Yellow acicular crystal
Tagetes erecta L
Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu (C. unshiu) peel. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM). Anti-inflammatory and anticancer properties.
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Tagetes lucida Cav. is an ancient medicinal plant used to treat different ailments involving neurological diseases and pain. However, scientific studies to validate their medicinal properties as analgesic have not been described. The aim of this study was to evaluate the T. lucida antinociceptive response using pain models. Bioactive compounds and a possible mechanism of action were also explored. Dose-response effects of an ethanol crude extract were investigated in the writhing and formalin tests in mice and rats, respectively. The extract was fractionated to isolate active fractions and bioactive compounds (quercetagetin 7‑O‑β‑d‑glucoside and 6,7‑dimethoxycoumarin) using the formalin test. The antinociceptive effects were compared to the reference drugs (tramadol 10 mg/kg, diclofenac 50 mg/kg, and/or ketorolac 1 mg/kg, i.p.). The ethanol extract was explored in the presence of naloxone (3 mg/kg, i.p. a non-selective opioid receptor antagonist) and WAY100635 (0.5 mg/kg, s.c., a selective 5-HT1A receptor antagonist) to screen their participation as possible inhibitory mechanisms involved in the antinociceptive response of T. lucida. The ethanol crude extract, fractions, and pure compounds caused a significant antinociceptive response resembling the effect of the reference drugs. Both opioid and 5-HT1A receptors participated in the analgesic -like activity of the extract, which did not produce gastric damage. On the contrary, the gastric damage produced as an adverse effect of the analgesic ketorolac was prevented when combined with the extract. In conclusion, these preliminary data provide evidence and give support to the properties attributed to T. lucida in the traditional medicine to alleviate pain.
Copyright © 2019. Published by Elsevier Inc.
Analgesia; Asteraceae; Coumarins; Flavonoids; Tagetes lucida Cav.; Traditional medicine
Identification of some bioactive metabolites and inhibitory receptors in the antinociceptive activity of Tagetes lucida Cav.
Gonzalez-Trujano ME1, Gutierrez-Valentino C2, Hernandez-Aramburo MY2, Diaz-Reval MI3, Pellicer F2.
2019 Aug 15
The utilization of layer-by-layer composite nanoparticles fabricated from zein and hyaluronic acid (HA) for the codelivery of curcumin and quercetagetin was investigated. A combination of hydrophobic effects and hydrogen bonding was responsible for the interaction of zein with both curcumin and quercetagetin inside the nanoparticles. Electrostatic attraction and hydrogen bonding were mainly responsible for the layer-by-layer deposition of hyaluronic acid on the surfaces of the nanoparticles. The secondary structure of zein was altered by the presence of the two nutraceuticals and HA. The optimized nanoparticle formulation contained relatively small particles ( d = 231.2 nm) that were anionic (ζ = -30.5 mV). The entrapment efficiency and loading capacity were 69.8 and 2.5% for curcumin and 90.3 and 3.5% for quercetagetin, respectively. Interestingly, the morphology of the nanoparticles depended on their composition. In particular, they changed from coated nanoparticles to nanoparticle-filled microgels as the level of HA increased. The nanoparticles were effective at reducing light and thermal degradation of the two encapsulated nutraceuticals and remained physically stable throughout 6 months of long-term storage. In addition, the nanoparticles were shown to slowly release the nutraceuticals under simulated gastrointestinal tract conditions, which may help improve their oral bioavailability. In summary, we have shown that layer-by-layer composite nanoparticles based on zein and HA are an effective codelivery system for two bioactive compounds.
composite nanoparticles; curcumin; hyaluronic acid; layer-by-layer stepwise deposition; quercetagetin; zein
Fabrication and Characterization of Layer-by-Layer Composite Nanoparticles Based on Zein and Hyaluronic Acid for Codelivery of Curcumin and Quercetagetin.
Chen S1, Han Y1, Huang J1, Dai L1, Du J2, McClements DJ3, Mao L1, Liu J1, Gao Y1.
2019 May 8;
The antisolvent coprecipitation method was utilized for fabricating the zein and hyaluronic acid complex at different mass ratios (100:5, 100:10, 100:15, 100:20, 100:25 and 100:30). Results showed that negatively charged zein-hyaluronic acid complex with small size (181.5 nm) was formed through the driving force of electrostatic attraction, followed by hydrogen bonding and hydrophobic effects. The incorporation of hyaluronic acid led to conformational change of zein, and improved its physical and thermal stability. Native hyaluronic acid showed a three-dimensional network structure, while zein-hyaluronic acid binary complex exhibited two different microstructures, including nanoparticles (zein: hyaluronic acid, above 100:20) and particle-filled-microgel (zein: hyaluronic acid, below 100:20). In addition, zein-hyaluronic acid complex was designed as a new delivery vehicle to anti- thermal degradation and control release of quercetagetin. These findings indicated that zein-hyaluronic acid complex would be a useful and promising delivery vehicle for embedding and protecting bioactive compounds.
Copyright © 2018 Elsevier Ltd. All rights reserved.
Binary complex; Hyaluronic acid; Quercetagetin; Structural characterization; Zein
Zein-hyaluronic acid binary complex as a delivery vehicle of quercetagetin: Fabrication, structural characterization, physicochemical stability and in vitro release property.
Chen S1, Han Y2, Wang Y1, Yang X1, Sun C1, Mao L1, Gao Y3.
2019 Mar 15