Licochalcone A, a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch, presents obvious anti-cancer effects. The IC50 value is 0.97 μM for UGT1A1.
p-Hydroxycinnamic acid, a common dietary phenol, could inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.
Praeruptorin B is an inhibitor of sterol regulatory element-binding proteins (SREBPs).
Inosine, an endogenous purine nucleoside, has immunomodulatory, neuroprotective, and analgesic properties. In vitro: Inosine has been shown to stimulate axonal growth in cell culture and promote corticospinal tract axons to sprout collateral branches after stroke, spinal cord injury and TBI in rodent models.[1] Inosine dose-dependently stimulates cAMP production mediated through the A2AR. Inosine dose-dependently induces A2AR-mediated ERK1/2 phosphorylation.[2] In vivo: The reference for Inosine is 1 or 10 mg/kg, i.p. Preventive treatment with inosine inhibits the development and progression of EAE in C57Bl/6 mice. neuroinflammation and demyelinating processes are blocked by inosine treatment. Additionally, inosine consistently inhibits IL-17 levels in peripheral lymphoid tissue, as well as IL-4 levels and A2AR up-regulation in the spinal cord, likely, through an ERK1-independent pathway. [3] inosine acting through adenosine receptors (ARs) exerts a wide range of anti-inflammatory and immunomodulatory effects in vivo. [2]
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.
Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.
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]
D-Gluconic acid is the carboxylic acid by the oxidation with antiseptic and chelating properties.
20(R)-Protopanaxatriol is a natural aglycone of ginsenosides Re, Rf, Rg1, Rg2 and Rh.
Hydroxycotinine is the main nicotine metabolite detected in smokers urine.
5-Hydroxydopamine is a naturally occurring amine in human urine.
Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
5-Methoxytryptophol is a natural indole present in the pineal gland.
N-Methylsarcosine is an amino acid building block for protein, found in a small amount in the body.
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP.
Isospaglumic acid is a neuropeptide found in millimolar concentrations in brain.
Stigmasterol is a plant sterol which has been focused on the cholesterol-lowering activity and is valued as an anti-stiffness factor in the therapy of rheumatic diseases.
Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer.IC50 value:Target:In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].In vivo:
N-Acetyl-D-Glucosamine is a monosaccharide derivative of glucose.
1,3-Diaminopropane, a three carbon diamine, is an ornithine decarboxylase inhibitor.
Nagilactone B, extracted from the root bark of Podocarpus nagi, is a liver X receptor (LXR) agonist.
(+)-Sparteine is a natural alkaloid acting as a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.
Daurisoline is a hERG inhibitor and also an autophagy blocker.
Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM.
Lobetyolin is derived from Codonopsis pilosula and has antioxidative effect.
Scopolamine hydrobromide is a high affinity (nM) muscarinic antagonist. 5-HT3 receptor-responses are reversibly inhibited by Scopolamine with an IC50 of 2.09 μM.
6-Aminocaproic acid is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.Target: Others6-aminohexanoic acid is a derivative and analogue of the amino acid lysine, which makes it an effective inhibitor for enzymes that bind that particular residue. Such enzymes include proteolytic enzymes like plasmin, the enzyme responsible for fibrinolysis. Aminocaproic acid is also an intermediate in the polymerization of Nylon-6, where it is formed by ring-opening hydrolysis of caprolactam.Aminocaproic acid is used to treat excessive postoperative bleeding, especially after procedures in which a great amount of bleeding is expected, such as cardiac surgery. Aminocaproic acid can also be used to treat the overdose and/or toxic effects of the thrombolytic pharmacologic agents tissue plasminogen activator and streptokinase [1, 2].
Ethylmalonic acid is non-carcinogenic potentially toxic and associated with anorexia nervosa and malonyl-CoA decarboxylase deficiency.
Benzoylaconine(Isaconitine; Pikraconitin) is an alkaloid in the Chinese traditional medicine Radix Aconiti Lateralis Preparata (Fuzi).
β-Lapachone is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.