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In mice, topical apigenin improved skin permeability barrier function by promoting skin cell growth and the production of fatty molecules and antimicrobial proteins. This suggests it may help with conditions characterized by permeability barrier dysfunction such as atopic dermatitis [ 7]. Apigenin is one of the most renowned phenolic compounds with many beneficial properties, and it is available in nutraceutical formulations and dietary supplements. It also killed and reduced the growth, invasion, and migration of the following cancer cell types [ 27, 28, 29, 30, 31, 32]: Rats experiencing a severe reaction to infection (sepsis) had reduced inflammatory responses when treated with apigenin [ 12]. Using a circulating concentration for efficacy of 1–5μmol/L as the target, we evaluated data from both human and rodent pharmacokinetic studies to determine if a therapeutic concentration would be feasible. We find that oral intake of dietary materials would require heroic ingestion amounts and is not feasible. However, use of supplements of semi-purified apigenin in capsule form could reach target blood levels using amounts that are within the range currently acceptable for other supplements and medications. Modified formulations or parenteral injection are suitable but may not be necessary.
Due to its ability to reduce stress and promote relaxation, we advise taking Apigenin one hour before bedtime. Can I take Apigenin when pregnant or breastfeeding? To capture cellular mechanistic and pharmacodynamic data with particular attention to gastrointestinal cancers, the following search strategies were used in the same framework:Therefore in principle it should be possible, using oral dosing of apigenin capsules, to reach circulatory concentrations that are able to influence the biology of systemic targets. Circulatory apigenin should be available to act through the extracellular milieu for a substantial time. As indicated above there is a persistence of 6–9h after oral ingestion from human parsley consumption ( Meyer et al., 2006) and a T 1/ 2 of 2.1–4.2h in rodents ( Teng et al., 2012; Ding et al., 2014). With reasonable dosing several times per day, effective levels could be maintained for long enough a period to exert effects on the cell behaviors described in this review.
To capture all articles relevant to the pharmacokinetics of apigenin, a broad search strategy using those two terms was used on PubMed, considering only articles written in English or available as an English translation. This yielded (as of September 2020) an additional 314 articles which were manually curated together with those already available to provide the basis for this review. Selection was for relevance to the questions posed, informed by the perspectives of the authors. We considered i) wide information from a variety of analytical and preclinical models, ii) comparisons between oral and other administration routes, and iii) all information relevant to absorption, distribution, metabolism and excretion (ADME; the four parts of pharmacokinetics or how the body handles a bioactive molecule). As discussed in the previous section, Apigenin may increase testosterone and reduce cortisol levels, which creates an anabolic (muscle growth-promoting) environment in the body. There is substantial evidence for beneficial anti-cancer effects of apigenin, particular in the context of gastrointestinal cancers ( Lefort and Blay, 2013). However, much of the preclinical in vitro data utilizes highly selected lines of cancer cells that have been adapted to culture and that in monolayer may not well represent the behavior of cells within 3-dimensional tissue frameworks ( Lowthers et al., 2003; Howes et al., 2014). These cell populations may have different genotypes and behaviors compared with primary tumor isolates. As well, few in vivo studies use cancers implanted orthotopically, which better recapitulate the disease evolution compared to subcutaneous tumors ( Lensch et al., 2002; Flatmark et al., 2004). Our team comprises of trained MDs, PhDs, pharmacists, qualified scientists, and certified health and wellness specialists.Apigenin has been demonstrated to alleviate cardiovascular conditions by preserving the vascular lining in the aorta. It also induced the direct reduction of blood pressure by inhibiting of the activity of the angiotensin-converting enzyme, preventing blood vessel constriction. Doses as low as 2.5mg have been used to improve sleep. Upper doses are shown to be safe. When to take Apigenin? Apigenin’s high Vd and enterohepatic/enteric recycling processes indicate the elimination patterns of this lipophilic molecule will be delayed. Indeed, the elimination patterns in rat models using a single dose of 10mg of radiolabeled apigenin supports this ( Gradolatto et al., 2005). Following oral administration, ∼50% of apigenin was recovered in urine and ∼12% in feces ( Gradolatto et al., 2005). Unchanged, glucuronidated, and to a lesser extent sulfonated species, were recovered in all excrements ( Gradolatto et al., 2005). Although most products were excreted within the first 24 h, about 25% of the original apigenin dose was retained 10 days after treatment ( Gradolatto et al., 2005). Plasma clearance was estimated at 2ml/h ( Gradolatto et al., 2005). For humans, monoglucoronidated and monosulfonated species of apigenin have been recovered from urine and identified by HPLC ( Nielsen and Dragsted, 1998). SelfDecode has an AI-powered app that allows you to see how Apigenin benefits your personal genetic predispositions. These are all based on clinical trials. The red sad faces indicate an increased likelihood to develop conditions that Apigenin may improve. A database of 1,447 literature sources within the laboratory relating to flavonoid action in the gastrointestinal tract was used as the initial resource and to define best search parameters to capture all relevant articles relating to the pharmacokinetic and pharmacodynamic profile of apigenin.
