Halofuginone hydrobromide (RU-19110 hydrobromide) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga[1]. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM[2]. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3].
Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
(S)-Glutamic acid acts as an excitatory transmitter, shows a direct activating effect on the release of DA from dopaminergic terminals.
Apamin, an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known to block Ca2+-activated K+ channels and prevent carbon tetrachloride-induced liver fibrosis.
Alisol B 23-acetate, a natural triterpenoid, produces protective effects against EE-induced cholestasis, due to FXR-mediated gene regulation.IC50 Value:Target: Anti-hepatotoxic natural product. In vitro: Alisol-B 23-acetate has an effect on FXR activation in a dose-dependent manner using luciferase reporter assay in HepG2 cells [3].In vivo: In alisol B 23-acetate-treated mice, the changes in transporters and enzymes, as well as ameliorative liver histology were abrogated by FXR antagonist guggulsterone [1]. Alisol B 23-acetate treatment in a dose-dependent manner resulted in protection against hepatotoxicity induced by CCl4via FXR activation. Through FXR activation, alisol B 23-acetate promoted hepatocyte proliferation via an induction in hepatic levels of FoxM1b, Cyclin D1 and Cyclin B1. Alisol B 23-acetate also reduced hepatic bile acids through a decrease in hepatic uptake transporter Ntcp, bile acid synthetic enzymes Cyp7a1, Cyp8b1, and an increase in efflux transporter Bsep, Mrp2 expression. In addition, alisol B 23-acetate induced the expression of STAT3 phosphorylation, and STAT3 target genes Bcl-xl and SOCS3, resulting in decreased hepatocyte apoptosis [2].
Bavachinin(7-O-Methylbavachin) is a natural compound isolated from the Chinese herb Fructus Psoraleae;has potent anti-angiogenic activity.IC50 value:Target:in vitro: Isobavachalcone significantly inhibits both oligomerization and fibrillization of Aβ42, whereas bavachinin inhibits fibrillization and leads to off-pathway aggregation. Both of the compounds attenuated Aβ42-induced toxicity in a SH-SY5Y cell model [1]. Bavachinin, has potent anti-angiogenic activity in vitro and in vivo. Bavachinin inhibited increases in HIF-1α activity in human KB carcinoma (HeLa cell derivative) and human HOS osteosarcoma cells under hypoxia in a concentration-dependent manner, probably by enhancing the interaction between von Hippel-Lindau (VHL) and HIF-1α [2].in vivo: significantly inhibited Th2 cytokine production, including IL-4, IL-5 and IL-13. Notably, this compound almost completely blocked inflammation in the ovalbumin (OVA)-sensitized animal asthma model [3].
Lappaconitine hydrobromide, a diterpene alkaloid, is a drug for the treatment of cardiac arrhythmias.IC50 value:Target: A natural product for anti-cardiac arrhythmiasIn vitro: Lappaconitine hydrobromide was found to exert an inhibitory effect on inward tetrodotoxin-sensitive sodium currents without changing their voltage dependence [1]. In vivo: The effect of Lappaconitine hydrobromide on aconitine--induced arrhythmias is due to modulation of genes encoding Na(+)-, K(+)-, Ca(2+)-channels, conducting ionic currents (I(Na), I(to), I(Ks), I(K1), I(CaT)), which are involved in the formation of different phases of the action potential [2]. Lappaconitine hydrobromide was found to be beneficial both in ventricular and supraventricular premature beats. Oral allapinine usually showed its effect 40-60 minutes following its administration, its maximum action being 4-5 hours later, its duration was some 8 hours. The optimal dose of the drug amounted to 75 mg/day [3].
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
D-threitol serves as a antifreeze agent in the Alaskan beetle Upis ceramboides.
Tanshinone IIA sulfonate (sodium) is a water-soluble derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders.
Cholesterol myristate is a natural steroid present in traditional Chinese medicine.
Protoporphyrin IX is the final intermediate in the heme biosynthetic pathway.
