Two new diterpenoids from the stems of Rhododendron dauricum as GABAA receptor agonists

Abstract Two new diterpenoids, dauricumins A (1) and B (2), together with two known aromatic meroterpenoids (3 and 4), were isolated from the petroleum ether soluble fraction of the stems from Rhododendron dauricum through an HPLC-MS-SPE-NMR combination strategy. The absolute configurations of 1 and 2 were elucidated by ECD calculations and [Rh2 (OCOCF3)4]-induced CD spectrum analysis. In a membrane potential FLIPR assay, confluentin (4) showed an agonistic effect on GABAA receptor (EC50 = 20 µM).

[1]  Shishan Yu,et al.  Three new antinociceptive diterpenoids from the roots of Rhododendron micranthum , 2020, Journal of Asian natural products research.

[2]  Haibo Yu,et al.  Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABAA1 receptor with potent anticonvulsant activity and low toxicity. , 2019, European journal of medicinal chemistry.

[3]  Lisa M Sagardia,et al.  147 , 2019, Critical Care Medicine.

[4]  Yu-huan Li,et al.  Minor Nortriterpenoids from the Twigs and Leaves of Rhododendron latoucheae. , 2018, Journal of natural products.

[5]  D. Lu,et al.  Antinociceptive Diterpenoids from the Leaves and Twigs of Rhododendron decorum. , 2018, Journal of natural products.

[6]  H. Lv,et al.  Antinociceptive Grayanoids from the Roots of Rhododendron molle. , 2015, Journal of natural products.

[7]  Jia Li,et al.  Two Enantiomeric Pairs of Meroterpenoids from Rhododendron capitatum. , 2015, Organic letters.

[8]  S. C. Taneja,et al.  New natural compounds from Rhododendron lepidotum , 2013, Natural product research.

[9]  B. Kopp,et al.  The genus Rhododendron: an ethnopharmacological and toxicological review. , 2013, Journal of ethnopharmacology.

[10]  K. Gao,et al.  Chemical Constituents of Plants from the Genus Rhododendron , 2011, Chemistry & biodiversity.

[11]  S. Kitanaka,et al.  Tetracyclic chromane derivatives from Rhododendron anthopogonoides. , 2010, Journal of natural products.

[12]  L. Kong,et al.  Flavonol glycosides with α-D-aldohexoses from Rhododendron irroratum , 2010, Natural product research.

[13]  T. Liljefors,et al.  GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic. , 2004, Biochemical pharmacology.

[14]  X. Yao,et al.  Structures and histamine release inhibitory effects of prenylated orcinol derivatives from Rhododendron dauricum. , 2004, Journal of natural products.