They are produced by plants as part of their self-defense mechanism[6] with important sub-classes including ginsenosides[7] and eleutherosides. Phytomedicine 19:32–37, Kuang H-X, Li H-W, Wang Q-H, Yang B-Y, Wang Z-B, Xia Y-G (2011) Triterpenoids from the roots of Sanguisorba tenuifolia var. Diabetologia 45:1528–1532, Ali MS, Jahangir M, ul Hussan SS, Choudhary MI (2002) Inhibition of α-glucosidase by oleanolic acid and its synthetic derivatives. The use of triterpenes as AGEs inhibitors may be a potentially effective strategy to prevent diabetic complications. Both compounds have enone functions in their A- and C-rings and an electron-withdrawing nitrile group at the C-2 position in the A-ring.46 A chemical feature shown to be essential for the activity of the synthetic triterpenoids focuses on the electron-withdrawing nitrile group that activates the A-ring enone, thereby allowing it to serve as an acceptor of a Michael addition to covalently, but reversibly, bind activated sulfhydryl groups of cysteine residues in protein targets.47 Relevant chemical structures are shown in the succeeding text. An interesting finding for TGR5 is its role in energy metabolism. 2011). According to the result of ” Phytochemical screening, antioxidant, and antimicrobial activities of the crude leaves’ extract from Ipomoea batatas (L.) Lam? 2012). Triterpenes can become prototypes for anti-diabetic drugs. Article ID 128402, Lipson VV, Zamigajlo LL, Petrova ON (2011) Development of 11β-HSD1 inhibitors for the treatment of metabolic syndrome. Calceolarioside B is abundant in both Akebia and Stauntonia. In a study of ” Suppression of the inflammatory response by triterpenes isolated from the mushroom Ganoderma lucidum” by Dudhgaonkar S, Thyagarajan A, Sliva D. (Source Cancer Research Laboratory, Methodist Research Institute, 1800 N Capitol Ave, E504, Indianapolis, IN 46202, USA), posted in PubMed, researchers found that Apart from its anti-inflammatory activity, GLT suppressed cell proliferation of RAW264.7 cells through cell cycle arrest at G0/G1-G2M, which was mediated by the down-regulation of expression of cell cycle regulatory proteins cyclin D1, CDK4 and cyclin B1, respectively. This study aimed to characterize the hepatotoxic potential of OA. Phytother Res 22:1303–1306, Lai Y-C, Chen C-K, Tsai S-F, Lee S-S (2012) Triterpenes as α-glucosidase inhibitors from Fagus hayatae. Liver oil of shark (e.g., gray reef shark, Africa, the Mediterranean Basin from Portugal to the Levant, the Arabian Peninsula, and southern Asia as far east as China, as well as the Canary Islands, Mauritius and Reunion, Native (for many species endemic) to the Americas, from the southern United States south through to northern Argentina, Native to the Neotropics, Madagascar, New Guinea, and southern Asia from Pakistan east to Vietnam, Native to Tropical Asia and Queensland, Australia, Native to Europe, northern Asia, Greenland, western Canada, and the western United States, Native and abundant throughout northern Europe, Iceland, northern Asia, and Greenland, Various species from Cucurbitaceae family, Native to Europe, Asia, northern Africa, and North America, Wild forms occur in Sweden, the Netherlands, and Britain, Native to tropical Indomalaya and Australia. When they were used at a concentration of 100 μM the percentage of enzyme inhibition was 48.2, 54.6 and 75.9 %, respectively (Matsuda et al. Other compounds with agonistic properties include betulinic acid and ursolic acid (Genet et al. Planta Med 72:261–263, Na M, Kim BY, Osada H, Ahn JS (2009) Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta. Ursolic acid administrated to insulin-deficient diabetic mice at a dose of 0.01 %, as a food supplement prevented diabetic nephropathy through significant inhibition in 75 % of glomerular hypertrophy and suppression of type IV collagen accumulation in glomeruli. A review of literature revealed a multidirectional effect of triterpenes. A handbook of bioactive compounds from plants. Plant glycosyltransferases, which catalyze this glycosylation reaction, play a key step in preparing structure diverse and valuable triterpene glycosides. Further, particular secondary metabolites, namely caloncobalactones A and B (94 and 95) [39], glaucartanoic acid B (104) [43], donellanic acids A–C (128–130) [52], and 16,22-diacetyl-2,26-dihydroxy-29-nor-24-methyl-19(9→1)-abeocycloart-9(11),24(24a)-dien-3,23-dione (167) [58], have been obtained from Cameroonian medicinal plants Caloncoba glauca, Donella ubanguiensis, and Neoboutonia melleri. Some of the natural compounds examined were more active or had activity similar to RK-682 (IC50 4.5 μM), which was used almost in all experiments as a positive control. All saponins tend to be immune modulating and have consistently shown antineoplastic effects (Singh, 1984; Bouic, 1999; Awad, 2000). Animals, plants and fungi all produce triterpenes, including squalene, the precursor to all steroids.