Limits...
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.


Spirolactone-type 6,7-seco-kaurane diterpenoid derivatives 43 and 44.
© Copyright Policy
Related In: Results  -  Collection

License
getmorefigures.php?uid=PMC5037675&req=5

ijms-17-01395-f022: Spirolactone-type 6,7-seco-kaurane diterpenoid derivatives 43 and 44.

Mentions: The spirolactone-type 6,7-seco-ent-kaurane diterpenoid derivatives (43) were also obtained from commercial-available oridonin (Figure 22) [34,37]. These derivatives showed improved antiproliferative activity against a panel of human cancer cell lines, and some of them were more potent than the positive control Taxol. For example, the most potent Compound 44 with chloro substitution at the ortho-position of the benzene ring showed IC50 values of 0.39, 1.28, 0.60 and 1.39 μM against K562, MGC-803, CaEs-17 and Bel-7402 cells, which were 11.2-, 3.4-, 17.4- and 4.3-fold stronger than oridonin, correspondingly. The cellular mechanisms showed that Compound 44 could induce apoptosis at low micromolar concentrations in human hepatoma Bel-7402 cells.


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
Spirolactone-type 6,7-seco-kaurane diterpenoid derivatives 43 and 44.
© Copyright Policy
Related In: Results  -  Collection

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

ijms-17-01395-f022: Spirolactone-type 6,7-seco-kaurane diterpenoid derivatives 43 and 44.
Mentions: The spirolactone-type 6,7-seco-ent-kaurane diterpenoid derivatives (43) were also obtained from commercial-available oridonin (Figure 22) [34,37]. These derivatives showed improved antiproliferative activity against a panel of human cancer cell lines, and some of them were more potent than the positive control Taxol. For example, the most potent Compound 44 with chloro substitution at the ortho-position of the benzene ring showed IC50 values of 0.39, 1.28, 0.60 and 1.39 μM against K562, MGC-803, CaEs-17 and Bel-7402 cells, which were 11.2-, 3.4-, 17.4- and 4.3-fold stronger than oridonin, correspondingly. The cellular mechanisms showed that Compound 44 could induce apoptosis at low micromolar concentrations 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.