Triterpenoids antitumor activity

Other common plant-derived triterpenoid acids, such as oleanolic and ursolic acid, exhibit weak antiinflammatory and antitumor activities, and studies have been directed at the synthesis of new analogues having increased potencies. These studies have led to the synthesis of 2-cyano-3,12-dioxoolean-l,9-dien-28-oic acid (CDDO) (54) and its methyl ester (55), which exhibit potent in vitro and in vivo antitumor activity against a wide range of tumors, including breast and pancreatic carcinomas and leukemias. ... 

In the course of these research programmes, many characteristic bioactive compounds have been reported. Polyester sesquiterpenes and pyridine-sesquiterpene alkaloids with insect antifeedant or insecticidal properties have been isolated from some species and recently sesquiterpene pyridine alkaloids with immunosuppressive or antitumoral activities have also been described. Diterpene triepoxides with potent antileukemic and immunosupressive activities and triterpenoid quinonemethides, named as celastroloids , with antibiotic and cytostatic activities, have been isolated from species of the Celastraceae family. 

Cycloartane triterpenoids are interesting not only because of the fundamental biogenesis issues. The wide variety of structures makes them attractive as subjects for chemical modification. At the same time this compounds possess abroad spectrum of biological activity. It is noteworthy that some representatives of this class have hypolipidemic, hypotensive, diuretic, anti-inflammatory, sedative, analgesic, immunosti-mulating, and cardiotonic activity. Moreover, several compounds have antiviral and antitumor activity, and interferon inducers were found among them. 

Wu, Q., Wang, Y, Guo, M. Triterpenoid Saponins from the seeds of Celosiae argentea and their anti-infahnmatory and antitumor activities. Chem. Pharm. Bull. 59(5), 666-671 (2011)... 

ANTITUMOR-PROMOTING AND ANTIINFLAMMATORY ACTIVITIES OF TRITERPENOIDS AND STEROLS FROM PLANTS AND FUNGI... 

As discussed in the previous sections, a number of triterpenoids with great structural diversity have antitumor-promoting activities. In contrast, 28-deacetylbelamcandal (288), a spiroiridal-type triterpenoid, has recently been reported to possess tumor promoting activity [92]. Compound 288, which stimulated differentiation of human promyelocytic leukemia (HL-60) cells (a fast method for screening TPA-type tumor promoters),... 

The concept that inflammation and carcinogenesis are related phenomena has been the subject of many studies that have attempted to link these two processes in a mechanistic fashion [94-99]. In connection with this, as is evident in some triterpenoids such as oleanolic acid (142), glycyrrhetic acid (147), and ursolic acid (210) in Table 2, those possessing anti-inflammatory activity in various experimental models exhibited antitumor-promoting activity as well. This suggests that most of the other anti-inflammatory triterpenoids and sterols listed in Table 2 might have antitumor-promoting properties which have not been evaluated, yet. 

Tiiterpenoid saponin exists widely in plants of Araliaceae, Campanulaceae, Polygalaceae, Leguminosae, Umbelliferae, etc. Tiiterpenoid saponin is consisted of triteipenoid sapogenins and saccharide chain. Tetracyclic and pentacyclic triteipenoid saponins are very common and showed extensive activity on immune system, cardiovascular system, even with antitumor effect. They have long been under study to elucidate their activity and mechanism, new structural compounds, and develop rapid and accurate analytical methods. The isolation of triterpenoid saponins is tedious due to their high polarity, and so is the structure identification due to the presence of more than three monosaccharides. New analytical tools and approaches have been developed for qualitative and quantitative analysis of triteipenoid saponins in food, medicinal plant and health care products. This chapter describes spectrophotometry, mass spectrometry, and chromatography coupled with different detector for triterpenoid saponin analysis in matrix. 

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