Research

Apigenin

77 peer-reviewed studies curated from PubMed and Semantic Scholar.

4
Meta-analyses
3
Systematic reviews
3
RCTs
67
Other studies
Meta-analyses (5%)
Systematic reviews (4%)
RCTs (4%)

Studies

Sorted by quality and recency

2024·Mini reviews in medicinal chemistry·Thikra Majid Muhammed, Abduladheem Turki Jalil, Waam Mohammed Taher, et al

The Effects of Apigenin in the Treatment of Diabetic Nephropathy: A Systematic Review of Non-clinical Studies.

Systematic reviewInflammation

Systematic review of non-clinical studies on the effects of apigenin in treating diabetic nephropathy. Apigenin administration was found to reverse hyperglycemia-induced renal adverse effects in animal models, suggesting its potential nephroprotective role through antioxidant, anti-apoptotic, and anti-inflammatory activities.

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2024·Inflammopharmacology·Tosin A Olasehinde, Oyinlola O Olaokun

Apigenin and inflammation in the brain: can apigenin inhibit neuroinflammation in preclinical models?

Systematic reviewBrain Health Inflammation

Systematic review of 16 preclinical studies examining the anti-neuroinflammatory effects of apigenin. Apigenin inhibited neuroinflammation through various mechanisms, suggesting a neuroprotective effect against neuronal degeneration in neurodegenerative conditions.

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2024·Biomedicines·T. Olasehinde, O. O. Olaokun

The Beneficial Role of Apigenin against Cognitive and Neurobehavioural Dysfunction: A Systematic Review of Preclinical Investigations

Systematic reviewBrain Health Mental Clarity Mood

Systematic review of 34 preclinical studies on apigenin's effects on cognitive and neurobehavioural dysfunction in rats and mice. Apigenin enhanced learning and memory, exhibited anxiolytic effects, attenuated depressive-like behaviour, and improved sensorimotor and motor coordination. Mechanisms include modulation of neurotransmitter systems and inhibition of pro-inflammatory cytokine production.

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2024·Cancer medicine·Koohyar Ahmadzadeh, Shayan Roshdi Dizaji, Fatemeh Ramezani, et al

Potential therapeutic effects of apigenin for colorectal adenocarcinoma: A systematic review and meta-analysis.

Meta-analysis

This systematic review and meta-analysis investigates the effects of apigenin on colorectal adenocarcinoma. The analysis included 39 articles, showing that apigenin reduces cell viability, induces growth inhibition, apoptosis, and cell cycle arrest in in vitro studies, and decreases tumor size in in vivo studies. The findings suggest apigenin as a potential adjuvant agent in managing colorectal adenocarcinoma, though further in vivo studies are needed.

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2023·The Journal of asthma : official journal of the Association for the Care of Asthma·Fangfang Wang, Lianghua Xiao, Huahua Zhang, et al

Systemic meta-analysis: apigenin's effects on lung inflammation and oxidative stress.

Meta-analysisn = 226Inflammation Longevity

Systematic review and meta-analysis investigating the anti-inflammatory and antioxidant effects of apigenin in rat models of acute lung injury (ALI). The study found that apigenin may have potential anti-inflammatory and antioxidant effects, but further investigation through prospective controlled randomized trials is needed.

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2022·Inflammopharmacology·Ali Rahimi, Mina Alimohammadi, Fatemeh Faramarzi, et al

The effects of apigenin administration on the inhibition of inflammatory responses and oxidative stress in the lung injury models: a systematic review and meta-analysis of preclinical evidence.

Meta-analysisInflammation

This systematic review and meta-analysis evaluated the effects of apigenin on inflammatory markers and oxidative stress parameters in animal models of lung injuries. The findings showed that apigenin administration significantly decreased inflammatory biomarkers and oxidative stress markers, suggesting its potential as an alternative treatment for lung injury diseases.

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2022·Critical reviews in oncology/hematology·Deepti Singh, Meenakshi Gupta, Maryam Sarwat, et al

Apigenin in cancer prevention and therapy: A systematic review and meta-analysis of animal models.

Meta-analysis

Systematic review and meta-analysis of 25 animal studies investigating the anticancer effects of Apigenin. Apigenin was found to reduce tumor volume, weight, number, and load across various cancer types, primarily through apoptosis and cell-cycle arrest. No significant effect on animal body weight was observed.

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2022·Free radical biology & medicine·Gina Borges, Reedmond Y Fong, Jodi L Ensunsa, et al

Absorption, distribution, metabolism and excretion of apigenin and its glycosides in healthy male adults.

RCT

The study investigated the bioavailability of apigenin and its O-glycosides in healthy male adults. Apigenin was poorly absorbed, with metabolites excreted in urine. Different forms of apigenin intake, such as parsley drink and chamomile tea, showed variations in absorption and excretion patterns.

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2016·International journal of molecular medicine·Sungjin Choi, Jeungyeun Youn, Karam Kim, et al

Apigenin inhibits UVA-induced cytotoxicity in vitro and prevents signs of skin aging in vivo.

RCTSkin Hair Health

The study investigated the protective effects of apigenin on skin, showing that it restored the viability of UVA-exposed human dermal fibroblasts and decreased MMP-1 expression. In clinical application, an apigenin-containing cream increased dermal density and elasticity, reduced fine wrinkle length, and improved skin moisture and texture.

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2023·Carbohydrate polymers·Yunxiang Ma, Zidi Chen, Zhipeng Wang, et al

Molecular interactions between apigenin and starch with different amylose/amylopectin ratios revealed by X-ray diffraction, FT-IR and solid-state NMR.

