Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
Cholesterol myristate is a natural steroid present in traditional Chinese medicine.
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.
Ercalcidiol is a metabolite of vitamin D2, is regarded as an indicator of vitamin D nutritional status.
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
Daucosterol is a natural sterolin. IC50 value:Target:In vitro: In the study of the effects of daucosterol on the survival of cultured cortical neurons after neurons were subjected to oxygen and glucose deprivation and simulated reperfusion (OGD/R)(2), the results showed that post-treatment of daucosterol significantly reduced neuronal loss, as well as apoptotic rate and caspase-3 activity, displaying the neuroprotective activity. We also found that daucosterol increased the expression level of IGF1 protein, diminished the down-regulation of p-AKT(3) and p-GSK-3β(4), thus activating the AKT(5) signal pathway [1]. Cell counting kit-8 (CCK-8) assay showed that daucosterol significantly increased the quantity of viable cells and the effectiveness of daucosterol was similar to that of basic fibroblast growth factor (bFGF) and epidermal growth factor (EGF) [2]. Daucosterol inhibits the proliferation of human breast cancer cell line MCF-7 and gastric cancer cell lines MGC803, BGC823 and AGS in a dose-dependent manner. Furthermore, daucosterol inhibits murine hepatoma H22 cell growth in ICR mice. Daucosterol treatment induces intracellular ROS generation and autophagy, but not apoptotic cell death. Treatment with ROS scavenger GSH (reduced glutathione), NAC (N-acetyl-l-cysteine) or autophagy inhibitor 3-Methyladenine (3-MA) counteracted daucosterol-induced autophagy and growth inhibition in BGC823 and MCF-7 cancer cells [3].In vivo:
Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.IC50 Value:Target:In vitro: The effects of Resibufogenin on the outward delayed rectifier potassium current (IK) and outward transient potassium current (IA) in rat hippocampal neurons was investigated, and it inhibited both IK and IA, at 1 μM concentration RBG could alter some channel kinetics and gating properties of IK, such as steady-state activation and inactivation curves, open probability and time constants [1].In vivo: Resibufogenin prevented evidence of oxidative stress in "preeclamptic" rats [2].
Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
Stigmastanol is a phytosterol found in a variety of plant sources.
Cimiracemoside D is a natural product found in Actaea racemosa with unknown details.
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:
Allopregnanolone is a progesterone metabolite. Allopregnanolone is an allosteric modulator of the GABA receptor.
Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
Beta-Sitosterol weakly inhibits porcine pancreatic lipase (PPL) activity. Sitosterol is an important compound extracted from the leaves of Aloe vera.
Ginsenoside Re is an extract from Panax notoginseng. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
Vitamin D2 (Ergocalciferol) is a form of vitamin D, used as a vitamin D supplement. Target: Ergocalciferol is a secosteroid formed by a photochemical bond breaking of a steroid, specifically, by the action of ultraviolet light on ergosterol.
(20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.IC50 value:Target: apoptosis inducer(20S)-Protopanaxadiol was used to induce cytotoxicity for two human glioma cell lines, SF188 and U87MG. For the SF188 cells, (20S)-Protopanaxadiol activated caspases-3, -8, -7, and -9 within 3 h and induced rapid apoptosis, which could be partially inhibited by a general caspase blocker and completely abolished when the caspase blocker was used in combination with an antioxidant. (20S)-Protopanaxadiol also induced cell death in U87MG cells but did not activate any caspases in these cells [1]. aPPD was able to inhibit P-gp activity as potently as verapamil on MDR cells. The blockage of P-gp activity was highly reversible as wash-out of aPPD resulted in an immediate recovery of P-gp activity. Unlike verapamil, aPPD did not affect ATPase activity of P-gp suggesting a different mechanism of action [2].
Prednisone (Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound.Target: OthersPrednisone is a synthetic corticosteroid drug that is particularly effective as an immunosuppressant drug. It is used to treat certain inflammatory diseases (such as moderate allergic reactions) and (at higher doses) some types of cancer, but has significant adverse effects. Because it suppresses the immune system, it leaves patients more susceptible to infections.Prednisone can also be used in the treatment of decompensated heart failure to potentiate renal responsiveness to diuretics, especially in heart failure patients with refractory diuretic resistance with large dose of loop diuretics. The mechanism is prednisone, as a glucocorticoid, can improve renal responsiveness to atrial natriuretic peptide by increasing the density of natriuretic peptide receptor type A in the renal inner medullary collecting duct, inducing a potent diuresis.
25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.
Alisol A is a natural product.
Gypenoside XVII, a novel phytoestrogen belonging to the gypenosides, can activate estrogen receptors.
Alisol A 24-acetate is a natural product.
Sarsasapogenin is a sapogenin from the Chinese medical herb Anemarrhena asphodeloides Bunge, with antidiabetic, anti-oxidative, anticancer and anti-inflamatory activities.
Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su; has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro.IC50 value:Target: Anticaner natural compoundin vitro: bufalin remarkably inhibited growth in human gallbladder cancer cells by decreasing cell proliferation, inducing cell cycle arrest and apoptosis in a dose-dependent manner. Bufalin also disrupted the mitochondrial membrane potential (ΔΨm) and regulated the expression of cell cycle and apoptosis regulatory molecules. Activation of caspase-9 and the subsequent activation of caspase-3 indicated that bufalin may be inducing mitochondria apoptosis pathways [1]. bufalin suppressed the protein levels associated with DNA damage and repair, such as a DNA dependent serine/threonine protein kinase (DNA-PK), DNA repair proteins breast cancer 1, early onset (BRCA1), 14-3-3 σ (an important checkpoint keeper of DDR), mediator of DNA damage checkpoint 1 (MDC1), O6-ethylguanine-DNA methyltransferase (MGMT) and p53 (tumor suppressor protein) [2]. TNF-α significantly increased p65 translocation into nucleus (P < 0.01) and enhanced NF-κB DNA-binding activity, which were dose-dependently inhibited by bufalin. Furthermore, bufalin attenuated the TNF-α-induced interleukin-1beta (IL-1β), IL-6, and IL-8 production in RAFLSs in a concentration-dependent manner [3]. bufalin enhanced TRAIL-induced apoptosis in MCF-7 and MDA-MB-231 breast cancer cells by activating the extrinsic apoptotic pathway. Bufalin also promoted the clustering of death receptor 4 (DR4) and DR5 in aggregated lipid rafts [4].in vivo: bufalin (0.3 and 0.6 mg/kg, i.p.) potently decreased carrageenan-induced paw edema. Bufalin down regulated the expression levels of nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) during these treatments [5].
5α-Cholestan-3β-ol is a derivitized steroid compound, which is isolated from the testes of White Carneau pigeons.
Pseudobufarenogin is a natural compound extracted from toad species with unknown details.
Lathosterol is a cholesterol-like molecule. Serum Lathosterol concentration is an indicator of whole-body cholesterol synthesis.