Comparison of chemical profiles and effectiveness between Erxian decoction and mixtures of decoctions of its individual herbs : a novel approach for identification of the standard chemicals

Acknowledgements This study was partially supported by grants from the Seed Funding Programme for Basic Research (Project Number 201211159146 and 201411159213), the University of Hong Kong. We thank Mr Keith Wong and Ms Cindy Lee for their technical assistances.Peer reviewedPublisher PD

Sexual enhancement products for sale online : raising awareness of the psychoactive effects of Yohimbine, Maca, Horny Goat Weed and Ginkgo Biloba

Copyright © 2014 Ornella Corazza et al.This is an open access article distributed under theCreativeCommonsAttribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly citedIntroduction. The use of unlicensed food and herbal supplements to enhance sexual functions is drastically increasing. This phenomenon, combined with the availability of these products over the Internet, represents a challenge from a clinical and a public health perspective. Methods. A comprehensive multilingual assessment of websites, drug fora, and other online resources was carried out between February and July 2013 with exploratory qualitative searches including 203 websites. Additional searches were conducted using the Global Public Health Intelligence Network (GPHIN). Once the active constitutes of the products were identified, a comprehensive literature search was carried out using PsycInfo and PubMed. Results. The most common sexual enhancement products available on the Internet were identified. Their active ingredients included yohimbine, maca, horny goat weed and Ginkgo biloba. These four substances were reported with the occurrence of adverse events and the induction of psychological symptoms, such as mood changes, anxiety, and hallucinations as well as addictive behaviours. Conclusions. Uncontrolled availability of sexual enhancement products that contain potentially harmful substances is a major public healthconcern.Thepossible impact on population health, particularly among subjects with psychiatric disorders, usually at risk for sexual dysfunction, may be significant. This new trend needs to be extensively studied and monitoredPeer reviewedFinal Published versio

Enhancement of Icariin Aphrodisiac Effect by Solid-SNEDDS Method Using Shark Liver Oil Phase

The Epimedium brevicornu Maxim plant contains icariin, a flavonoid compound known for its aphrodisiac effects. However, icariin has low solubility and bioavailability. This study aims to find the best formula for S-SNEDDS icariin, its physical properties, characteristics, and aphrodisiac activity. Using the S-SNEDDS (Solid-Self Nanoemulsifying Drug Delivery System) method with shark liver oil phase is expected to increase the solubility and bioavailability of icariin. The optimum formula used is tween 80 (72.5%): PEG 400 (13.75%) and shark liver oil (13.75%). The optimal formula of S-SNEDDS icariin with the adsorption method to solid carriers requires aerosol 200 as much as 783±28.86mg per 1mL. S-SNEDDS icariin has characteristics with an average emulsification time of 12.88±0.26 seconds, transmittance value of 98.08±0.94%, droplet size 171.8±8.9 nm, zeta potential -35.2±1.1 mV, flow speed less than 10 seconds, resting angle 35.159°. The dissolution test of S-SNEDDS icariin is better than icariin instead of S-SNEDDS. S-SNEDDS icariin dose 50 mg/KgBW has a better aphrodisiac effect than pure icariin 100 mg/kgBW

Icariin stimulates differentiation of bone marrow-derived mesenchymal stem cells (BM-MSCs) through activation of cAMP/PKA/CREB

Icariin, a prenylated flavonol glycoside isolated from Epimedium, has been considered as a potential alternative therapy for osteoporosis. The present study aimed to clarify the detailed molecular mechanisms of action of icariin on osteoblast function, using bone marrow-derived mesenchymal stem cells (BM‑MSCs). BM-MSCs were first stimulated by icariin. Then, gene and protein expression of cAMP/ PKA/CREB signaling molecules were analyzed by RT-PCR and western blotting (WB), and alkaline phosphatase (ALP) was analyzed in cell lysates by ELISA. MTT assays indicated that icariin did not have significant effects on cell viability up to 1 μM. Icariin showed a dose-dependent effect on the alkaline phosphatase activity of BM-MSCs. WB analysis showed that icariin treatment of BM-MSCs significantly enhanced the protein expression of protein kinase A (PKA) and cAMP-responsive element binding protein (CREB), while RT-PCR results showed that icariin dose-dependently increased the mRNA levels of PKA and CREB. Icariin induced BM-MSC differentiation by BMP2, Smad1, and Runx2. RT‑PCR and WB results indicated that icariin significantly increased the expression of BMP2, Smad1, and Runx2 in BM‑MSCs. These results suggest that icariin is an agonist of the cAMP/PKA/CREB pathway in BM-MSC differentiation, raising the possibility that it could be used in the treatment of osteoporosis

