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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 oridonin fluorescent probe 33.
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ijms-17-01395-f016: The oridonin fluorescent probe 33.

Mentions: Early in this year, a series of oridonin fluorescent probes linked with coumarin moieties were designed and synthesized to explore the anticancer mechanism by our research group (Figure 16) [27]. Most of the probe molecules displayed optimal antiproliferative activity and a fluorescent property. Fluorescence microscopy and confocal imaging studies were examined by using typical probes. The results indicated that oridonin fluorescent probe 33 could be rapidly taken up into tumor cells, and the mitochondrion was the main site where it accumulated. Moreover, we confirmed that the α,β-unsaturated ketone group is the active moiety, which is crucial to its cytotoxicity, localization and uptake. The studies on mitochondrial physiology suggested that the mitochondrion-related pathway was involved in oridonin-induced apoptosis, and cytochrome c played an important role. These results provide new insights into the cellar mechanism of oridonin and may be useful to study the insight of the anticancer action and the targets of other ent-kaurane diterpenoids.


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
The oridonin fluorescent probe 33.
© Copyright Policy
Related In: Results  -  Collection

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

ijms-17-01395-f016: The oridonin fluorescent probe 33.
Mentions: Early in this year, a series of oridonin fluorescent probes linked with coumarin moieties were designed and synthesized to explore the anticancer mechanism by our research group (Figure 16) [27]. Most of the probe molecules displayed optimal antiproliferative activity and a fluorescent property. Fluorescence microscopy and confocal imaging studies were examined by using typical probes. The results indicated that oridonin fluorescent probe 33 could be rapidly taken up into tumor cells, and the mitochondrion was the main site where it accumulated. Moreover, we confirmed that the α,β-unsaturated ketone group is the active moiety, which is crucial to its cytotoxicity, localization and uptake. The studies on mitochondrial physiology suggested that the mitochondrion-related pathway was involved in oridonin-induced apoptosis, and cytochrome c played an important role. These results provide new insights into the cellar mechanism of oridonin and may be useful to study the insight of the anticancer action and the targets of other ent-kaurane diterpenoids.

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.