeloperoxidase, MMP-2, and MMP-9, whereas it decreases the expression of AQP-1 and AQP-5 in pulmonary tissue, all of which are attenuated by SalB pretreatment[1]. SalB administration (10 mg/kg) significantly ameliorate the Aβ25-35 peptide-induced memory impairment in the passive avoidance task (P<0.05). SalB treatment also reduced the number of activated microglia and astrocytes that are observed during the inflammatory reaction after the administration of the Aβ25-35 peptide. Moreover, SalB markedly reduce inducible nitric oxide synthase and cyclooxygenase-2 expression levels and thiobarbituric acid reactive substances, which are increased by the administration of the Aβ25-35 peptide. Furthermore, SalB administration significantly rescue the Aβ25-35 peptide-induced decrease of choline acetyltransferase and brain-derived neurotrophic factor protein levels[2].