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Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound

View Article: PubMed Central - PubMed

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.

No MeSH data available.


Natural spirolactone- and enmein-type 6,7-seco-kaurane diterpenoids.
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ijms-17-01395-f018: Natural spirolactone- and enmein-type 6,7-seco-kaurane diterpenoids.

Mentions: 6,7-seco-ent-Kaurane diterpenoid derivatives (including enmein- and spirolactone-type 6,7-seco-ent-kaurane diterpenoids) showed stronger cytotoxicity than oridonin. These compounds also have more complex structures (Figure 18) and are more difficult to isolate from natural sources [74,75,76,77,78,79]. We used oridonin as the starting material to semi-synthesize enmein- and spirolactone-type core structures by the ring-opening reaction between C-6 and C-7. A compound library containing more than 100 enmein- and spirolactone-type diterpenoid derivatives was built up mainly by our research group for further medicinal study.


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
Natural spirolactone- and enmein-type 6,7-seco-kaurane diterpenoids.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC5037675&req=5

ijms-17-01395-f018: Natural spirolactone- and enmein-type 6,7-seco-kaurane diterpenoids.
Mentions: 6,7-seco-ent-Kaurane diterpenoid derivatives (including enmein- and spirolactone-type 6,7-seco-ent-kaurane diterpenoids) showed stronger cytotoxicity than oridonin. These compounds also have more complex structures (Figure 18) and are more difficult to isolate from natural sources [74,75,76,77,78,79]. We used oridonin as the starting material to semi-synthesize enmein- and spirolactone-type core structures by the ring-opening reaction between C-6 and C-7. A compound library containing more than 100 enmein- and spirolactone-type diterpenoid derivatives was built up mainly by our research group for further medicinal study.

View Article: PubMed Central - PubMed

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.

No MeSH data available.