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Osteoarthritis
Published in Nicole M. Farmer, Andres Victor Ardisson Korat, Cooking for Health and Disease Prevention, 2022
Wogonin is a unique aglycone flavone that may offer protection from OA. The flavone is primarily found in Chinese herbal teas. Unlike other flavonoids that originate from the flower parts of a plant, wogonin originates from the root of the herb Scutellaria baicalensis (Zhao et al., 2016). In vitro studies show that the flavone exerts direct anti-inflammatory and chondroprotective effects through suppressing the expression and production of inflammatory mediators including IL-6, COX-2, PGE2, iNOS, and NO in IL-1β-stimulated OA chondrocytes (Khan et al., 2017). Wogonin also exhibited chondroprotective potential through inhibiting the expression, production, and activities of matrix-degrading proteases including MMP-13, MMP-3, MMP-9, and ADAMTS-4 in OA chondrocytes (Khan et al., 2017).
Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
Flavones and related derivatives are very important to develop new and novel phytoceuticals. An important flavone is an apigenin, which has been tested and showed therapeutic promise of becoming a chemo-preventive agent (Shankar et al., 2017). Apigenin is known to have several medicinal properties that affect different molecular and cellular pathways on various diseases. This flavone also demonstrated anti-cancer, anti-inflammatory, and anti-oxidant properties. Apigenin lowered down the risk of several cancers and has synergized the chemotherapeutic outcome of some anticancer drugs (Shankar et al., 2017). Furthermore, apigenin has not only been used to prevent the risk of cancer but has also been studied for its activity to reduce neuroinflammation. Apigenin is capable of restoring cAMP which is the response element-binding protein, and this protein is essential for the up-regulation of brain-derived neurotrophic transcription factors (Bonetti et al., 2017). In vivo animal studies of this flavone showed an effect on inflammatory cytokines which are originated in certain immune cells and influence other cells.
Cognition Enhancers
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Ramneek Kaur, Rashi Rajput, Sachin Kumar, Harleen Kaur, R. Rachana, Manisha Singh
Though, 4-MC given in Figure 18.2 is able to cross the BBB of young mice (Fukumitsu et al., 1999; Fukuhara et al., 2012), another activator of TrkB, 7,8-dihydroxyflavone crosses the BBB and has an effect on emotional learning in the brain (specifically amygdala portion) (Andero et al., 2011; Zeng et al., 2012). Even though the specificity and affinity of flavone is quite low, it can be used as a preliminary point for development of drug. An alternative method can be activation of the pathways downstream of TrkB which would lead to the increase in specificity. There are three pathways (listed below) are activated by TrkB that play an important role in memory and growth of synapse (Yamada and Nabeshima, 2003). These are as follows:
Discovery of polymethoxyflavones as potential cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX) and phosphodiesterase 4B (PDE4B) inhibitors
Published in Journal of Receptors and Signal Transduction, 2022
Muhd Hanis Md Idris, Siti Norhidayah Mohd Amin, Siti Norhidayu Mohd Amin, Agustono Wibowo, Zainul Amiruddin Zakaria, Zurina Shaameri, Ahmad Sazali Hamzah, Manikandan Selvaraj, Lay Kek Teh, Mohd Zaki Salleh
Flavone is among the major plant secondary metabolites that are broadly distributed across the plant kingdom. It consists of a phenyl ring that attaches to chromone at 2-position. With a high degree of chemical diversity by modifications of the chemical backbones, flavone and its derivatives have multiple roles in biological functions and attract great interest from the researchers as privilege structures in drug discovery [9, 10]. In recent years, in vitro and in vivo studies as well as clinical studies have reported flavones as anti-inflammatory agent [11–13]. For instance, flavones displayed the reduction of COX-2 mediated prostaglandin E2 (PGE2) production and inhibited the activity of 5-lipoxygenase (5-LOX) [14]. Another study also reported that natural flavone was able to inhibit formation of nitric oxide (NO) in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages and indicated as potent anti-lipoxygenase inhibitor without significant cytotoxic effect [15].
Gelatin hydrogel/contact lens composites as rutin delivery systems for promoting corneal wound healing
Published in Drug Delivery, 2021
Lianghui Zhao, Xia Qi, Tao Cai, Zheng Fan, Hongwei Wang, Xianli Du
Quercetin, a member of the flavonoid family, is an important second metabolite that is widely distributed in vegetables, fruits, grains, tea, red wine, and so on. The flavone aglycone exhibits various biological activities, including antioxidant, anti-inflammatory, anti-fibrosis, immunomodulatory, anti-cancer, vascular protection, and neuroprotection functions (Quideau et al., 2011; Veitch, 2013; Lu et al., 2011). It has been used for the treatment of keratoconus, Graves ophthalmopathy, conjunctivitis, cataract, dry eye disease, retinopathy, and other ophthalmological diseases (Zhao et al., 2021). Rutin, the glycoside form of quercetin, has also been demonstrated efficacy for the prevention and treatment of inflammation, cataract, retinal neurovascular disease, and other ophthalmic diseases (Ola et al., 2015; Sasikala et al., 2013). However, the poor solubility of rutin in aqueous media leads to poor bioavailability after administration, which restricts the direct clinical applications. Several strategies, including cyclodextrins complexation, nanocarriers, and hydrogel carriers, have been proposed in recent years for enhancing the bioavailability of rutin (Júlio et al., 2019; Lee et al., 2018; Paczkowska et al., 2020). Among them, hydrogel offers a convenient and readily available approach.
Prevention of recognition memory loss and moderation of mitochondrial dynamic tendency toward fusion by flavone derivatives in Aβ-injected rats: a comparison between two flavonoids with different polarity
Published in Nutritional Neuroscience, 2019
Farshad Arsalandeh, Fariba Khodagholi, Shahin Ahmadian, Forough Foolad, Hamed Mohammadi Kamsorkh, Mahdi Moridi Farimani, Fatemeh Shaerzadeh
Following the determination of the effects of flavones on fear-motivated memory,24 the present study was aimed to evaluate the effects of two structurally different flavonoids 5-hydroxy-6,7,4ʹ-trimethoxyflavone (flavone 1) and 5,7,4ʹ-trihydroxyflavone (flavone 2) on object memorization using novel object recognition (NOR) test. Since, in novelty recognition, several parameters including detection, attention, and motivation are involved, NOR test has been considered to analyze cognition and neuropsychological issues in rats and mice.25 However, it has been reported that the hippocampus is necessary for object recognition memory.26 Also, cFos protein level was assessed to confirm whether oral intake of flavones prevents memory impaired by Aβ injection. Moreover, in order to specify mechanisms by which flavonoids exert their protective effects, the hippocampal protein level of mitochondrial dynamic markers was determined in intrahippocampally Aβ-injected rats.