Integrated Phytochemical Analysis Based on UPLC–MS/MS and Network Pharmacology Approaches to Explore the Effect of Odontites vulgaris Moench on Rheumatoid Arthritis

Odontites vulgaris Moench has the effect of clearing away heat, detoxification, dispelling wind, and clearing dampness. In this study, the potential anti-inflammatory compounds of O. vulgaris were investigated using ultra-high-performance liquid chromatography–mass spectrometry (UPLC–MS/MS) combined with the network pharmacology approach and further confirmed on an LPS-activated RAW 264.7 macrophage model. Monomer compounds were prepared from the active fraction using modern advanced separation and purification methods. UPLC–Q-Exactive HRMS was used to identify the chemical compounds in the active fractions of O. vulgaris. D-mannitol, geniposidic acid, salidroside, shanzhiside methyl ester, eleutheroside B, geniposide, 7,8-dihydroxycoumarin, gardoside methyl ester, arenarioside, vanillic acid, p-hydroxy-cinnamic acid, melampyroside, syringaresinol, tricin, and diosmetin were isolated from O. vulgaris for the first time. A compound database of O. vulgaris was established based on the existing literature to predict the mechanism of O. vulgaris in the treatment of rheumatoid arthritis. The results suggest that the PI3K-Akt pathway mediates O. vulgaris and deserves more attention in the treatment of RA. Finally, the anti-rheumatoid arthritis effects of the four target compounds were validated with the decreased levels of NO, TNF-α, IL-6 and IL-1β in RAW 264.7 macrophage cells treated with LPS. The present study explored the potential targets and signaling pathways of O. vulgaris in the treatment of RA, which may help to illustrate the mechanisms involved in the action of O. vulgaris and may provide a better understanding of the relationship between O. vulgaris and RA. This study provides novel insights into the development of new drugs and utilization of Mongolian traditional Chinese medicine resources.

Tissue-Specific Metabolic Response of Acanthopanax Senticosus (Rupr. Et. Maxim.) Harms Leaf To UV-B radiation

This study aims to evaluate the effects of medium and high UV-B radiation on leaves of Acanthopanax senticosus (Rupr. et. Maxim.) Harms. Two-year-old potted A. senticosus plant samples were respectively exposed to two levels of artificial, biologically effective UV-B radiation under glasshouse-controlled conditions: 1.972KJ/m2 and 3.442KJ/m2. Ordinary sunlight treatment was included as a control group, in which major effects of UV-B were observed. It was discovered that UV-B enhanced the medicinal value (especially eleutheroside B and E) of A. senticosus but impaired its growth. The sensitivity of leaves to UV-B radiation varied across different parts of the plant, among which the upper leaves responded most strongly. Furthermore, multiple types of phenolic compounds are synergistically involved in stress resistance in different aspects, including up-regulation of UV-absorbing substances (C6C3C6-type, kaempferol and rutin) and antioxidant enzyme synergists (C6C1-type, salicylic acid) as well as down-regulation of antioxidants (C6C3-type, p-coumaric acid). Conclusion of this study may provide a new perspective to improve the exploitation of A. senticosus.

Pharmacognostic Evaluation and HPLC–PDA and HS–SPME/GC–MS Metabolomic Profiling of Eleutherococcus senticosus Fruits

Eleutherococcus senticosus (Rupr. et Maxim.) Maxim. is a medicinal plant used in Traditional Chinese Medicine (TCM) for thousands of years. However, due to the overexploitation, this species is considered to be endangered and is included in the Red List, e.g., in the Republic of Korea. Therefore, a new source of this important plant in Europe is needed. The aim of this study was to develop pharmacognostic and phytochemical parameters of the fruits. The content of polyphenols (eleutherosides B, E, E1) and phenolic acids in the different parts of the fruits, as well as tocopherols, fatty acids in the oil, and volatile constituents were studied by the means of chromatographic techniques [HPLC with Photodiode-Array Detection (PDA), headspace solid-phase microextraction coupled to gas chromatography-mass spectrometry (HS–SPME/GC–MS)]. To the best of our knowledge, no information is available on the content of eleutherosides and phenolic acids in the pericarp and seeds. The highest sum of eleutheroside B and E was detected in the whole fruits (1.4 mg/g), next in the pericarp (1.23 mg/g) and the seeds (0.85 mg/g). Amongst chlorogenic acid derivatives (3-CQA, 4-CQA, 5-CQA), 3-CQA was predominant in the whole fruits (1.08 mg/g), next in the pericarp (0.66 mg/g), and the seeds (0.076 mg/g). The oil was rich in linoleic acid (C18:3 (n-3), 18.24%), ursolic acid (35.72 mg/g), and α-tocopherol (8.36 mg/g). The presence of druses and yellow oil droplets in the inner zone of the mesocarp and chromoplasts in the outer zone can be used as anatomical markers. These studies provide a phytochemical proof for accumulation of polyphenols mainly in the pericarp, and these structures may be taken into consideration as their source subjected to extraction to obtain polyphenol-rich extracts.

