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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.


The hybrid of oridonin and nitrogen mustard (29).
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ijms-17-01395-f013: The hybrid of oridonin and nitrogen mustard (29).

Mentions: In 2014, a series of oridonin and nitrogen mustard hybrids were designed and synthesized by Xu et al. to find more efficacious and less toxic antitumor agents (Figure 13) [30]. The antiproliferative activity of the hybrids was more potent than oridonin and the clinically used nitrogen mustards against four selected human cancer cell lines (Bel-7402, MCF-7, K562 and MGC-803). Some representative derivatives exhibited antiproliferative activities against the multidrug-resistant cell lines (NCI-H460/MX20 and SW620/AD300). The most effective compound (29) of this series showed strong inhibitory activity with an IC50 value (0.67 μM) 21-fold lower than that of oridonin (14.60 μM) against MCF-7 cells and also exhibited selective cytotoxicity toward different cancer cells. It was demonstrated to affect cell cycle progression and significantly induce apoptosis in human hepatoma Bel-7402 cells.


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
The hybrid of oridonin and nitrogen mustard (29).
© Copyright Policy
Related In: Results  -  Collection

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

ijms-17-01395-f013: The hybrid of oridonin and nitrogen mustard (29).
Mentions: In 2014, a series of oridonin and nitrogen mustard hybrids were designed and synthesized by Xu et al. to find more efficacious and less toxic antitumor agents (Figure 13) [30]. The antiproliferative activity of the hybrids was more potent than oridonin and the clinically used nitrogen mustards against four selected human cancer cell lines (Bel-7402, MCF-7, K562 and MGC-803). Some representative derivatives exhibited antiproliferative activities against the multidrug-resistant cell lines (NCI-H460/MX20 and SW620/AD300). The most effective compound (29) of this series showed strong inhibitory activity with an IC50 value (0.67 μM) 21-fold lower than that of oridonin (14.60 μM) against MCF-7 cells and also exhibited selective cytotoxicity toward different cancer cells. It was demonstrated to affect cell cycle progression and significantly induce apoptosis in human hepatoma Bel-7402 cells.

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.