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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.


Antimycobacterial enmein-type 6,7-seco-kaurane diterpenoid derivatives 37–40.
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ijms-17-01395-f020: Antimycobacterial enmein-type 6,7-seco-kaurane diterpenoid derivatives 37–40.

Mentions: The antimycobacterial activity of some enmein-type 6,7-seco-kaurane diterpenoid derivatives (35) was also evaluated [31,32]. Most of the derivatives showed antimycobacterial activity against M. phlei, of which Compounds 37–39 (Figure 19) exhibited the strongest activity with MIC of 0.5 μg/mL and were 15-fold stronger than that of oridonin (8 μg/mL). The trans-cinnamic acid moiety benefitted the antimycobacterial activity. Compounds 38 and 40 (Figure 20) also showed moderate antitubercular activity against M. tuberculosis H37Rv with MICs of 28.8 and 24.0 μg/mL, respectively. These findings could provide new insights into the development of novel antitubercular agents from enmein-type 6,7-seco-kaurane diterpenoid derivatives.


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
Antimycobacterial enmein-type 6,7-seco-kaurane diterpenoid derivatives 37–40.
© Copyright Policy
Related In: Results  -  Collection

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

ijms-17-01395-f020: Antimycobacterial enmein-type 6,7-seco-kaurane diterpenoid derivatives 37–40.
Mentions: The antimycobacterial activity of some enmein-type 6,7-seco-kaurane diterpenoid derivatives (35) was also evaluated [31,32]. Most of the derivatives showed antimycobacterial activity against M. phlei, of which Compounds 37–39 (Figure 19) exhibited the strongest activity with MIC of 0.5 μg/mL and were 15-fold stronger than that of oridonin (8 μg/mL). The trans-cinnamic acid moiety benefitted the antimycobacterial activity. Compounds 38 and 40 (Figure 20) also showed moderate antitubercular activity against M. tuberculosis H37Rv with MICs of 28.8 and 24.0 μg/mL, respectively. These findings could provide new insights into the development of novel antitubercular agents from enmein-type 6,7-seco-kaurane diterpenoid derivatives.

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.