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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 1- or/and 14-position modified oridonin derivatives (31 and 32) with antibacterial activity.
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ijms-17-01395-f015: The 1- or/and 14-position modified oridonin derivatives (31 and 32) with antibacterial activity.

Mentions: From 2014–2016, the antibacterial activity of 1- or/and 14-position modified oridonin derivatives (31) was evaluated (Figure 15) [29,31,32]. Some derivatives were screened against Mycobacterium marinum, Mycobacterium smegmatis and Mycobacterium phlei. Among them, the compounds containing the trans-cinnamic acid moiety showed the most potent inhibitory activity against M. phlei with MICs of 0.5 μg/mL, and the SARs were analyzed. Five compounds were tested against Mycobacterium tuberculosis H37Rv based on the preliminary screening results. Among them, Compound 32 showed an IC50 value of 17.1 μg/mL. The antibacterial activity of some derivatives against Escherichia coli, Staphylococcus aureus, Bacillus subtilis and Monilia albicans was evaluated for the first time. Most of them showed good antibacterial activity against Gram-positive bacteria B. subtilis and S. aureus. Additionally, no obvious inhibitory activity was observed against Gram-negative bacterium E. coli and fungus M. albicans (MIC > 100 μg/mL).


Oridonin, a Promising ent -Kaurane Diterpenoid Lead Compound
The 1- or/and 14-position modified oridonin derivatives (31 and 32) with antibacterial activity.
© Copyright Policy
Related In: Results  -  Collection

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

ijms-17-01395-f015: The 1- or/and 14-position modified oridonin derivatives (31 and 32) with antibacterial activity.
Mentions: From 2014–2016, the antibacterial activity of 1- or/and 14-position modified oridonin derivatives (31) was evaluated (Figure 15) [29,31,32]. Some derivatives were screened against Mycobacterium marinum, Mycobacterium smegmatis and Mycobacterium phlei. Among them, the compounds containing the trans-cinnamic acid moiety showed the most potent inhibitory activity against M. phlei with MICs of 0.5 μg/mL, and the SARs were analyzed. Five compounds were tested against Mycobacterium tuberculosis H37Rv based on the preliminary screening results. Among them, Compound 32 showed an IC50 value of 17.1 μg/mL. The antibacterial activity of some derivatives against Escherichia coli, Staphylococcus aureus, Bacillus subtilis and Monilia albicans was evaluated for the first time. Most of them showed good antibacterial activity against Gram-positive bacteria B. subtilis and S. aureus. Additionally, no obvious inhibitory activity was observed against Gram-negative bacterium E. coli and fungus M. albicans (MIC > 100 μg/mL).

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.