Schisandrin has various therapeutic effects on a range of medical conditions such as anti-asthmatic, anti-cancer, and anti-inflammatory effects.IC50 value:Target:in vitro: Sch inhibited the pro-fibrotic activity of TGF-β1 in AML12 cells; thus, it suppressed the accumulation of ECM proteins. Also, Sch inhibited the EMT as assessed by reduced expression of vimentin and fibronectin, and increased E-cadherin and ZO-1 in TGF-β1 induced AML12 cells. Sch reduced TGF-β1-mediated phosphorylation of Smad2/3 and Smad3/4 DNA binding activity. On the other hand, Sch reduced TGF-β1-induced ERK1/2 and PI3K/Akt phosphorylation in the non-Smad pathway [1]. the anti-inflammatory properties of schisandrin result from the inhibition of nitric oxide (NO) production, prostaglandin E(2) (PGE(2)) release, cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) expression, which in turn results from the inhibition of nuclear factor-kappaB (NF-kappaB), c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) activities in a RAW 264.7 macrophage cell line [2].
Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity.
Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.
Salicylic acid inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation.
Methylmalonate is an indicator of Vitamin B-12 deficiency in cancer.
Ketanserin tartrate is a selective 5-HT receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
Apigenin-7-glucoside exhibits significant anti-proliferative and antioxidant activity, scavengers of ROS.In vitro: exhibits significant anti-proliferative activity against B16F10 melanoma cells after 24 and 48 h of incubation. Apigenin-7-glucoside provoks an increase of subG0/G1, S and G2/M phase cell proportion with a significant decrease of cell proportion in G0/G1 phases. Apigenin-7-glucoside enhances melanogenesis synthesis and tyrosinase activity of B16F10 melanoma cells. [1] Api7G specifically induced the differentiation of CD34+ cells towards the erythroid lineage and inhibited the myeloid differentiation. [2] APIG had strong antioxidant activity against reactive oxygen species (ROS) in vitro in a concentration-dependent manner.
[6]-Gingerol is an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
Fluvoxamine is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.Target: SSRIsFluvoxamine is effective in inhibiting 5-ht uptake by blood platelets and brain synaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine [1]. fluvoxamine appears to improve combat-related PTSD symptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits the conclusions of our study. Controlled studies of fluvoxamine in the treatment of PTSD are warranted [2]. Fluvoxamine was less potent at decreasing ethanol self-administration when food was available concurrently versus when ethanol was available in isolation [ED50: 4.0 (2.7-5.9) and 5.1 (4.3-6.0)]. Effects on food were similar under each condition in which food was available. The results demonstrate that the potency of fluvoxamine in reducing ethanol-maintained behavior depends on whether ethanol is available in isolation or in the context of concurrently scheduled food reinforcement [3].Clinical indications: Depression; Obsessive compulsive disorder; Social phobia FDA Approved Date: December 5, 1994Toxicity: Anorexia, Constipation, Dry mouth, Headache, Nausea, Nervousness, Skin rash, Sleep problems, Somnolence, Liver toxicity, Mania, Increase urination, Seizures, Sweating increase, Tremors, or Tourette's syndrome.
D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A2α (cPLA2α) activity.
L-Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine.Target: mAChRHyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.)Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care [1].
Ethynyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.Target: Estrogen ReceptorEthinyl estradiol (EE), also sometimes written as ethinylestradiol, ethynyl estradiol, or ethinyl estradiol, is a derivative of 17β-estradiol (E2), the major endogenous estrogen in humans. EE is an orally bioactive estrogen used in many formulations of combined oral contraceptive pills. It is one of the most commonly used medications for this purpose. Transdermal ethinyl estradiol carries a greater risk of clot formation and venous thromboembolism than 17 beta estradiol, which some have theorized to be related to different amounts of hepatic metabolism after absorption. The same contraindications and precautions apply for EE as with other estrogen medications.Estinyl was a preparation of EE alone that was used for the management of menopausal symptoms and female hypogonadism. EE is released into the environment as a xenoestrogen from the urine and feces of people who take it as a medication. The major concern with unopposed estrogen is of endometrial cancer. As such, the medication is generally prescribed with progesterone in the setting of birth control. The first orally active semisynthetic steroidal estrogen, EE (17α-ethynylestradiol), the 17α-ethynyl analog of E2, was synthesized in 1938 by Hans Herloff Inhoffen and Walter Hohlweg at Schering AG in Berlin.
Octanedioic acid is found to be associated with carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency.
Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
Thiostrepton is a natural cyclic oligopeptide antibiotic, is a natural product of the ribosomally synthesized and post-translationally modified peptide (RiPP) class.
Ercalcidiol is a metabolite of vitamin D2, is regarded as an indicator of vitamin D nutritional status.
8-O-Acetyl shanzhiside methyl ester (ND01) is an iridoid glucoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant in Xi-zang. 8-O-Acetyl shanzhiside methyl ester could inhibt NF-κB.