Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
Monomelittoside is a natural compound.
Wilforlide A is a natural product, separated from the ethanolic extract of tripterygium wilfordii. IC50 value:Target:In vitro:In vivo: Carrageenan-induced rat pedal swelling, tampon-induced rat granulation, and mice ear inhibition rate of swelling trail results show that high-dose wilforlide A has obvious anti-inflammatory effect, but has no significant immune suppressive activity [1].
Ingenol-3,4,5,20-diacetonide is a natural compound.
1-O-Acetylbritannilactone is an active compound isolated from Inula Britannica L. 1-O-Acetylbritannilactone inhibits VEGF-mediated activation of Src and FAK. 1-O-Acetylbritannilactone inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
Alisol F is a natural product.
Epoxymicheliolide is a micheliolide derivative.
Ginsenoside Rh2 is isolated from the root of Ginseng. Ginsenoside Rh2 induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.
Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
Alisol G is a natural product extracted from Rhizoma Alismatis.
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
Isoalantolactone is an apoptosis inducer, which also acts as an alkylating agent.
Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
Genipin 1-β-D-gentiobioside (Genipin 1-gentiobioside) is one of the most abundant and bioactive iridoid glycosides in Gardenia jasminoides Ellis, which possesses hepatoprotective, anti-inflammatory, antioxidant, and antithrombotic activities.
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
Ajugol is an iridiod glucoside.
Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.
Farnesol is a sesquiterpene alcohol that modulates cell-to-cell communication in Candida albicans, and has the activity in inhibiting bacteria.
Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
Alismoxide is a natural product.
Dipsacoside B is a major bioactive saponin, which can be used as a marker.
Astragaloside II is a natural isolated from Astragalus.IC50 value:Target:In vitro:In vivo: The developed and validated method has been successfully applied to the quantification and pharmacokinetic study of AST II in rats after intravenous and oral administration of AST II. The oral absolute bioavailability (F) of AST II was calculated to be 0.79 ± 0.16% with an elimination half-life (t1/2) value of 1.92 ± 0.30 h, suggesting its poor absorption and/or strong metabolism in vivo [1].
Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties.
Arglabin is a sesquiterpene gamma-lactone is isolated from Artemisia glabella; anticancer natural compound.IC50 value:Target: anticancerin vitro: Arglabin-stimulated macrophages displayed a strong cytotoxic activity and the lowest doses (1.25 micrograms/mL and 0.125 micrograms/mL) induced a significant stimulation of cell mitochondrial metabolism, which correlated with [3H]TdR uptake by J774.1 cells under the same experimental conditions. Arglabin triggered the production of the three cytokines from J774-1 cells. However, the pattern of cytokine secretion differed to some extent, according to the methodology used for cytokine measurement: either traditional bioassay or specific immunoassay (ELISA) [1]. Arglabin exhibits antiexudative and antiproliferative properties on the models of acute aseptic inflammation caused by formalin, carrageenan, and histamine, and on the model of proliferative inflammation accompanying cotton-pellet granuloma [2]. Arglabin is able to reduce the proportion of AML stem cells (CD34+CD38-) in primary AML cells [3].
Costunolide, a sesquiterpene lactone, exhibits anti-inflammatory and anti-oxidant properties and mediates apoptosis.IC50 Value: 6.2 - 9.8 ug/mL(sarcoma cells viability)[3]Target: Apoptosis inducerin vitro: Costunolide significantly inhibited RANKL-induced BMM differentiation into osteoclasts in a dose-dependent manner without affecting cytotoxicity. Costunolide did not regulate the early signaling pathways of RANKL, including the mitogen-activated protein kinase and NF-κB pathways. However, costunolide suppressed nuclear factor of activated T-cells, cytoplasmic 1 (NFATc1) expression via inhibition of c-Fos transcriptional activity without affecting RANKL-induced c-Fos expression. The inhibitory effects ofcostunolide were rescued by overexpression of constitutively active (CA)-NFATc1 [1]. Exposure of T24 cells to costunolide was also associated with increased expression of Bax, down-regulation of Bcl-2, survivin and significant activation of caspase-3, and its downstream target PARP [2]. Both costunolide and dehydrocostus lactone inhibited cell viability dose- and time-dependently. IC50 values ranged from 6.2 ug/mL to 9.8 ug/mL. Cells treated with costunolide showed no changes in cell cycle, little in caspase 3/7 activity, and low levels of cleaved caspase-3 after 24 and 48 h [3].in vivo: Neither costunolide nor alpha-MGBL affected the blood-ethanol elevation in pylorus-ligated rats or that induced by intraperitoneal and intraduodenal ethanol administration [4]. Costunolide and alpha-MGBL suppressed gastric emptying in rats given 20% ethanol and 1% sodium carboxymethyl cellulose.Clinical trial:
Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
Betulonic acid belongs to the pentacyclic triterpenic derivative class, has antitumor activities.In vitro: BEA-NP is found over three-times more permeable than that solubilized by DMSO in Caco-2 cell monocultures.[1]In vivo: The tumor growth in the S180 berry mice orally doses with BEA-NP at 75 mg/kg is inhibited by 50%. Rubusoside is effective in solubilizing BEA, maintaining its cytotoxicity, enhancing its permeability and reducing tumor growth when orally administered.[1] antitumor activities against MGC-803, PC3, Bcap-37, A375, and MCF-7 human cancer cell lines In vivo: The animals are treated with betulonic acid amide (50 mg/kg in Tween aqueous solution) and heptral (6 mg/kg) as hepatoprotective compounds. It is found that betulonic acid amide stimulats the regenerative response in hepatocytes under conditions of combined toxic exposure and promots recovery of their qualitative and quantitative characteristics. [2]
Quillaic acid(Quillaja sapogenin) is the major aglycone of the widely studied saponins of the Chilean indigenous tree Quillaja saponaria Mol; can elicit dose-dependent antinociceptive effects in two murine thermal models.
Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.In vitro: Additions of pulsatilloside A and anemoside A3, at dosages ranging from 0.1, 1 and 10 μg/ml, protected PC12 cells from apoptosis. [1]In vivo:AA3 also acts as a non-competitive NMDA receptor (NMDAR) modulator with a neuroprotective capacity against ischemic brain injury and overexcitation in rats. [2] Anemoside A3 produces relaxation in rat renal arteries through multiple mechanisms. [3]