Triterpenes

Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.

Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities.

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.

Ursolic acid (Prunol) is a natural pentacyclic triterpenoid carboxylic acid, exerts anti-tumor effects and is an effective compound for cancer prevention and therapy.

Saponins (Saponin) is a class of chemical compound of glycosides found in particular abundance in various plant species. In plants, Saponins may serve as anti-feedants, and to protect the plant against microbes and fungi.

Cholic acid-Cit is a citrinate-conjugated form of Cholic acid (HY-N0324). Cholic acid-Cit can be used in studies related to Crohn's disease.

3-epi-18β-Glycyrrhetinic acid is an inhibitor of 11β-HSD1 and 11β-HSD2, with an IC₅₀ of 0.17 μM against 11β-HSD2. 3-epi-18β-Glycyrrhetinic acid acts as a weak substrate for sulfotransferase 2A1. It serves as a biomarker for the toxicity of licorice-related pseudoaldosteronism. 3-epi-18β-Glycyrrhetinic acid is applicable to studies related to pseudoaldosteronism.

Polygalasaponin XXXII is an orally active cognitive enhancer. Polygalasaponin XXXII promotes the phosphorylation of ERK, CREB, Synapsin I and TrkB. Polygalasaponin XXXII enhances basal synaptic transmission. Polygalasaponin XXXII attenuates Scopolamine (HY-N0296)-induced cognitive impairment and improves hippocampus-dependent learning and memory abilities. Polygalasaponin XXXII can be used in research related to cognitive dysfunction.

Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.

Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses TGF-β/Smad signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.

Ginsenoside Rg1 is one of the major active components of Panax ginseng. Ginsenoside Rg1 ameliorates the impaired cognitive function, displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

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. Betulinic acid can cross the blood-brain barrier.

20(S)-Ginsenoside Rg3 is the main component of Panax ginseng C. A. Meyer. Ginsenoside Rg3 inhibits Na⁺ and hKv1.4 channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

7-Ketocholesterol is an oxidation product of cholesterol, widely present in atherosclerotic plaques, and has a stronger atherogenic effect than cholesterol. 7-Ketocholesterol can inhibit the rate-limiting enzymes involved in bile acid and cholesterol synthesis, such as cholesterol 7α-hydroxylase and HMG-CoA reductase. 7-Ketocholesterol exhibits pro-inflammatory effects both in vivo and in vitro and can induce cell apoptosis (apoptosis).

Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na⁺, K⁺-ATPase activity with an IC₅₀ of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .

Squalene (Super Squalene) is an intermediate product in the synthesis of cholesterol, and shows several pharmacological properties such as hypolipidemic, hepatoprotective, antiatherosclerotic, cardioprotective, antioxidant, and antitumour activity.

18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhiza uralensis and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC₅₀s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.

Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases.

Ginsenoside Rh2 (20(S)-Ginsenoside Rh2) induces the activation of caspase-8 and caspase-9. Ginsenoside Rh2 induces cancer cell apoptosis in a multi-path manner.