Study

The study investigated intermolecular interactions between apigenin and starch with different amylose/amylopectin ratios using various analytical techniques. It found that corn starch with high amylose/amylopectin ratios had a better complexing ability with apigenin, involving hydrogen bonds as the molecular mechanism.

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2023·Scientific Reports·S. Akash, Imren Bayıl, Md. Saddam Hossain, et al

Novel computational and drug design strategies for inhibition of human papillomavirus-associated cervical cancer and DNA polymerase theta receptor by Apigenin derivatives

Study

The study uses in-silico analyses to explore the potential of Apigenin derivatives as inhibitors of human papillomavirus-associated cervical cancer and DNA polymerase theta. Molecular docking and dynamics simulations revealed promising interactions, with Apigenin derivatives showing significant binding energy against targeted proteins. Further validation through wet-lab experiments is suggested.

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2021·Food chemistry·Bin Li, Ying Hu, Ting Wu, et al

Apigenin-oxymatrine binary co-amorphous mixture: Enhanced solubility, bioavailability, and anti-inflammatory effect.

StudyInflammation

The study developed a co-amorphous mixture of apigenin and oxymatrine to enhance apigenin's solubility and bioavailability. The mixture showed improved solubility, dissolution, and anti-inflammatory effects compared to pure apigenin, suggesting potential applications in functional foods.

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1998·Journal of chromatography. B, Biomedical sciences and applications·S E Nielsen, L O Dragsted

Column-switching high-performance liquid chromatographic assay for determination of apigenin and acacetin in human urine with ultraviolet absorbance detection.

RCTn = 100

The paper describes an HPLC method for determining apigenin and acacetin in human urine using column-switching and UV detection. The method was applied to measure apigenin levels in 100 human urine samples from an intervention study with parsley.

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2024·Scientific Reports·Abouzar Najafi, Hossein Mohammadi, S. D. Sharifi, et al

Apigenin supplementation substantially improves rooster sperm freezability and post-thaw function

Animal study

This study investigated the effects of apigenin supplementation on rooster sperm cryosurvival. Supplementation with 100 μmol/L apigenin significantly improved total motility, progressive motility, membrane integrity, mitochondrial function, viability, and total antioxidant capacity compared to control. It also reduced abnormal morphology, reactive oxygen species, and apoptosis. The study identifies 100 μmol/L as the optimal concentration for enhancing rooster sperm cryosurvival.

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2023·Turkish Journal of Chemistry·Yuting Sun, Ming Guo, Xiaoxue Zhao, et al

Imaging supermolecular interactions of the pharmaceutical-cocrystal of apigenin-nicotinamide binding with serum albumin

Study

The study synthesized a pharmaceutical cocrystal using apigenin and nicotinamide, and investigated its interaction with human serum albumin (HSA) in vivo. The cocrystal showed improved solubility and cumulative release compared to raw apigenin. The binding mechanism to HSA was explored using molecular dynamic simulation and fluorescence spectroscopy.

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2023·Molecules·Xueyan Ji, W. Du, Wenqing Che, et al

Apigenin Inhibits the Progression of Osteoarthritis by Mediating Macrophage Polarization

Animal studyJoint Bone Health

The study investigated the protective effect of apigenin on chondrocytes in osteoarthritis using a mouse model. Apigenin was found to have a protective effect on cartilage degeneration, reduce inflammatory markers, and modulate macrophage polarization, promoting M2 polarization and inhibiting M1 polarization.

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2023·Life sciences·V. Singh, Debasish Sahoo, Kirti Agrahari, et al

Anti-inflammatory, anti-proliferative and anti-psoriatic potential of apigenin in RAW264.7 cells, HaCaT cells and psoriasis like dermatitis in BALB/c mice.

Animal studyInflammation Skin Hair Health

The study investigated the anti-inflammatory and anti-proliferative activity of apigenin in vitro and in vivo. Apigenin significantly reduced PASI and CosCam scores, improved histopathology, and downregulated pro-inflammatory cytokines in psoriasis-like conditions in BALB/c mice and LPS-induced RAW264.7 cells.

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2023·Journal of agricultural and food chemistry·Zhuoqun Meng, Min Gao, Chunyun Wang, et al

Apigenin Alleviated High-Fat-Diet-Induced Hepatic Pyroptosis by Mitophagy-ROS-CTSB-NLRP3 Pathway in Mice and AML12 Cells.

Animal studyInflammation

The study investigates the effect of apigenin on high-fat-diet-induced hepatic pyroptosis in C57BL/6J mice and AML12 cells. Apigenin was found to alleviate liver cell pyroptosis by reducing levels of inflammatory markers and promoting mitophagy, thereby reducing oxidative stress and inflammation.

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2023·European journal of pharmacology·Kun Xu, Yao Yang, M. Lan, et al

Apigenin alleviates oxidative stress-induced myocardial injury by regulating SIRT1 signaling pathway.

Animal studyHeart Health

The study investigates the protective effects of apigenin on oxidative stress-induced myocardial injury using an isoproterenol-induced mouse model and a hypoxia/reoxygenation-induced H9c2 cell model. Apigenin alleviated oxidative stress, cell apoptosis, and myocardial remodeling, and improved cardiomyocyte morphology by modulating the SIRT1 signaling pathway.

