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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.


Enmein-type 6,7-seco-kaurane diterpenoid derivatives 35 and 36.
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ijms-17-01395-f019: Enmein-type 6,7-seco-kaurane diterpenoid derivatives 35 and 36.

Mentions: Several series of ester derivatives (35) of enmein-type diterpenoid at 14-O were synthesized from commercially-available oridonin by efficient and practical synthetic methods (Figure 19) [33,36]. The antiproliferative activity was evaluated against a set of human cancer cell lines. Some derivatives showed even smaller IC50 values than positive control paclitaxel. The apoptotic properties of the selected Compound 36 (IC50 = 0.71 μM) in human hepatocarcinoma Bel-7402 cells were evaluated. It caused cell-cycle arrest at the G2/M phase and induced apoptosis. Moreover, Compound 36 exhibited potent antitumor activity in vivo in MGC-803 mice. These results warranted further preclinical investigations of these enmein-type diterpenoid derivatives as potential anticancer agents.


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
Enmein-type 6,7-seco-kaurane diterpenoid derivatives 35 and 36.
© Copyright Policy
Related In: Results  -  Collection

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

ijms-17-01395-f019: Enmein-type 6,7-seco-kaurane diterpenoid derivatives 35 and 36.
Mentions: Several series of ester derivatives (35) of enmein-type diterpenoid at 14-O were synthesized from commercially-available oridonin by efficient and practical synthetic methods (Figure 19) [33,36]. The antiproliferative activity was evaluated against a set of human cancer cell lines. Some derivatives showed even smaller IC50 values than positive control paclitaxel. The apoptotic properties of the selected Compound 36 (IC50 = 0.71 μM) in human hepatocarcinoma Bel-7402 cells were evaluated. It caused cell-cycle arrest at the G2/M phase and induced apoptosis. Moreover, Compound 36 exhibited potent antitumor activity in vivo in MGC-803 mice. These results warranted further preclinical investigations of these enmein-type diterpenoid derivatives as potential anticancer agents.

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.