Abstract
Oridonin belongs to ent-kaurane tetracyclic diterpenoid and was first isolated from Isodon species. It exhibits inhibitory activities against a variety of tumor cells, and pharmacological study shows that oridonin could inhibit cell proliferation, DNA, RNA and protein synthesis of cancer cells, induce apoptosis and exhibit an antimutagenic effect. In addition, the large amount of the commercially-available supply is also very important for the natural lead oridonin. Moreover, the good stability, suitable molecular weight and drug-like property guarantee its further generation of a natural-like compound library. Oridonin has become the hot molecule in recent years, and from the year 2010, more than 200 publications can be found. In this review, we summarize the synthetic medicinal chemistry work of oridonin from the first publication 40 years ago and share our research experience of oridonin for about 10 years, which may provide useful information to those who are interested in this research field.
Highlights
Oridonin (1, Figure 1) is an ent-kaurane diterpenoid isolated from Isodon of the Labiatae family, the structure and absolute configuration of which were first confirmed in the year 1970 [1]
The importance hydrogenofbond and the ester chain for the antitumor activity was demonstrated in the derivatives of oridonin; while the 1,14-diacetate derivative of oridonin could be obtained by theintreatment of oridonin with acetic in pyridine
Regioselective enone construction strategies were established. These derivatives significantly induced apoptosis and exhibited superior antitumor effects to oridonin against drug-resistant and aggressive breast cancer cells in vitro and in vivo (26 suppressed MDA-MB-231 xenograft tumor growth at 5.0 mg/kg) and exhibited low toxicity to normal human mammary epithelial cells
Summary
Oridonin (1, Figure 1) is an ent-kaurane diterpenoid isolated from Isodon of the Labiatae family, the structure and absolute configuration of which were first confirmed in the year 1970 [1]. Oridonin is a good lead in the field of medicinal chemistry: (a) it shows antitumor activities against many tumor-related cells [2,3] (e) there are many functional (double bond,groups carbonyl groupbond, and hydroxyl from lead to drug-like candidate (e) theregroups are many functional (double carbonyl groupsand in different chemical which provide good synthetic to efficiently group hydroxyl groupsenvironments), in different chemical environments), whichaccessibility provide good synthetic generate libraries of derivatives; andlibraries (f) last, of butderivatives; not least, for all (f) natural products, it isfor commercially accessibility to efficiently generate and last, but not least, all natural available for compound supply.
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