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2023·Food and Bioprocess Technology·San-San Ang, Y. Thoo, L. Siow

Encapsulation of Hydrophobic Apigenin into Small Unilamellar Liposomes Coated with Chitosan Through Ethanol Injection and Spray Drying

In vitro

The study investigated the encapsulation of apigenin into chitosan-coated liposomes to improve its aqueous solubility and delivery in foods. The encapsulated apigenin showed improved solubility, antioxidant capacity, and stability against simulated gastrointestinal digestion compared to unencapsulated apigenin.

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2022·Cancers·Ya-Hui Chen, Jyun-Xue Wu, Shun-Fa Yang, et al

Anticancer Effects and Molecular Mechanisms of Apigenin in Cervical Cancer Cells

In vitro

The study investigated the anticancer effects and molecular mechanisms of apigenin in cervical cancer in vitro and in vivo. Apigenin inhibited cell viability, induced cell cycle arrest, and inhibited migration and EMT of cervical cancer cells. In a cervical tumor xenograft mouse model, apigenin suppressed the growth of C33A xenograft tumors, suggesting potential as a chemotherapeutic agent for cervical cancer.

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2022·Frontiers in Microbiology·Yuan Qiao, Zhichun Zhang, Yuanyuan Zhai, et al

Apigenin Alleviates Obesity-Associated Metabolic Syndrome by Regulating the Composition of the Gut Microbiome

Animal studyGut Health Inflammation Nutrition

The study investigates the effects of apigenin on obesity-associated metabolic syndrome in high-fat diet-induced obese mice. Apigenin supplementation reduced body weight, low-grade inflammation, and insulin resistance, improved intestinal dysbiosis, and restored gut barrier damage. The study highlights apigenin's prebiotic role and its contribution to gut health and metabolic improvement.

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2022·Frontiers in Nutrition·Rui Ge, Haihua Zhu, Jian Zhong, et al

Storage stability and in vitro digestion of apigenin encapsulated in Pickering emulsions stabilized by whey protein isolate–chitosan complexes

In vitroNutrition

The study investigated the encapsulation of apigenin in Pickering emulsions stabilized by whey protein isolate-chitosan complexes to enhance its bioavailability. Different lipids were used to create lipid-based delivery systems, with medium-chain triglycerides showing the highest apigenin retention and bioaccessibility after storage and in vitro digestion experiments.

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2022·Lebensmittel-Wissenschaft + [i.e. und] Technologie. Food science + technology. Science + technologie alimentaire·Shan Hong, V. Dia, S. Baek, et al

Nanoencapsulation of apigenin with whey protein isolate: physicochemical properties, in vitro activity against colorectal cancer cells, and bioavailability.

In vitro

The study focused on nanoencapsulation of apigenin with whey protein isolate using a pH-cycle method. It characterized the physicochemical properties, in vitro anticancer activities against human colorectal cancer cells, and in vivo bioavailability. Nanoencapsulation enhanced apigenin's cellular uptake, pro-apoptotic effects, and bioavailability compared to unencapsulated apigenin.

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2021·Redox Biology·Changwon Yang, Jisoo Song, S. Hwang, et al

Apigenin enhances apoptosis induction by 5-fluorouracil through regulation of thymidylate synthase in colorectal cancer cells

In vitro

The study investigates the effect of apigenin on enhancing the efficacy of 5-fluorouracil (5-FU) in colorectal cancer cells. Apigenin was found to enhance the inhibitory effect of 5-FU on cell viability, inhibit thymidylate synthase upregulation, and potentiate 5-FU-induced apoptosis and cell cycle disruption in HCT116 cells.

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2021·Journal of Food and Drug Analysis·Man-Chen Hsu, Bei‐Chia Guo, Chia-Hui Chen, et al

Apigenin ameliorates hepatic lipid accumulation by activating the autophagy-mitochondria pathway

In vitro

In vitro study using Huh7 cells to investigate the effect of apigenin on hepatic lipid accumulation. Apigenin attenuated oleic acid-induced lipid accumulation by activating the autophagy-mitochondria pathway, increasing autophagy-related protein expression and mitochondrial function.

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2020·Planta Medica·M. Rittá, A. Marengo, A. Civra, et al

Antiviral Activity of a Arisaema Tortuosum Leaf Extract and Some of its Constituents against Herpes Simplex Virus Type 2

In vitro

The study evaluated the antiviral activity of Arisaema tortuosum leaf extract against HSV-2, including acyclovir-resistant strains. The extract and its constituents, apigenin and luteolin, showed significant inhibitory activity on the HSV-2 replicative cycle.

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2020·Biochemical pharmacology·M. Sudhakaran, M. Parra, Hayden Stoub, et al

Apigenin by targeting hnRNPA2 sensitizes triple-negative breast cancer spheroids to doxorubicin-induced apoptosis and regulates expression of ABCC4 and ABCG2 drug efflux transporters.

In vitro

The study investigates the role of apigenin in sensitizing triple-negative breast cancer (TNBC) spheroids to doxorubicin-induced apoptosis. Apigenin was found to induce apoptosis more effectively than apigenin-glycoside and inhibited the growth of TNBC patient-derived organoids. It sensitized spheroids to doxorubicin by triggering caspase-mediated apoptotic pathways and reducing efflux transporter expression.

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2020·International Journal of Nanomedicine·Pingping Li, S. N. Bukhari, Tahseen Khan, et al

Apigenin-Loaded Solid Lipid Nanoparticle Attenuates Diabetic Nephropathy Induced by Streptozotocin Nicotinamide Through Nrf2/HO-1/NF-kB Signalling Pathway

Animal studyInflammation

The study investigated the protective effects of Apigenin-loaded solid lipid nanoparticles (SLNPs) on renal damage induced by streptozotocin in rats. Apigenin-SLNPs enhanced the expression of nuclear factor erythroid 2-related factor 2 and heme oxygenase-1, and suppressed Nuclear Factor-κB expression, indicating protective mechanisms through anti-inflammatory and antioxidant activities.