Eleutheroside-b and e in Acanthopanax Senticosus has Anti-PRV Activity via an Enhanced Body Immune Response in Vivo

BackgroundAcanthopanax senticosus extract (Eleutheroside-b and e, Acanthopanax senticosus extract, AS) is a multi-functional medicine involving in antiviral response in rodents and humans. Pseudorabies virus (PRV) is essential pathogens especially in swine farms. However, little is known about the biological functions of AS in vivo during PRV infection. MethodsIn order to confirm function of AS during PRV infection in vivo. We investigated that AS treatment (2mg/g, 4mg/g and 6mg/g) mice for 5 days affecting the mouse survival time during PRV infection. Furthermore, we investigated that AS treatment (4mg/g) mice for 1 day, 3 days and 5 days, respectively, affected the mouse survival time during PRV infection. We then treated mice with AS (4 mg/g) for 5 days and then challenged with PRV. Three days after PRV infection, we harvested mouse-samples to analyze PRV copies, performed pathological and immunohistochemical assays and the expression of immune-genes.ResultsWe found that AS treatment decreased the PRV copies and degree of pathological damage in mice brains and lungs. The AS treatment also stimulated a high level of IFN-γ, IL-2, and CCL-5 in the rodent serum, but suppressed IL-10 expression, suggesting that AS enhances the immunity response. Conclusionswe showed that AS promoted the anti-PRV ability in vivo by activating the expression of immunity genes. In summary, these findings offer a novel understanding of the immunity response during PRV infection.

Extracts from Eleutherococcus senticosus (Rupr. et Maxim.) Maxim. Roots: A New Hope Against Honeybee Death Caused by Nosemosis

Pollinators, the cornerstones of our terrestrial ecosystem, have been at the very core of our anxiety. This is because we can nowadays observe a dangerous decline in the number of insects. With the numbers of pollinators dramatically declining worldwide, the scientific community has been growing more and more concerned about the future of insects as fundamental elements of most terrestrial ecosystems. Trying to address this issue, we looked for substances that might increase bee resistance. To this end, we checked the effects of plant-based adaptogens on honeybees in laboratory tests and during field studies on 30 honeybee colonies during two seasons. In this study, we have tested extracts obtained from: Eleutherococcus senticosus, Garcinia cambogia, Panax ginseng, Ginkgo biloba, Schisandra chinensis, and Camellia sinensis. The 75% ethanol E. senticosus root extract proved to be the most effective, both as a cure and in the prophylaxis of nosemosis. Therefore, Eleutherococcus senticosus, and its active compounds, eleutherosides, are considered the most powerful adaptogens, in the pool of all extracts that were selected for screening, for supporting immunity and improving resistance of honeybees. The optimum effective concentration of 0.4 mg/mL E. senticosus extract responded to c.a. 5.76, 2.56 and 0.07 µg/mL of eleutheroside B, eleutheroside E and naringenin, respectively. The effect of E. senticosus extracts on honeybees involved a similar adaptogenic response as on other animals, including humans. In this research, we show for the first time such an adaptogenic impact on invertebrates, i.e., the effect on honeybees stressed by nosemosis. We additionally hypothesised that these adaptogenic properties were connected with eleutherosides—secondary metabolites found exclusively in the Eleutherococcus genus and undetected in other studied extracts. As was indicated in this study, eleutherosides are very stable chemically and can be found in extracts in similar amounts even after two years from extraction. Considering the role bees play in nature, we may conclude that demonstrating the adaptogenic properties which plant extracts have in insects is the most significant finding resulting from this research. This knowledge might bring to fruition numerous economic and ecological benefits.

Antioxidant Activities of Ficus elastica Leaves Ethanol Extract and Its Compounds

Background: The excessive free radicals condition called oxidative stress can harmful for the body. To prevent and cure it, the antioxidant agents are required. Nowadays, the natural product extracted from plants have been widely used in folk medicine as antioxidant for the treatment of many diseases. Ficus elastica (rubber tree) has some compounds that has several biological activities, i.e., quercitrin, myricitrin, morin, and eleutheroside B. The F. elastica works against the free radicals and can be potential as antioxidant agent. The purpose of this study was to evaluate antioxidant properties of F. elastica ethanolic extract (FEE), quercitrin, myricitrin, morin, and eleutheroside B.Materials and Methods: The antioxidant activities of FEE and standard compounds were evaluated by free radical-scavenging activity of 2,2-diphenyl-1-picrylhydrazil (DPPH), hydrogen peroxide (H2O2), 2,2’-azinobis-(3-ethylbenzothiazoline- 6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) activities using spectrophotometry method.Results: FEE has the lowest of DPPH scavenging activity (IC50=13.82 µg/mL) than other compounds. In ABTS scavenging activity, FEE has moderate activity with IC50 value 23.29 µg/mL. In FRAP activity, FEE has moderate activity with value 241.58 µM Fe(II)/µg, while in H2O2 scavenging activity, FEE also show moderate activity with IC50=83.97 µg/mL compared to other compounds.Conclusion: In summary, FEE and the pure compounds (quercitrin, myricitrin, morin, and eleutheroside B) have potential as antioxidant agent.Keywords: free radical, morin, myricitrin, quercitrin, rubber tree, scavenging activities