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The American Journal of Chinese Medicine 2021Breviscapine is one of the extracts of several flavonoids of . Scutellarin is the main active component of breviscapine, and the qualitative or quantitative criteria as... (Review)
Review
Breviscapine is one of the extracts of several flavonoids of . Scutellarin is the main active component of breviscapine, and the qualitative or quantitative criteria as well. Scutellarin and its analogs share a similar skeleton of the flavonoids. Breviscapine has been widely used in the treatment of cerebral infarction and its sequelae, cerebral thrombus, coronary heart disease (CHD), and angina pectoris. Breviscapine has a broad spectrum of pharmacological activities, such as increasing blood flow, improving microcirculation, dilating blood vessels, decreasing blood viscosity, promoting fibrinolysis, inhibiting platelet aggregation, and thrombosis formation, etc. In addition, breviscapine and its analogs have significant value for drug research and development because of the superiority of those significant bioactivities. Furthermore, an increasing number of pharmacokinetic studies have explored the mechanism of scutellarin and its analogs. To provide a comprehensive understanding of the current research on breviscapine, scutellarin, and the analogs, the structural features, distribution situation, preparation method, content determination method, clinical applications, pharmacological action as well as pharmacokinetics are summarized in the present review.
Topics: Apigenin; Flavonoids; Glucuronates; Humans; Molecular Structure; Plant Extracts
PubMed: 34263720
DOI: 10.1142/S0192415X21500646 -
International Journal of Molecular... Feb 2023The prominent flavonoids apigenin and chrysin have been demonstrated to have systemic benefits. Our previous work was first to establish the impact of apigenin and...
The prominent flavonoids apigenin and chrysin have been demonstrated to have systemic benefits. Our previous work was first to establish the impact of apigenin and chrysin on cellular transcriptome. In the current study, we have revealed the ability of apigenin and chrysin to alter the cellular metabolome based on our untargeted metabolomics. Based on our metabolomics data, both these structurally related flavonoids demonstrate diverging and converging properties. Apigenin demonstrated the potential to possess anti-inflammatory and vasorelaxant properties through the upregulation of intermediate metabolites of alpha-linolenic acid and linoleic acid pathways. Chrysin, on the other hand, exhibited abilities to inhibit protein and pyrimidine synthesis along with downregulation of gluconeogenesis pathways based on the altered metabolites detected. Chrysin-mediated metabolite changes are mostly due to its ability to modulate L-alanine metabolism and the urea cycle. On the other hand, both the flavonoids also demonstrated converging properties. Apigenin and chrysin were able to downregulate metabolites involved in cholesterol biosynthesis and uric acid synthesis, namely 7-dehydrocholesterol and xanthosine, respectively. This work will provide understanding regarding the diverse therapeutic potential of these naturally occurring flavonoids and help us in curbing an array of metabolic complications.
Topics: Apigenin; Flavonoids; Up-Regulation; Metabolomics
PubMed: 36835484
DOI: 10.3390/ijms24044066 -
Environmental Science and Pollution... Oct 2021Cadmium (Cd) is one of the most important heavy metals in the environment which has several effects on the morphology, physiology, and anatomy of plants. It is a mobile...
Cadmium (Cd) is one of the most important heavy metals in the environment which has several effects on the morphology, physiology, and anatomy of plants. It is a mobile heavy metal that can be transferred easily into plants, thus entering into the human food chain. Chamomile (Matricaria chamomilla L.) as an important medicinal plant can uptake and accumulate Cd in its root and aerial organs. In this research, the effects of different concentrations of Cd (90, 180, and 360 μM) were investigated on the growth parameters, anatomical features, and enzymatic antioxidant activities in flowers of chamomile after 7 days of exposure. The content of apigenin, a flavone compound mostly synthesizing in chamomile flowers, was also analyzed after 72 h from Cd treatment. The results showed that all concentrations of Cd reduced the length and biomass of roots and shoots, the diameter of flowers, as well as the number of pollen grains in tubular florets, while increased trichome density on the florets. Cd-treated plants showed an increase in antioxidant enzymes, superoxide dismutase (SOD), and peroxidase (POX) activities. After 7 days of treatment to Cd major concentration, flowers accumulated Cd and enhanced the apigenin production with the increase of Cd contamination in hydroponic solution. This increase of apigenin is most likely due to its antioxidant and sequestering property as a resistance response to Cd excess.