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2020·Pharmaceutics·Mohsin Kazi, Abdullah M Alhajri, S. Alshehri, et al

Enhancing Oral Bioavailability of Apigenin Using a Bioactive Self-Nanoemulsifying Drug Delivery System (Bio-SNEDDS): In Vitro, In Vivo and Stability Evaluations

In vitroInflammation

The study aimed to enhance the solubility and bioavailability of apigenin using a bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS). The Bio-SNEDDS demonstrated efficient nanosized formation, improved dissolution rate, and significant increases in pharmacokinetic parameters compared to the pure drug in Wister rats. The antimicrobial study showed moderate inhibition of bacterial growth.

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2018·Saudi Pharmaceutical Journal : SPJ·S. Alshehri, F. Shakeel, M. Ibrahim, et al

Dissolution and bioavailability improvement of bioactive apigenin using solid dispersions prepared by different techniques

Study

The study aimed to improve the dissolution and bioavailability of apigenin (APG) using solid dispersions (SDs) prepared by different techniques. The SDs were characterized and showed significant improvement in in vitro dissolution and in vivo oral absorption in rats, with microwave SDs showing a 3.19-fold increase in bioavailability compared to a marketed capsule.

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2024·International Journal of Molecular Sciences·Karine Charrière, Vincent Schneider, Manon Perrignon-Sommet, et al

Exploring the Role of Apigenin in Neuroinflammation: Insights and Implications

ReviewBrain Health

This review explores the potential of apigenin as an anti-inflammatory agent in various neurological conditions, cancer, cardiovascular diseases, cognitive and memory disorders, and toxicity related to trace metals and other chemicals. It summarizes apigenin’s effects and mechanisms in neuroinflammation, highlighting its therapeutic promise.

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2024·Biomedicines·K. Allemailem, A. Almatroudi, H. Alharbi, et al

Apigenin: A Bioflavonoid with a Promising Role in Disease Prevention and Treatment

ReviewInflammation Immunity Heart Health Gut Health Skin Hair Health Brain Health

This narrative review discusses the health-promoting benefits of apigenin, a flavone compound found in fruits and vegetables. It highlights apigenin's anti-inflammatory and antioxidant properties, its positive effects on various body systems, and its potential in treating diseases like cancer, liver, lung, heart, kidney, and neurological diseases. The review also covers apigenin's interactions with drugs and its role in enhancing chemotherapy efficacy.

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2024·Frontiers in Nutrition·Daniel J. Kramer, Adiv A. Johnson

Apigenin: a natural molecule at the intersection of sleep and aging

ReviewSleep Longevity Mood

Narrative review discussing apigenin, a natural flavonoid, and its effects on sleep and aging. Apigenin elevates NAD+ levels, improves learning and memory, reduces tumor proliferation, and induces sedative effects in animal models. It also elongates survival in fly models and increases lifespan in worms. Human studies with chamomile extract, containing apigenin, show improvements in anxiety, mood, and pain relief.

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2023·International Journal of Molecular Sciences·J. Yoon, Mi-Yeon Kim, J. Cho

Apigenin: A Therapeutic Agent for Treatment of Skin Inflammatory Diseases and Cancer

ReviewSkin Hair Health Inflammation

This narrative review discusses the role of apigenin, a flavonoid used as a dietary supplement, in reducing skin inflammation by downregulating inflammatory markers and molecular targets. It explores current knowledge about inflammatory reactions in the skin and apigenin's mechanisms of action.

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2023·Nutrients·Shilu Deepa Thomas, N. Jha, S. Jha, et al

Pharmacological and Molecular Insight on the Cardioprotective Role of Apigenin

ReviewHeart Health

This review focuses on the cardioprotective role of apigenin, a dietary flavonoid with antioxidant, anti-inflammatory, anticancer, and antibacterial effects. It discusses the pharmacological mechanisms and potential therapeutic applications of apigenin in treating cardiovascular diseases, advocating for further preclinical and clinical investigations.

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2023·International Journal of Food Properties·Zarina Mushtaq, N. Sadeer, Muzzamal Hussain, et al

Therapeutical properties of apigenin: a review on the experimental evidence and basic mechanisms

ReviewInflammation Brain Health Skin Hair Health Heart Health Gut Health

This narrative review explores the anti-inflammatory mechanisms of apigenin, a flavonoid found in various plants. Apigenin is shown to decrease proinflammatory cytokines and block nitric oxide-mediated pathways, offering potential benefits in managing inflammatory-related diseases such as cancer, diabetes, and neurodegenerative diseases.

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2023·Frontiers in Nutrition·Peng Chen, Fuchao Chen, Zhi Guo, et al

Recent advancement in bioeffect, metabolism, stability, and delivery systems of apigenin, a natural flavonoid compound: challenges and perspectives

Review

This review discusses the biological effects, metabolism, stability, and bioactivity of apigenin, a bioflavonoid compound. It highlights advancements in delivery systems for apigenin, such as emulsions and liposomes, to improve its bioavailability and potential health benefits. The paper emphasizes the need for further research to develop effective delivery systems for food commercialization.