[1][2]. Article Chronically elevated local glucocorticoid action as a result of increased 11β-HSD1 activity is associated with metabolic syndrome, obesity, insulin resistance, type 2 diabetes mellitus and cardiovascular complications (Wamil and Seckl 2007). 2008). It can be achieved through the inhibition of α-glucosidases and α-amylases which delay the absorbance of carbohydrates in the intestine, leading to a decrease in the postprandial insulin level (de Sales et al. Lancet 378:182–197, Tan M-J, Ye J-M, Turner N, Hohnen-Behrens C, Ke C-Q, Tang C-P, Chen T, Weiss C-H, Gesing E-R, Rowland A, James DE, Ye Y (2008) Antidiabetic activities of triterpenoids isolated from bitter melon associated with activation of the AMPK pathway. In particular the lupane-, oleanane-, and ursane triterpenes display various pharmacological effects while being devoid of prominent toxicity. They are responsible for dephosphorylation process of the receptor β-subunit (Goldstein 2002). This material was further converted into the high purity 3,24;16,22-di-, Protostane triterpenes belong to a group of tetracyclic triterpene that exhibit unique structural characteristics. Ezzat SM, Abdallah HM, Fawzy GA, El-Maraghy SA (Source from a Department of Pharmacognosy, Faculty of Pharmacy , Cairo University , Cairo 11562 , Egypt), posted in PubMed, researchers found that The hepatoprotection of the AE and its fractions was assessed in terms of the reduction in histological damage, accompanied by restoration of the liver enzymes (alanine amino transferase (ALT), aspartate amino transferase (AST), lactate dehydrogenase (LDH)), a reduction in the inflammatory markers (tumour necrosis-α (TNF-α), nitric oxide (NO), N-acetyl-β-D-glucosaminidase (NAG) and myloperoxidase (MPO) in serum) and restoration of the oxidant balance by decreasing the serum and hepatic malondialdehyde (MDA) levels, along with increasing the activity of hepatic catalase (CAT), glutathione peroxidase (GSHPx) and the non-enzymatic antioxidant glutathione (GSH). Triterpenes as α-glucosidase and α-amylase inhibitors The therapeutic approach to treating type 2 DM is to decrease postprandial glucose levels. PLoS One 7:1–12, Zhang W, Hong D, Zhou Y, Zhang Y, Shen Q, Li J-Y, Hu L-H, LI J (2006) Ursolic acid and its derivative inhibit protein tyrosine phosphatase 1B, enhancing insulin receptor phosphorylation and stimulating glucose uptake. those of the individual authors and contributors and not of the publisher and the editor(s). 2011). Among animal models of DM those with pharmacologically induced diabetes and surgical or genetic models of diabetes are used. Chem Pharml Bull 59:1396–1399, Sato M, Tai T, Nunoura Y, Yajima Y, Kawashima S, Tanaka K (2002) Dehydrotrametenolic acid induces preadipocyte differentiation and sensitizes animal models of noninsulin-dependent diabetes mellitus to insulin. For G. sylvestre it is 15 min–24 h, for Z. jujube it is 5–10 min and for H. dulcis it is 1–4 min (Suttisri et al. The objective of this review is to provide an update on the sources, pharmacological effects, structure–activity relationship, and clinical studies of anticancer triterpenoid saponins with a particular focus on the molecular mechanisms underlying their anticancer properties. Atherosclerosis 219:409–416, Wamil M, Seckl JR (2007) Inhibition of 11ß-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Triterpenes are considered the major active components in Centella asiatica (L.) Urb. 2000). Phytochemical investigation of the acetone extract from the roots of, Triterpenes are demonstrably effective for accelerating re-epithelialisation of wounds and known to improve scar formation for superficial lesions. Among the variety of triterpenes, betuline is of particular medical interest. 6) has been demonstrated for many semisynthetic (nanomolar value of IC50) and natural ursane and oleanane derivatives (Blum et al. The most active inhibitors of the enzyme were euscaphic acid and p-coumaroylursolic acid whose IC50 values were 0.67 and 0.62 mM, respectively, comparable with acarbose having an IC50 value of 0.79 mM (Kuang et al. 2007; Genet et al. However this distinction is not always adhered to in scientific literature, with the two terms triterpene and triterpenoid often being used interchangeably. in a study of “Analgesic and anti-nociceptive activity of hydroethanolic extract of Drymaria cordata Willd” by Barua CC, Roy JD, Buragohain B, Barua AG, Borah P, Lahkar M. (Source from.