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Potential of Fenugreek in Management of Fibrotic Disorders
Published in Dilip Ghosh, Prasad Thakurdesai, Fenugreek, 2022
Amit D. Kandhare, Sunil Bhaskaran, Subhash L. Bodhankar
Furthermore, experimental studies suggested that daily intake of anti-fibrotic fenugreek seed phytoconstituents (trigonelline, glycosides, apigenin) did not show any toxic effect during long-term administration (Kandhare, Bodhankar et al. 2016; Kandhare et al. 2019; Salehi et al. 2019; Zeiger and Tice 1997). Trigonelline demonstrated excellent safety (LD50 > 5000 mg/kg) with no adverse effects at doses 50 mg/kg for 21 days or 3500 mg for 70 days, no carcinogenicity or mutagenicity (Zeiger and Tice 1997). Acute oral toxicity study suggested flavonoid glycosides (Vicenin-1) exhibited median lethal dose (LD50) of 4837.5 mg/kg and NOAEL of 75 mg/kg during a subacute toxicity study (Kandhare, Bodhankar et al. 2016). Apigenin is considered safe, and evidence from experimental studies has shown that apigenin is non-mutagenic and non-genotoxic (Salehi et al. 2019). Moreover, fenugreek seed is a certified GRAS (Generally Recognized as Safe) ingredient (21 CFR § 182.20 2010). Thus, fenugreek seed and its phytoconstituents have a broad margin of safety and can be evaluated for further clinical development to manage fibrotic disorders.
Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Apigenin (Figure 12.8) is found in many fruits and vegetables, but celery, celeriac, parsley, and chamomile tea are the most common sources. In chamomile plants it is particularly abundant in their flowers, constituting nearly 70% of the total flavonoids.
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.
Possible anti-inflammatory, antioxidant, and neuroprotective effects of apigenin in the setting of mild traumatic brain injury: an investigation*
Published in Immunopharmacology and Immunotoxicology, 2023
Pınar Kuru Bektaşoğlu, Dilan Demir, Türkan Koyuncuoğlu, Meral Yüksel, İrem Peker Eyüboğlu, Ayça Karagöz Köroğlu, Dilek Akakın, Alper Yıldırım, Erhan Çelikoğlu, Bora Gürer
The current study is not without limitations. In this study, we aimed to eliminate the effects of secondary injury mechanisms via immediate apigenin treatment after TBI induction and by reaching an effective blood concentration readily. For clinical applications in cases of acute injuries, this timing may not be feasible or appropriate. We investigated 20 and 40 mg treatments and concluded that given the overall results, apigenin 20 mg treatment is enough for the desired neuroprotective effect. In a recent study, a 20 mg/kg dose of apigenin was nontoxic and 40 mg/kg was found to be ineffective and escalated the inflammatory and oxidative response [18]. In future studies, 20 mg/kg of apigenin treatment may be enough for investigating efficacy. The neuroprotective efficacy of apigenin treatment at different treatment durations could be investigated more comprehensively within various TBI models. The cytokine levels, except IL-10, were not significantly altered among groups. The reason for this may be the timing and method of measurement. Otherwise, mild TBI may not alter cytokine levels as expected; or they may return to baseline values 24 h after TBI. Further research is needed in order to clarify the effectiveness of apigenin treatment after TBI.
Apigenin Enhanced Antitumor Effect of Cisplatin in Lung Cancer via Inhibition of Cancer Stem Cells
Published in Nutrition and Cancer, 2021
Yunxia Li, Xin Chen, Wei He, Shuyue Xia, Xiaochuan Jiang, Xiaoyang Li, Jiayu Bai, Nan Li, Lei Chen, Biao Yang
Apigenin (4, 5, 7-trihydroxy flavone; API) is a natural flavone present in common fruits and vegetables including parsley, celery, celeriac, and chamomile tea. It exerts strong anti-inflammatory and protective effects in collagen-induced arthritis (11). Moreover, antimetastatic effects have been reported in multiple cancers including breast, prostate, skin, lung and ovarian cancers (12–14). Additionally, API suppresses CSC-like properties in triple-negative breast cancer cells (15), and it represses hypoxia-induced CSC marker gene expression in a head and neck squamous cell carcinoma cell line (16). In NSCLC, API induces human lung cancer H460 cell death (17), and enhances the cytotoxic effects of CDDP (18). Thus, we are interested in whether API plays an anti-tumor role in the CDDP-induced increase in CSCs and acquired resistance in NSCLC.
Protective effect of myricetin, apigenin, and hesperidin pretreatments on cyclophosphamide-induced immunosuppression
Published in Immunopharmacology and Immunotoxicology, 2021
Mehmet Berköz, Serap Yalın, Ferbal Özkan-Yılmaz, Arzu Özlüer-Hunt, Mirosław Krośniak, Renata Francik, Oruç Yunusoğlu, Abdullah Adıyaman, Hava Gezici, Ayhan Yiğit, Seda Ünal, Davut Volkan, Metin Yıldırım
The experiment was carried out for 14 d. In the untreated control group, 0.5 mL of saline was administered intraperitoneally and 1 mL of saline was administered orally without any medication for 14 d. In Group 3 and 4, myricetin was orally administered to the animals for 14 d at 100 and 200 mg/kg doses (dissolved in 1 mL of saline), respectively. In Group 5 and 6, apigenin was orally administered to the animals for 14 d at 100 and 200 mg/kg doses (dissolved in 1 mL of saline), respectively. In Group 7 and 8, hesperidin was orally administered to the animals for 14 d at 100 and 200 mg/kg doses (dissolved in 1 mL of saline), respectively. Cyclophosphamide (200 mg/kg, dissolved in 0.5 mL saline) was injected intraperitoneally in all rats except group 1 on the 4th day of the study. After the experimental period, all the animals were fasted for 12 h before being sacrificed by intraperitoneal injection of ketamine hydrochloride (15 mg/kg/i.p.) and xylazine (10 mg/kg/i.p.).