Chemical profiling of root bark extract from Oplopanax elatus and its in vitro biotransformation by human intestinal microbiota

Oplopanax elatus (Nakai) Nakai, in the Araliaceae family, has been used in traditional Chinese medicine (TCM) to treat diseases as an adaptogen for thousands of years. This study established an ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC-Q-TOF/MS) method to identify chemical components and biotransformation metabolites of root bark extract from O. elatus. A total of 18 compounds were characterized in O. elatus extract, and 62 metabolites by human intestinal microbiota were detected. Two polyynes, falcarindiol and oplopandiol were recognized as the main components of O. elatus, whose metabolites are further illustrated. Several metabolic pathways were proposed to generate the detected metabolites, including methylation, hydrogenation, demethylation, dehydroxylation, and hydroxylation. These findings indicated that intestinal microbiota might play an essential role in mediating the bioactivity of O. elatus.

Sesquiterpenes From Oplopanax elatus Stems and Their Anti-Photoaging Effects by Down-Regulating Matrix Metalloproteinase-1 Expression via Anti-Inflammation

In the process of continuing to investigate ultraviolet b (UVB) irradiation protective constituents from Oplopanax elatus stems, nine new sesquiterpenes, named as eurylosesquiterpenosides A–D (1–4), eurylosesquiterpenols E–I (5–9), and ten known ones (10–19) were gained. Their structures were established by analysis of their NMR spectroscopic data, and electronic circular dichroism calculations were applied to define their absolute configurations. In addition, UVB induced HaCaT cells were used to study their anti-photoaging activities and mechanism. The results consolidated that compounds 7, 11, and 14 could improve the survival rate of HaCaT cells in concentration dependent manner at 10, 25, and 50 μM. Furthermore, western blot assay suggested that all of them could inhibit the expression of matrix metalloproteinase-1 (MMP-1), and increase the level of type I collagen markedly. Compounds 11 and 14 could reduce the phosphorylation of extracellular signal-regulated kinase and p38, respectively. Besides, compounds 7, 11, and 14 could significantly down-regulate the expression of inflammation related protein, such as tumor necrosis factor-α and cyclooxygenase-2, which indicated that they played anti-photoaging activities by reducing MMP-1 expression via down-regulating the production of inflammatory mediators and cytokines in UVB-induced HaCaT cells.

Total saponins from Oplopanax elatus Nakai: An optimization study of the extraction process using response surface methodology and its psychopharmacological activities

Background: Oplopanax elatus Nakai is an ancient angiosperm plant member. It belongs to the Araliaceae family and has biological activities similar to those of Panax ginseng. However, the psychopharmacological effects of O. elatus Nakai have not been characterized. Thus, in the present study, we determined the optimal process for extracting total saponins and then screened the psychopharmacological activities of O. elatus Nakai extract (ONE).Methods: A three-level Box-Behnken design with 3 variables was used to evaluate the treatment variables that influenced the total saponin content (TSC) extracted from O. elatus Nakai. ONE was orally administered to mice and drosophila to evaluate its psychomotor, sedative-hypnotic, anti-stress, and anxiolytic effects.Results: The optimal variables for ethanol extraction were 60 min, 70% ethanol, 30 g/mL and 80 °C, and the total saponin yield reached 18.06±0.17%. Treatment with ONE extended cold swimming endurance time, reduced anxiety-like behaviour, decreased spontaneous locomotor activity, prolonged sleep duration, and ameliorated the sleep-wake rhythm. The ginseng extract (GE) is characterized by low-dose excitation and high-dose inhibition of the central nervous system.Conclusion: Some of the properties of ONE and GE were not identical, but ONE has potentially psychopharmacological activities.

RESEARCH OF NEW PHYTOADAPTOGENS AND POSSIBILITIES OF HERBAL FORMULAS APPLICATION

Classic phytoadaptogens (Panax ginseng, Rhodiola rosea, Aralia mandshurica, Oplopanax elatus, Eleutherococcus senticosus, Leuzea carthamoides, Schisandra chinensis) have a complex protective effects, increasing the antitumor control of organisms. However, resistance to some adaptogens can develop. Therefore, the elaboration of multicomponent phytoadaptogen complexes based on the principle of a rational combination of complementary biologically active substances are relevant and scientifically significant. The use of several adaptogens in the herbal formula considers the absence of the organisms resistance. The review presents Russian and foreign studies devoted to the search for potential phytoadaptogens, as well as the development of complexes based on them. The possibility of regulating the protective systems of organism by components of phytoextracts with different points of pharmacological action has been shown. The advantages of multicomponent phytomixtures in comparison with individual adaptogens are substantiated. The many-sided experimental in vitro and in vivo investigations of Russian herbal formula are colligated. Its clinical application has been demonstrated in relation to a benign tumour, precancerous disease, advanced cancer process, and neurodegenerative pathology. The prospects of using the herbal formula preparations as a part of integrative medicine including oncological and age-related pathologies are shown.