Effects of icariin and quercetin on high glucose-induced neuronal cell apoptosis

Purpose: To study the effects of icariin and quercetin on cell apoptotic changes in neurons induced by elevated glucose condition, and the  mechanism involved. Methods: Neonatal male Sprague Dawley rats (n = 48) weighing 5 – 7 g were used. Neuronal cells were isolated from rat hippocampus and cultured after purification. The cells were randomly assigned to six groups: control, high glucose, icariin, quercetin, serine/threonine-specific protein kinase (Akt) inhibitor, and Akt agonist groups. The Akt inhibitor and agonist used in this study were MK-22062hci and SC79, respectively. The influence of icariin and quercetin on neuronal apoptotic changes were determined flow cytometrically, while their effects on levels of expression of Akt, p-Akt, bax and bcl-2 were determined with Western blotting. Results: Treatment with icariin or quercetin significantly inhibited apoptosis induced by high glucose. The concentrations of Akt, p-Akt, and bcl-2 proteins were markedly upregulated in high glucose group, relative to control (p < 0.05). The corresponding expression of bax was significantly down-regulated in high glucose group, relative to control (p < 0.05). Treatment with icariin or quercetin, or their agonists reversed high glucose-mediated alterations in these protein levels (p < 0.05). Conclusion: Icariin and quercetin inhibit neuronal cell apoptosis induced by high glucose through upregulation of bcl-2 expression and down- regulations of bax expression and Akt-induced protein phosphorylation. Thus, Icariin and quercetin possess potential benefits for the treatment of neurological diseases. Keywords: Apoptosis, High glucose condition, Hippocampal neurons, Icariin, Querceti

Effectiveness of Active Compounds of Herbal Plants as Aphrodisiacs Through Molecular Docking Against Human Phosphodiesterase-5 Receptors

Based on the evaluation of side effects the use of sildenafil as a human phosphodiesterase 5 inhibitor drug (HPDE5) has prompted the search for new compounds that have the potential to be aphrodisiacs. The purpose of this study was to determine the interaction of the active compounds nilocitin, stigmasterol, protodioscin, icariin, yohimbine, and ginsenoside against the HPDE5 receptor as an aphrodisiac. The method used in this study was experimental conducted in silico. The metabolite structure is downloaded from the PubChem application, the protein is downloaded from PDB (Protein Data Bank) with the code 2H42. The result of this study is that the active compound may interact with HPDE5 receptors. The interaction that occurs results in the formation of van der waals bonds, hydrogen, carbon hydrogen, sigma, sulfur cation anions, T-shape and alkyls. The active compounds each have a sildenafil bond energy of -9.5 kcal/mol; niloticin -7.8 kcal/mol; stigmasterol -10.7 kcal/mol; protodioscin -13.1 kcal/mol; icariin -11.1 kcal/mol; yohimbine -10.1 kcal/mol and ginsenoside -12.1 kcal/mol with RMSD 0. The interaction with the HPDE5 receptor results in the formation of the same amino acid residue as the comparison ligand. The residual equation shows that the compounds have the same activity and can be predicted as aphrodisiac

Icariin and its Derivative Icariside II Extend Healthspan via Insulin/IGF-1 Pathway in C. elegans

Compounds that delay aging might also postpone age-related diseases and extend healthspan in humans. Icariin is a flavonol extracted from several plant species of the Epimedium family. The icariin and its metabolic derivatives have been shown to exert wide protective effects in age-related diseases. However, whether icariin and its derivatives have the potency of delaying aging remains unclear. Here, we report that icariin and its derivative icariside II extend C. elegans lifespan. Using HPLC, we found high level of icariside II in the animals treated with icariin, suggesting icariside II is the bioactive form in vivo of icariin. Icariside II also increased the thermo and oxidative stress tolerance, slowed locomotion decline in late adulthood and delayed the onset of paralysis mediated by polyQ and Aβ1–42 proteotoxicity. The lifespan extension effect of icariside II is dependent on the insulin/IGF-1 signaling (IIS) since the daf-16(mu86) and daf-2(e1370) failed to show any lifespan extension upon icariside II treatment. Consistently, icariside II treatment upregulates the expression of DAF-16 targets in the wild-type. Moreover, our data suggests that the heat shock transcription factor HSF-1 has a role in icariside II-dependent lifespan extension further implicating the IIS pathway. In conclusion, we demonstrate a novel natural compound, icariside II as the bioactive form of icariin, extends the healthspan via IIS pathway in C. elegans