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2023·International Journal of Molecular Sciences·Laura Fossatelli, Zaira Maroccia, Carla Fiorentini, et al

Resources for Human Health from the Plant Kingdom: The Potential Role of the Flavonoid Apigenin in Cancer Counteraction

ReviewInflammation Longevity

Narrative review discussing the potential anticancer efficacy of apigenin, a flavonoid, in both in vitro and in vivo studies. Apigenin targets various signaling pathways involved in cancer development and progression, and has been studied for its synergistic effects with chemotherapy. Challenges include its low bioavailability, with novel drug-delivery systems being investigated to improve its solubility.

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2022·Biotechnology Reports·Moein Adel, Masoumeh Zahmatkeshan, A. Akbarzadeh, et al

Chemotherapeutic effects of Apigenin in breast cancer: Preclinical evidence and molecular mechanisms; enhanced bioavailability by nanoparticles

Review

The paper reviews the chemotherapeutic effects of apigenin in breast cancer, discussing preclinical evidence and molecular mechanisms. It highlights the enhanced bioavailability of apigenin through the use of nanoparticles.

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2022·Phytochemistry·Pantea Majma Sanaye, Mohammad Reza Mojaveri, Roohollah Ahmadian, et al

Different mechanisms by which apigenin improves treatment of dermatological disorders Apigenin and its dermatological applications: A comprehensive review.

ReviewSkin Hair Health

This narrative review provides an overview of the effects of apigenin on dermatological complications. Preclinical studies suggest beneficial effects on UV-induced skin damage, vitiligo, dermatitis, wounds, skin aging, and some skin cancers, primarily through anti-inflammatory and antioxidant mechanisms. No clinical studies have yet evaluated apigenin as a supplement for skin conditions.

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2022·Molecules·A. Rahmani, M. Alsahli, A. Almatroudi, et al

The Potential Role of Apigenin in Cancer Prevention and Treatment

ReviewInflammation

The review discusses the potential role of apigenin, a plant-derived flavonoid, in cancer prevention and treatment. It highlights apigenin's ability to modulate various cell signaling pathways, including tumor suppressor genes, angiogenesis, apoptosis, and inflammation, suggesting its anti-cancer potential.

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2021·Journal of food biochemistry·Piyush Kashyap, Deep Shikha, M. Thakur, et al

Functionality of apigenin as a potent antioxidant with emphasis on bioavailability, metabolism, action mechanism and in vitro and in vivo studies: A review.

ReviewInflammation Brain Health Heart Health

This review discusses the antioxidant potential of apigenin, a flavonoid, focusing on its bioavailability, metabolism, and action mechanisms. It highlights apigenin's ability to inhibit oxidant enzymes, modulate redox signaling pathways, and its protective effects in in vitro and in vivo studies, suggesting its potential to combat oxidative stress and related chronic diseases.

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2021·Cancer Cell International·Zeeshan Javed, H. Sadia, Muhammad Javed Iqbal, et al

Apigenin role as cell-signaling pathways modulator: implications in cancer prevention and treatment

Review

This narrative review focuses on the role of apigenin, a naturally-occurring flavonoid, in modulating oncogenic pathways in various cancers. It highlights apigenin's interactions with microRNAs and its potential in nano-formulations for targeted cancer therapy.

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2021·Frontiers in Pharmacology·Eva DeRango-Adem, J. Blay

Does Oral Apigenin Have Real Potential for a Therapeutic Effect in the Context of Human Gastrointestinal and Other Cancers?

Review

The paper reviews the potential of oral apigenin as a therapeutic agent against cancer, focusing on its pharmacokinetics and feasibility of achieving therapeutic concentrations in humans. It suggests that while dietary intake may be insufficient, supplements could reach target blood levels, and highlights the potential for beneficial interactions with chemotherapeutic drugs.

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2020·Frontiers in Chemistry·M. Ashrafizadeh, M. Bakhoda, Zahra Bahmanpour, et al

Apigenin as Tumor Suppressor in Cancers: Biotherapeutic Activity, Nanodelivery, and Mechanisms With Emphasis on Pancreatic Cancer

Review

This narrative review discusses the biotherapeutic activity of apigenin, a bioactive flavonoid, in cancer treatment, with a focus on pancreatic cancer. Apigenin is highlighted for its ability to suppress cancer cell proliferation, induce cell cycle arrest and apoptosis, inhibit metastasis, and sensitize cells to chemotherapy.

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2019·International Journal of Molecular Sciences·Noelia Sánchez-Marzo, A. Pérez-Sánchez, V. Ruiz-Torres, et al

Antioxidant and Photoprotective Activity of Apigenin and Its Potassium Salt Derivative in Human Keratinocytes and Absorption in Caco-2 Cell Monolayers

In vitroSkin Hair Health Inflammation

The study compared the antioxidant and photoprotective activity of apigenin and its potassium salt derivative (apigenin-K) in human keratinocytes and their absorption in Caco-2 cell monolayers. Both compounds showed similar photoprotective capacities against UVA and UVB radiation and protected cell viability. Apigenin-K's increased water solubility makes it a better candidate for further development as a nutraceutical and topical photoprotective ingredient.

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2019·BMC Pharmacology & Toxicology·A. Korga, M. Ostrowska, A. Józefczyk, et al

Apigenin and hesperidin augment the toxic effect of doxorubicin against HepG2 cells

In vitro

In vitro study evaluating the effect of natural flavonoids apigenin and hesperidin on the cytotoxicity of doxorubicin against HepG2 cells. Apigenin and hesperidin augmented the toxic effect of doxorubicin, altering glycolytic gene expression and increasing cytotoxicity without increasing oxidative stress.