Apigenin can potentially improve testosterone production and may even delay lowering testosterone levels due to aging. Experimental studies have previously demonstrated increased testosterone production from apigenin treatment. Further, the apigenin-induced increase in testosterone levels can also help promote muscle mass gain . 6. Prevents cancer The recommended dietary intake value for apigenin is not established. According to reports, apigenin intake from a regular daily diet doesn't reach the therapeutic doses used in clinical trials.
REVIEW article
Apigenin taken orally is systemically absorbed and recirculated by enterohepatic and local intestinal pathways. Its bioavailability is in the region of 30%. Once absorbed from the oral route it reaches maximal circulating concentration (C max) after a time (T max) of 0.5–2.5h, with an elimination half-life (T 1/ 2) averaging 2.52 ± 0.56h. Apigenin is a naturally occurring compound found in some fruits, vegetables and herbs. Due to its function within humans, it is classified as an antioxidant flavonoid. Flavonoids play a vital role in keeping us healthy whilst preventing the development of chronic diseases, such as cardiovascular disease and dementia. Flavonoids also promote good health due to having antibacterial, antiparasitic, antiviral and antifungal properties. Apigenin in particular has specific and exclusive benefits, due to its biological structure. What does Apigenin do? One study showed apigenin could effectively suppress prostate cancer progression by targeting a carcinogenesis-required signaling pathway. Regular apigenin intake is also implicated in having protective roles in the context of lung and ovarian cancer. Experts suggest apigenin can be used as a chemotherapeutic agent in combination with immunotherapy. 7. Increases insulin secretion
Some flavonoids, including apigenin, are able to modulate intestinal smooth muscle peristalsis–potentially facilitating their absorption( Gharzouli and Holzer, 2004). In vitro studies in guinea pigs show that apigenin interferes with muscle excitation and/or excitation-contraction, to decrease distension sensitivity and peristaltic performance in a concentration-dependent manner, thereby advantaging the absorption process ( Gharzouli and Holzer, 2004). Biliary excretion and recycling enables a significantly increased half-life of the compound and prolonged exposure of the intestinal mucosa ( Chen et al., 2003; Min et al., 2017). In addition to enterohepatic recycling, apigenin can also undergo local enteric recycling, in a concentration and metabolite-dependent manner ( Hu et al., 2003). These enterohepatic/enteric recycling processes will tend to favor the persistence of apigenin in the gastrointestinal tract but reduce net systemic absorption. Variability in Apigenin Absorption, and Bioavailability Chamomile tea is a popular herbal beverage, with apigenin concentrations varying depending on the brewing method and brand.
However, increased dosage intake from dietary supplements may cause unwanted side effects. Some apigenin side effects include: In rats with an enlarged heart caused by high blood pressure, apigenin decreased blood pressure, heart weight, heart weight index, and free fatty acid levels [ 39]. Promoting Sleep As mentioned, apigenin in its aglycone form can undergo phase I metabolism by CYP enzymes. The flavonoid chemical structure (i.e., C2-C3 double bonds and A-ring hydroxylation) makes these small molecules as a class potent inhibitors of CYP1A1, CYP1A2 and CYP1B1 in yeast, rat and human models ( Androutsopoulos et al., 2010; Kimura et al., 2010). Apigenin is also a potent inhibitor of CYP1A2 and CYP2C9 ( Kale et al., 2008; Si et al., 2009). Concomitant use of apigenin and certain drugs ( Table 2) could result in either a Class C-D drug-drug interactions, or complete contraindications as defined in the healthcare professional resource Lexicomp ( Lexicomp Inc, 2021).