Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
Ginkgolic Acid is a natural compound with suspected cytotoxic, allergenic, mutagenic and carcinogenic properties, and it can inhibit protein SUMOylation both in vitro and in vivo without affecting in vivo ubiquitination.
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].
2',4'-Dihydroxyacetophenone (Resacetophenone) is acetophenone carrying hydroxy substituents at positions 2' and 4'. A plant metabolite.
Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.
4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth[1][2][3][4].
Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis.target: COX-LOX [1]In vitro: Chebulagic acid can enhance the autophagy. Chebulagic acid exert anti-inflammatory and anti-infective effects. [1] [2] Chebulagic acid also show a protective effect against 1-methyl-4-phenylpyridinium (MPP+) - induce cytotoxicity which mimics the pathological symptom of Parkinson's disease. Chebulagic acid inhibit the LPS-induced upregulation of TNF-α and IL-1β in a dose- and time-dependent manner. Furthermore, LPS-activated MAPK signaling is inhibited by CA treatment in the EA.hy926 cells. [3]
Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects[1].
Methyl Paraben, isolated from the barks of Tsuga dumosa the methyl ester of p-hydroxybenzoic acid, is a standardized chemical allergen. Methyl Paraben is a stable, non-volatile compound used as an antimicrobial preservative in foods, drugs and cosmetics. The physiologic effect of Methyl Paraben is by means of increased histamine release, and cell-mediated immunity[1].
Oxyresveratrol is neuroprotective and inhibits the apoptotic cell death in transient cerebral ischemia. It effectively scavenges H2O2, NO (IC50 = 45.3 μM), and the artificial free radical 2,2-diphenyl-l-picrylhydrazyl (IC50 = 28.9 μM) In vitro: 1)oxyresveratrol exhibited more than 50% inhibition at 100 μM on L-tyrosine oxidation by murine tyrosinase activity.2) oxyresveratrol showed an IC50 value of 52.7 μM on the enzyme activity. 3) oxyresveratrol works through reversible inhibition of tyrosinase activity rather than suppression of the expression and synthesis of the enzyme.[2] In vivo: 1) Oxyresveratrol (10 or 20 mg/kg) significantly reduced the brain infarct volume by approximately 54% and 63%, respectively, when compared to vehicle-treated MCAO rats.2) oxyresveratrol treatment diminished cytochrome c release and decreasedcaspase-3 activation in MCAO rats. [3]
4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[1].
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
Curcumin is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase ((HATs)) and also shows inhibitory effects on NF-κB and MAPKs.
4-Ethylphenol is a volatile phenolic compound associated with off-odour in wine.
Arbutin(β-Arbutin) is a glycoside; a glycosylated hydroquinone extracted from the bearberry plant in the genus Arctostaphylos; inhibits tyrosinase and thus prevents the formation of melanin.IC50 value:Target: tyrosinase
Probucol is an anti-hyperlipidemic drug by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.Target: OthersProbucol is a drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. Probucol inhibited cholesterol efflux up to 80% in J774 macrophages expressing ABCA1. probucol is an effective inhibitor of ABCA1-mediated cholesterol efflux without influencing scavenger receptor class B type I-mediated efflux. The inhibition of ABCA1 translocation to the plasma membrane may in part explain the reported in vivo high-density lipoprotein-lowering action of probucol [1].
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
Butein, a plant polyphenol isolated from Rhus verniciflua, inhibit the activation of protein tyrosine kinase and EGFR. target: EGFR [1]In vitro: 1) Butein inhibited the activation of AKT, extracellular signal-regulated kinase (ERKs) and p38 kinases in the presence of cisplatin.[2] 2) FoxO3a and its downstream molecules play a role in the synergistic effects of butein and cisplatin.[2]3) Butein suppresses cell proliferation and enhances apoptosis in paclitaxel-resistant ovarian cancer cells.[3]4) Butein activates FOXO3a/p27kip1 pathway in ALL cell lines.[4]5) Butein inhibited not only the epidermal growth factor (EGF)-stimulated auto-phosphotyrosine level of EGF receptor in HepG2 cells but also tyrosine-specific protein kinase activities of EGF receptor (IC50= 65 μM) and p60c-src(IC50= 65 μM)In vivo: 1) Butein in combination with cisplatin suppresses tumor growth and increases FoxO3a expression.[1]
Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation[1]. Anti-inflammatory activity[1].
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM[1], and also inhibits ACE-I activity[2]. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells[1]. Sinapinic acid shows antioxidant and antidiabetic activities[2]. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats[3].
Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor[3] properties[1]. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways[2]. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells[3].
(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
Syringic acid is correlated with high antioxidant activity and inhibition of LDL oxidation.
Eugenol is an essential oil found in cloves with antibacterial, anthelmintic and antioxidant activity. Eugenol is shown to inhibit lipid peroxidation.
Gallic acid is an antioxidant which can inhibit both COX-2.
Polydatin (Piceid), extracted from the roots of Polygonum cuspidatum Sieb, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models.
Paeonol is an active extraction from the root of Paeonia suffruticosa, Paeonol inhibits MAO-A and MAO-B with IC50 of 54.6 μM and 42.5 μM, respectively.
Bornyl acetate is a potent odorant, exhibiting one of the highest flavor dilution factor (FD factor).
2-Hydroxy-4-methoxybenzoic is a derivative of methoxybenzoic. 2-Hydroxy-4-methoxybenzoic is a potential biomarker.