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2019·Iranian Journal of Pharmaceutical Research : IJPR·Yannian Huang, Xiuhua Zhao, Y. Zu, et al

Enhanced Solubility and Bioavailability of Apigenin via Preparation of Solid Dispersions of Mesoporous Silica Nanoparticles

In vitro

The study investigates the use of mesoporous silica nanoparticles to enhance the solubility and bioavailability of apigenin. The AP-MSN solid dispersion showed improved in-vitro drug release and in-vivo bioavailability, with the AP area under curve0-t being 8.32 times higher than that of raw apigenin.

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2019·Frontiers in Pharmacology·Zisheng Chen, Dongbo Tian, Xiaowen Liao, et al

Apigenin Combined With Gefitinib Blocks Autophagy Flux and Induces Apoptotic Cell Death Through Inhibition of HIF-1α, c-Myc, p-EGFR, and Glucose Metabolism in EGFR L858R+T790M-Mutated H1975 Cells

In vitro

The study investigates the combination of apigenin and gefitinib on EGFR-resistant mutant non-small cell lung cancer cells. The combination inhibits oncogenic drivers, reduces protein expression related to glucose metabolism, and induces apoptotic cell death in EGFR L858R-T790M-mutated H1975 lung cancer cells.

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2019·Colloids and surfaces. B, Biointerfaces·K. Sen, Shubhadeep Banerjee, M. Mandal

Dual drug loaded liposome bearing apigenin and 5-Fluorouracil for synergistic therapeutic efficacy in colorectal cancer.

In vitro

The study investigates a dual drug-loaded liposome containing apigenin and 5-Fluorouracil for colorectal cancer treatment. The liposomal formulation aims to improve the bioavailability of apigenin and enhance the efficacy of 5-Fluorouracil. In vitro and in vivo tests showed increased cytotoxicity, inhibition of angiogenesis, and anti-tumorigenic effects in colon cancer models.

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2019·Biochemical pharmacology·Qian-ling Zhou, Ka-Wing Cheng, Jun Gong, et al

Apigenin and its methylglyoxal-adduct inhibit advanced glycation end products-induced oxidative stress and inflammation in endothelial cells.

In vitroInflammation

In vitro study examining apigenin's ability to scavenge reactive carbonyl species and inhibit advanced glycation end products-induced oxidative stress and inflammation in endothelial cells. Apigenin and its adducts reduced ROS production and decreased pro-inflammatory cytokine expression, suggesting potential protective effects against AGEs-associated health disorders.

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2019·Journal of pharmaceutical sciences·Shan Huang, Qian Xue, Jia Xu, et al

Simultaneously Improving the Physicochemical Properties, Dissolution Performance, and Bioavailability of Apigenin and Daidzein by Co-Crystallization With Theophylline.

Study

The study investigates the co-crystallization of apigenin and daidzein with theophylline to improve their physicochemical properties, dissolution performance, and bioavailability. The co-crystals showed improved solubility, dissolution rates, and bioavailability compared to the parent flavonoids.

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2018·Toxicology and Applied Pharmacology·H. Lim, Dong Suk Min, Haeil Park, et al

Flavonoids interfere with NLRP3 inflammasome activation

In vitroInflammation

The study investigated the effects of flavonoids on NLRP3 inflammasome activation in differentiated THP-1 cells. Apigenin, kaempferol, and quercetin significantly inhibited IL-1β production, with apigenin also reducing neutrophils and monocytes in MSU-induced peritonitis in mice. The study elucidates the structure-activity profiles of flavonoids in inflammasome activation.

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2018·Journal of Experimental & Clinical Cancer Research : CR·Lu Xu, Y. Zhang, Kang Tian, et al

Apigenin suppresses PD-L1 expression in melanoma and host dendritic cells to elicit synergistic therapeutic effects

Animal studyImmunity

The study investigated the effects of apigenin on PD-L1 expression and melanoma tumorigenesis. Apigenin showed growth-suppressive and pro-apoptotic effects on melanoma cells, inhibited IFN-γ-induced PD-L1 upregulation, and increased sensitivity to T cell-mediated killing. In vivo, apigenin inhibited melanoma xenograft growth and enhanced T cell infiltration. It also reduced PD-L1 expression in dendritic cells, enhancing the cytotoxicity of cytokine-induced killer cells.

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2017·Frontiers in Pharmacology·L. Masuelli, M. Benvenuto, Rosanna Mattera, et al

In Vitro and In Vivo Anti-tumoral Effects of the Flavonoid Apigenin in Malignant Mesothelioma

In vitro

The study investigates the anti-tumoral effects of the flavonoid apigenin (API) in malignant mesothelioma (MM) using both in vitro and in vivo models. API inhibited MM cell survival, induced apoptosis, and affected various signaling pathways in vitro. In vivo, API increased the median survival of mice transplanted with MM cells and reduced tumor growth risk.

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2017·PLoS ONE·David Bauer, Natalie Redmon, E. Mazzio, et al

Apigenin inhibits TNFα/IL-1α-induced CCL2 release through IKBK-epsilon signaling in MDA-MB-231 human breast cancer cells

In vitroInflammation

The study investigates the potential of apigenin to downregulate TNFα-mediated release of chemokines from human triple-negative breast cancer cells (MDA-MB-231). Apigenin suppressed the TNFα-induced rise of CCL2, GMCSF, IL-1α, and IL-6, and blocked signaling patterns associated with CCL2 through suppressed mRNA and protein synthesis of IKBKe.