Icariin induces autophagy and apoptosis of chondrocytes by inhibiting NF-κB signaling pathway

Purpose: To investigate the effect of icariin on autophagy and apoptosis of chondrocytes, and the associated mechanisms.Methods: The chondrocytes were randomly divided into control (PBS intervention), TNF-α intervention, icarin +TNF-α, and NF-κB inhibition +TNF-α, with 8 strains in each group. The levels of IL-1, IL-6 and IL-12 were assayed by ELISA. The mRNA and protein expressions of ATG5, ATG7, Bax and Bcl-2 cells were determined by polymerase chain reaction (PCR) and Western blotting, while protein expressions of p-p65 and IκBα were assayed using Western blotting.Results: In the cartilage tissue of rats in the icariin +TNF-α group and NF-κB inhibition +TNF-α group, IL-1, IL-6 and IL-12 levels were significantly lower than those in TNF-α treatment group (p < 0.05). The AATG5 mRNA and protein in cartilage tissues of rats in icariin +TNF-α and NF-κB inhibition +TNF-α groups were significantly higher than those in TNF-α group. Bax mRNA and protein in cartilage tissues of icariin +TNF-α and NF-κB inhibition +TNF-α groups were downregulated, relative to TNF-α group; on the other hand, Bcl-2 mRNA and protein were significantly higher than those of TNF-α group (p < 0.05). In the cartilage tissues of Icarin +TNF-α, NF-κB inhibition +TNF-α groups, P-p65 protein was significantly lower than that of TNF-α (p < 0.05).Conclusion: TNF-α enhances the production of a large number of inflammatory factors by cartilage cells, inhibits autophagy of cartilage cells, and promotes cell apoptosis through regulation of NF-κB signaling pathway. Keywords: Icariin, NF-κB signaling pathway, TNF-α, Inflammatory response, Chondrocytes, Autophagy, Apoptosi

Determination of icariin in urine by high performance liquid chromatography with tandem mass-spectrometric detection

C использованием метода высокоэффективной жидкостной хроматографии-тандемной масс-спектрометрии разработан способ селективного определения икариина в пробах мочи. Для анализа биологических проб использовали обращенно-фазовый вариант высокоэффективной хроматографии на сорбентах с привитыми C18 группами. Определение осуществляли методом тандемной масс-спектрометрии с ионизацией электрораспылением в режиме регистрации выбранных ионных переходов для положительных ионов (энергия соударений - 40 %, ионный переход - с m/z = 677.2433 → 313.0703 (100 %), 369.1330 (35 %)). Выбрана процедура пробоподготовки, включающая в себя твёрдофазную экстракцию на картриджах SUPELCO HLB, концентрирование органического экстракта в токе азота и перерастворение сухого остатка. Предел детектирования составил 1 нг∙мл⁻¹. При валидации методики оценивали степень извлечения икариина из биологической жидкости (97 %), селективность и специфичность определения целевого соединения, а также влияние матрицы на ионизацию (4 %).Using the liquid chromatography tandem mass spectrometry, the approach for the selective detection of icariin in urine samples was developed. Biological samples analysis was performed by the reversed-phase chromatography using the C18 sorbent. The method of tandem mass spectrometry with the multiple reaction monitoring (MRM) mode using the electrospray ionization technique in positive ion mode was used (the collision energy - 40 %, m/z = 677.2433 → 313.0703 (100 %), 369.1330 (35 %)). The sample preparation procedure comprising of the solid-phase extraction based on SUPELCO HLB cartridges, the evaporation of the organic extract in a stream of nitrogen and the reconstitution of residue was selected. The detection limit was 1 ng ml⁻¹. During the method validation, the extraction of icariin from a biological fluid (97%), the selectivity and the specificity of the target compound as well as the matrix effects of ionization (4 %) were studied