Planta Medica International Open 2017; 4(S 01): S1-S202
DOI: 10.1055/s-0037-1608579
Lecture Session – Natural Products Formulation
Georg Thieme Verlag KG Stuttgart · New York

NeoSolTMRCL40 is a novel Red Clover isoflavone aglycones extract preparation with improved solubility and increased availability of active compounds

M Cosentino
1   Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy
,
F Marino
1   Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy
,
E Rasini
1   Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy
,
R Bombelli
1   Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy
,
A Luini
1   Center for Research in Medical Pharmacology, University of Insubria, Varese, Italy
,
B Pacchetti
2   Linnea SA, Riazzino, TI, Switzerland
› Author Affiliations
Further Information

Publication History

Publication Date:
24 October 2017 (online)

 

Red clover (Trifolium pratense L, Fabaceae; RCL), a perennial plant rich in isoflavones, is a natural alternative for menopausal symptoms, as well as antiaging and antioxidant. Isoflavone preparations usually contain aglycones and β-glycosides. Aglycones, the active moieties, are absorbed slowly and unevenly due to reduced water solubility and biotransformation from β-glycosides. NeoSolTMRCL40 is a novel RCL isoflavone aglycones preparation based on active solubilization technologies [1].

Using in vitro models, we evaluated NeoSolTMRCL40-induced isoflavones solubilization, estrogenic and antioxidative effects in comparison to a standard RCL extract (RCLE).

Isoflavones aglycones, either as RCLE or as NeoSolTMRCL40, were dissolved in water (100 mg/50 mL). Total aglycones in solution, assayed by HPLC [2], were (mean ± SD) 0.009476 ± 0.001202 mg/ml with RCLE and 0.047401 ± 0.005760 mg/ml with NeoSolTMRCL40 (n = 11 – 13, P < 0.0001). Estrogenicity, assessed in MCF-7 cells [2], was: potency (EC50, mean dilution x 1000 [95% CI]) 1.237 (0.981 – 1.558) with RCLE and 0.361 (0.248 – 0.527) with NeoSolTMRCL40, and efficacy (EMAX, % of response to estradiol 0.1 nM) 116.0% (104.6 – 127.3%) with RCLE and 110.6% (98.2 – 123.0%) with NeoSolTMRCL40. NeoSolTMRCL40 was more antioxidant than RCLE (FRAP assay: 660.4 ± 51.3 vs. 328.3 ± 46.3µM FeSO4 equivalents, n = 6, P < 0.0001; DPPH assay: 69.6 ± 5.3 vs. 84.2 ± 3.3 arbitrary units, n = 5, P = 0.0001) [3].

Results support the ability of NeoSolTMRCL40 to promote isoflavones solubilization and availability. The ratio NeoSolTMRCL40/RCLE for isoflavones solubilization was 5.0 and NeoSolTMRCL40 had 3.4-fold higher estrogenic potency and was more antioxidant than RCLE. NeoSolTMRCL40 is therefore an interesting novel preparation providing improved availability of active isoflavones aglycones.

[1] Cram DJ. Science 1988; 240: 760 – 767

[2] Spagnuolo P, et al. Fitoterapia 2014; 94: 62 – 69

[3] Cosentino M, et al. Pharmacol Res 2007; 56: 140 – 147