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2017·Oncotarget·Shuai Meng, Yi Zhu, Jiangfeng Li, et al

Apigenin inhibits renal cell carcinoma cell proliferation

In vitro

The study evaluated the effects of apigenin on renal cell carcinoma (RCC) cells, showing that apigenin suppressed RCC cell proliferation in a dose- and time-dependent manner. Apigenin caused DNA damage, induced G2/M phase cell cycle arrest, and apoptosis, which collectively suppressed RCC cell proliferation in vitro and in vivo. Apigenin treatment reduced tumor growth and volume in a mouse model.

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2017·Oxidative Medicine and Cellular Longevity·R. Souza, P. Bonfim-Mendonça, F. Gimenes, et al

Oxidative Stress Triggered by Apigenin Induces Apoptosis in a Comprehensive Panel of Human Cervical Cancer-Derived Cell Lines

In vitro

The study evaluated the cytotoxic effects of apigenin on a panel of human cervical cancer-derived cell lines. Apigenin induced apoptosis selectively in cancer cells, increased ROS levels, and inhibited cancer cell migration and invasion, suggesting its potential as an anticancer drug for cervical cancer.

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2017·Experimental and Therapeutic Medicine·Kun Zhang, Wei Song, Dalin Li, et al

Apigenin in the regulation of cholesterol metabolism and protection of blood vessels

Animal studyHeart Health Inflammation

The study analyzed the mechanisms of apigenin in regulating cholesterol metabolism and protecting blood vessels using a mouse model of hyperlipidemia and in vitro cell experiments. Apigenin significantly reduced blood fat, cholesterol, triglycerides, and low-density lipoprotein cholesterol in high-fat diet mice, improved blood lipid metabolism, and increased superoxide dismutase activity and nitric oxide secretion in endothelial cells.

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2016·Oncotarget·Yuan Qin, Dong Zhao, Honggang Zhou, et al

Apigenin inhibits NF-κB and Snail signaling, EMT and metastasis in human hepatocellular carcinoma

In vitroInflammation

The study investigates the effects of apigenin on migration and metastasis in human hepatocellular carcinoma cell lines. Apigenin inhibited proliferation, migration, and invasion of HCC cells, suppressed tumor growth in xenografts, and reduced Snai1 and NF-κB expression, suggesting it may inhibit EMT by affecting the NF-κB/Snail pathway.

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2016·International Journal of Molecular Sciences·Horacio Cardenas, Daniel Arango, C. Nicholas, et al

Dietary Apigenin Exerts Immune-Regulatory Activity in Vivo by Reducing NF-κB Activity, Halting Leukocyte Infiltration and Restoring Normal Metabolic Function

Animal studyImmunity Inflammation Heart Health

The study investigates the immune-regulatory activity of apigenin in vivo. Apigenin improved survival in mice treated with a lethal dose of LPS by restoring normal cardiac function and modulating NF-κB activity in the lungs, reducing inflammation and leukocyte infiltration.

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2015·Evidence-based Complementary and Alternative Medicine : eCAM·S. Ju, Jun-Gue Kang, J. Bae, et al

The Flavonoid Apigenin Ameliorates Cisplatin-Induced Nephrotoxicity through Reduction of p53 Activation and Promotion of PI3K/Akt Pathway in Human Renal Proximal Tubular Epithelial Cells

In vitro

The study investigated the antiapoptotic effects of apigenin on cisplatin-treated human renal proximal tubular epithelial (HK-2) cells. Apigenin inhibited cisplatin-induced apoptosis by reducing p53 activation and promoting the PI3K/Akt pathway, suggesting a protective role against nephrotoxicity.

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2015·Cancer Cell International·Ming-Der Shi, Cheng-Kai Shiao, Yi-Chieh Lee, et al

Apigenin, a dietary flavonoid, inhibits proliferation of human bladder cancer T-24 cells via blocking cell cycle progression and inducing apoptosis

In vitro

The study investigates the anti-proliferative activity of apigenin in human bladder cancer T-24 cells. Apigenin inhibited cell proliferation in a dose-dependent manner by blocking cell cycle progression and inducing apoptosis, involving mitochondrial apoptotic pathways and increased ROS levels.

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2014·International Journal of Nanomedicine·Shu-min Ding, Zhen-hai Zhang, Jie Song, et al

Enhanced bioavailability of apigenin via preparation of a carbon nanopowder solid dispersion

In vitro

The study developed a carbon nanopowder drug carrier to improve the oral bioavailability of apigenin. Solid dispersions of apigenin with carbon nanopowder showed a 275% improvement in dissolution and 1.83 times higher bioavailability in rats compared to pure apigenin. Preliminary toxicity tests indicated no significant intestinal toxicity.

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2013·Molecules·Le Zhao, Jun-li Wang, Rui Liu, et al

Neuroprotective, Anti-Amyloidogenic and Neurotrophic Effects of Apigenin in an Alzheimer’s Disease Mouse Model

Animal studyBrain Health

The study examined the effects of apigenin on cognitive function in APP/PS1 double transgenic Alzheimer's disease mice. Apigenin treatment improved learning and memory, reduced amyloid-β burden, inhibited oxidative stress, and restored neurotrophic pathways, suggesting potential therapeutic effects for Alzheimer's disease.

