Astragaloside III is a natural product isolated from Astragalus.
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
Anemoside B4 is Pulsatilla koreana Nakai that have many numerous biological effects in vitro, including enhancing hypoglycemic, anti-tumor, neuroprotective and anti-angiogenic activity. AB4 can inhibit the secretion of IL-10; SSA, SSD and PNS up-regulated IL-2 expression.[1] AB4, with IC50 value more than 390 ug/mL. Anemoside B4 inhibits cell proliferation.[2] Anemoside B4 can significantly suppress the secretion of the inflammatory factor E-selectin by endothelial cells. [3]
Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
Ginsenoside Rk3 is present in the roots Panax notoginseng herbs. Ginsenoside Rk3 significantly inhibits TNF-α-induced NF-κB transcriptional activity, with an IC50 of 14.24±1.30 μM in HepG2 cells
(-)-Borneol has a highly efficacious positive modulating action at GABA receptor with an EC50 of 237 μM.
Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities[1]. Camphor is a TRPV3 agonist[2].
Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.Gracillin could induce cell cycle arrest, oxidative stress, and apoptosis in HL60 cells.[1]
Morroniside has neuroprotective effect by inhibiting neuron apoptosis and MMP2/9 expression.
(+)-Borneol (d-Borneol) is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of 248 μM.
Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced NF-κB activation and ERK phosphorylation in BMMs. [1] EA inhibit IL-1β-induced inflammation in chondrocytes. [2]In vivo: Echinocystic acid reduces reserpine-induced pain/depression dyad in mice. [3]
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptorA (GABAA)-mediated ion channel currents (IGABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β.
Siamenoside I is one of the mogrosides that has several kinds of bioactivities.
Geniposide is an iridoid glucoside extracted from Gardenia jasminoides Ellis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
Ginsenoside Rb2 is one of the main bioactive components of ginseng extracts. Rb2 can upregulate GPR120 gene expression.
Panaxadiol is a novel antitumor agent extracted from the Chinese medical herb Panax ginseng.
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]
Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.
Rebaudioside C(Dulcoside B) is used as natural sweeteners to diabetics and others on carbohydrate-controlled diets.
Forskolin is a potent adenylate cyclase activator, with IC50 and EC50 of 41 nM and 0.5 μM for type I adenylyl cyclase, respectively.
Astragaloside A is one of the major active constituents of Astragalus membranaceus in Traditional Chinese Medicine; has been widely used to treat ischemic diseases.IC50 value: Target: in vitro: AS-IV treatment promotes umbilical vein endothelial cells (HUVEC) proliferation, migration, and tube formation. AS-IV treatment also activates JAK2/STAT3 and ERK1/2 signaling pathways, and up-regulates endothelial nitric oxide synthase (eNOS) expression and nitric oxide (NO) production [1]. Administration of astragaloside IV (16, 32, and 64 μM) 1 h prior to lipopolysaccharide stimulation dose-dependently attenuated cardiac hypertrophy induced by lipopolysaccharide. Further studies demonstrated that astragaloside IV inhibited the increment of the resting intracellular free Ca2+, and its effect was similar to verapamil [2]. ASI could inhibit cells apoptosis induced by high glucose (25mmol/L) in dose-dependent and time-dependent manners. ASI also inhibited high glucose-induced expression of TGF-β1 and activation of p38 MAPK pathway at the protein level. Furthermore, ASI increased HGF production in human tubular epithelial cells [3].in vivo: the growth of tumor was suppressed by AS-IV treatment in vivo. AS-IV also could down-regulate regulatory T cells (Tregs) and up-regulate cytotoxic T lymphocytes (CTLs) in vivo and in vitro[4]. As an in vivo model, mice subjected to unilateral ureteral obstruction (UUO) were administered AS-IV (20 mg/kg) by intraperitoneal injection for 7 days. AS-IV significantly alleviated renal mass loss and reduced the expression of α-smooth muscle actin, fibronectin, and collagen IV both in vitro and in vivo [5].
Oxypaeoniflorin is a natural product derived from Radix Paeoniae Rubra and Radix Paeoniae Alba.
Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.IC50 value:Target:The anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside II are stronger than those of tubeimoside I, and the acute toxicity of tubeimoside II is lower than that of tubeimoside I; the anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside III are stronger than those of tubeimoside II, and the acute toxicity of tubeimoside III is also stronger than that of tubeimoside II.
Panaxatriol is a natural product that can relieve myelosuppression induced by radiation injury.
Artemisinin is an anti-malarial drug isolated from the aerial parts of Artemisia annua L. plants.
7-epi-Taxol is an active metabolite of taxol, with activity comparable to that of taxol against cell replication, promoting microtubule bundle formation and against microtubule depolymerization.
Brusatol, isolated from the Brucea javanica plant, inhibits Nrf2.
Madecassoside is a pentacyclic triterpene isolated from Centella asitica (L.), as an anti-inflammatory, anti-oxidative activities and anti-aging agent. [1]In vitro: Madecassoside exhibit significant anti-proliferative and anti-invasive effect in HGF-induced HepG2 and SMMC-77 cells. Madecassoside inhibit the HGF-induced activation of cMET-PKC-ERK1/2-COX-2-PGE2cascade. [1]In vivo: Administration of madecassoside, p.o. , exhibit a direct anti-PF effect in mice. Madecassoside increase the expression of hepatocyte growth factor (HGF) in colon tissues, and HGF receptor antagonists attenuated its anti-PF effect. madecassoside in mice are not mediated by its metabolites or itself after absorption into blood. Instead, madecassoside increases the activity of PPAR-γ, which subsequently increases HGF expression in colonic epithelial cells. [2] The reference for administration is 12 mg/kg. [3]
Isoastragaloside II is an astragaloside, which is isolated from the hairy root culture of Astragalus membranaceus.