Inhibition of [ 3 H]ponasterone A binding by ecdysone agonists in the intact Sf-9 cell line
Steroids, ISSN: 0039-128X, Vol: 65, Issue: 9, Page: 537-542
2000
- 55Citations
- 16Captures
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Metrics Details
- Citations55
- Citation Indexes55
- 55
- CrossRef54
- Captures16
- Readers16
- 16
Article Description
Ecdysone agonists, including dibenzoylhydrazines, significantly inhibited the binding of [ 3 H]ponasterone A ([ 3 H]PoA) in intact Sf-9 cells ( Spodoptera frugiperda ). The amount of [ 3 H]PoA binding varied in a concentration-dependent manner. According to the IC 50, concentration at which there is 50% inhibition, the order of potency of typical ecdysone agonists is tebufenozide (RH-5992) > methoxyfenozide (RH-2485) > PoA > 20-hydroxyecdysone > cyasterone > RH-5849, makisterone A ≥ inokosterone > ecdysone. The ranking is consistent with that obtained from a cultured integument system of the rice stem borer Chilo suppressalis except for methoxyfenozide. Other compounds whose modes of action are different from that of ecdysteroids, for example respiration inhibitors, plant steroid hormones, and chitin synthesis inhibitors, did not inhibit the binding of [ 3 H]PoA significantly. The mammalian hormones estradiol and diethylstilbestrol, and a secondary bile acid, lithocholic acid, significantly inhibited the binding of [ 3 H]PoA at 25 μM. However, their binding activity in terms of pIC 50 was either very low or not evaluated.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0039128X00001306; http://dx.doi.org/10.1016/s0039-128x(00)00130-6; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=0033817710&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/10978733; http://linkinghub.elsevier.com/retrieve/pii/S0039128X00001306; http://api.elsevier.com/content/article/PII:S0039128X00001306?httpAccept=text/xml; http://api.elsevier.com/content/article/PII:S0039128X00001306?httpAccept=text/plain; https://linkinghub.elsevier.com/retrieve/pii/S0039128X00001306; http://dx.doi.org/10.1016/s0039-128x%2800%2900130-6; https://dx.doi.org/10.1016/s0039-128x%2800%2900130-6
Elsevier BV
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