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2013·Cancer Cell International·Yi Zhu, Y. Mao, Hong Chen, et al

Apigenin promotes apoptosis, inhibits invasion and induces cell cycle arrest of T24 human bladder cancer cells

In vitro

In vitro study investigating the effects of apigenin on T24 human bladder cancer cells. Apigenin suppressed proliferation, inhibited migration and invasion, induced G2/M phase cell cycle arrest, and promoted apoptosis through a caspase-dependent mechanism involving the PI3K/Akt pathway and Bcl-2 family proteins.

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2012·Life sciences·M. Pinheiro, F. Boylan, P. Fernandes

Antinociceptive effect of the Orbignya speciosa Mart. (Babassu) leaves: evidence for the involvement of apigenin.

Animal study

The study investigated the antinociceptive effects of ethanol extract and dichloromethane fraction from Babassu leaves, as well as apigenin, using nociception models in mice. The extracts and apigenin showed antinociceptive activity comparable to morphine, mediated by opioid and cholinergic systems.

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2012·FASEB journal : official publication of the Federation of American Societies for Experimental Biology·Christopher D Lucas, Keith C Allen, David A Dorward, et al

Flavones induce neutrophil apoptosis by down-regulation of Mcl-1 via a proteasomal-dependent pathway.

In vitroInflammation

The study investigates the ability of flavones (apigenin, luteolin, and wogonin) to induce neutrophil apoptosis in vitro and resolve neutrophilic inflammation in vivo. All three flavones induced time- and concentration-dependent neutrophil apoptosis, which was caspase dependent and associated with down-regulation of the prosurvival protein Mcl-1. Wogonin enhanced resolution of neutrophilic inflammation in a zebrafish model.

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2011·PLoS ONE·Yimiao Xu, Yinqiang Xin, Y. Diao, et al

Synergistic Effects of Apigenin and Paclitaxel on Apoptosis of Cancer Cells

In vitro

The study investigates the synergistic pro-apoptotic effects of apigenin and paclitaxel on human cancer cell lines. Apigenin was found to sensitize cancer cells to paclitaxel-induced apoptosis by suppressing SOD activity, leading to ROS accumulation and caspase-2 cleavage.

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2010·Cell Death & Disease·M. Gonzalez-Mejia, O. Voss, E. Murnan, et al

Apigenin-induced apoptosis of leukemia cells is mediated by a bimodal and differentially regulated residue-specific phosphorylation of heat-shock protein–27

In vitro

The study investigates the mechanism of apigenin, a natural flavonoid, in inducing apoptosis in leukemia cells. It was found that apigenin induces bimodal phosphorylation of heat-shock protein-27 (Hsp27) at specific residues, which increases the susceptibility of leukemia cells to apoptosis.

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2007·Cancer research·S. Shukla, G. MacLennan, C. Flask, et al

Blockade of beta-catenin signaling by plant flavonoid apigenin suppresses prostate carcinogenesis in TRAMP mice.

Animal studyMens Health

The study investigated the effects of apigenin on prostate carcinogenesis in TRAMP mice. Oral intake of apigenin significantly decreased tumor volumes and abolished metastases, improved survival, and altered protein levels related to beta-catenin signaling, suggesting its potential in suppressing prostate cancer.

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2005·Molecular cancer therapeutics·Risa Torkin, Jean-François Lavoie, D. Kaplan, et al

Induction of caspase-dependent, p53-mediated apoptosis by apigenin in human neuroblastoma.

In vitroBrain Health

The study investigates the effects of apigenin, a dietary flavonoid, on human neuroblastoma cell lines. Apigenin inhibited growth and induced apoptosis in neuroblastoma cells, likely through a p53-Bax-caspase-3 apoptotic pathway, without affecting nontransformed cells.

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2019·BioMed Research International·Minqian Wang, Jenni Firrman, Linshu Liu, et al

A Review on Flavonoid Apigenin: Dietary Intake, ADME, Antimicrobial Effects, and Interactions with Human Gut Microbiota

ReviewGut Health

This review summarizes studies on the antimicrobial effects of apigenin and its interactions with human gut microbiota. It discusses apigenin's antibacterial, antifungal, and antiparasitic capabilities, and how it is metabolized by gut bacteria, potentially affecting human health.

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2019·International Journal of Molecular Sciences·B. Salehi, A. Venditti, M. Sharifi-Rad, et al

The Therapeutic Potential of Apigenin

Review

This narrative review provides an updated overview of apigenin, focusing on its health-promoting effects and therapeutic functions. It summarizes key findings from in vivo research, including animal models and human studies, discussing its potential benefits in conditions such as diabetes, amnesia, Alzheimer's disease, depression, insomnia, and cancer.

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2019·Antioxidants·Rashida Ginwala, R. Bhavsar, DeGaulle I. Chigbu, et al

Potential Role of Flavonoids in Treating Chronic Inflammatory Diseases with a Special Focus on the Anti-Inflammatory Activity of Apigenin

ReviewInflammation Brain Health

This review discusses the anti-inflammatory actions of flavonoids, with a special focus on apigenin, against chronic illnesses such as cancer, diabetes, cardiovascular diseases, and neuroinflammation. It highlights the potential of apigenin as a natural alternative therapy for chronic inflammatory conditions, particularly in CNS-related disorders.

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1999·Die Nahrung·J Hempel, H Pforte, B Raab, et al

Flavonols and flavones of parsley cell suspension culture change the antioxidative capacity of plasma in rats.

Animal studyInflammation

Flavonoid extracts from illuminated parsley cell suspension culture were administered to rats, temporarily increasing the antioxidative capacity of blood plasma with maximum values after 1 hour. The study suggests changes in plasma flavonoid content reflect antioxidative capacity.

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