Topics: Apigenin; Cadmium; Flowers; Humans; Hydroponics; Matricaria
PubMed: 34128167
DOI: 10.1007/s11356-021-14000-7 -
Journal of the Science of Food and... Sep 2021The flower of Dendranthema morifolium Ramat Tzvel has been widely used as a nutritional health supplement worldwide. However, most of the studies have focused on the...
BACKGROUND
The flower of Dendranthema morifolium Ramat Tzvel has been widely used as a nutritional health supplement worldwide. However, most of the studies have focused on the flower and the rest of the plant was neglected. Our hypothesis is that similar flavonoids may be present at different parts of D. morifolium, and the flavonoids may undergo a similar biotransformation pathway within the body. To investigate this hypothesis, an in vivo pharmacokinetic experimental model was developed to explore the comparative biotransformation of luteolin and apigenin after administration of D. morifolium extracts (10 g kg , p.o.) in freely moving rats. Because luteolin and apigenin mainly underwent phase II metabolism, the metabolic enzymes of β-glucuronidase/sulfatase or β-glucuronidase were used to hydrolyze the plasma sample, depending on the biotransformation pathway involved.
RESULTS
The results revealed that luteolin and apigenin mainly went through glucuronide and sulfate conjugations, respectively, in both the extract of flowers and the stem-and-leaf group. In addition, the area under the concentration curve (AUC ) of luteolin glucuronides and sulfates in the group administered the stem-and-leaf extract was approximately 4.6 times higher than that of the flower extract group. The dominant products of biotransformation for apigenin were sulfates.
CONCLUSION
These findings support our hypothesis that not only the flower parts of D. morifolium, but also the stem-and-leaf parts contain rich flavones, including glycosides and aglycone, and they undergo similar biotransformation pathways. © 2021 Society of Chemical Industry.
Topics: Animals; Apigenin; Chrysanthemum; Flavonoids; Flowers; Hydrolysis; Luteolin; Molecular Structure; Plant Extracts; Plant Leaves; Plant Stems; Rats; Rats, Sprague-Dawley
PubMed: 33543470
DOI: 10.1002/jsfa.11137 -
Domestic Animal Endocrinology 2023The study aimed to evaluate the involvement of apigenin, microRNA (miR)-152, and their interrelationships in the control of basic ovarian granulosa cell functions. The...
The study aimed to evaluate the involvement of apigenin, microRNA (miR)-152, and their interrelationships in the control of basic ovarian granulosa cell functions. The effects of apigenin (0, 10, and 100 µg/mL), miR-152 analogues or miR-152 inhibitor, and their combinations with apigenin on porcine granulosa cells were examined. Expression levels of miR-152, viability, proliferation, apoptosis, steroid hormones, IGF-I, oxytocin, and prostaglandin E2 release were analyzed. Apigenin increased the expression of miR-152, cell proliferation, and estradiol release and reduced apoptosis, progesterone, and IGF-I output. MicroRNA-152 analogues promoted cell viability and proliferation, as well as the release of progesterone, IGF-I, oxytocin, and prostaglandin E2; however, it inhibited apoptosis and estradiol output. miR-152 inhibitor had the opposite effect. Moreover, miR-152 analogues suppressed the effect of apigenin on cell apoptosis and estradiol release. These observations 1) confirm the involvement of apigenin in the control of basic ovarian cell functions; 2) are the first demonstration of importance of miR-152 in the control of these functions; 3) show the ability of apigenin to promote miR-152 expression and the ability of miR-152 to modify apigenin effects on ovarian cells.
Topics: Female; Swine; Animals; Progesterone; Insulin-Like Growth Factor I; Apigenin; Oxytocin; Dinoprostone; Cells, Cultured; Granulosa Cells; Estradiol; Cell Proliferation; Apoptosis; MicroRNAs
PubMed: 37354873
DOI: 10.1016/j.domaniend.2023.106805 -
Chemical Biology & Drug Design Jun 2023Cancer is a complicated malignancy controlled by numerous intrinsic and extrinsic pathways. There has been a significant increase in interest in recent years in the... (Review)
Review
Cancer is a complicated malignancy controlled by numerous intrinsic and extrinsic pathways. There has been a significant increase in interest in recent years in the elucidation of cancer treatments based on natural extracts that have fewer side effects. Numerous natural product-derived chemicals have been investigated for their anticancer effects in the search for an efficient chemotherapeutic method. Therefore, the rationale behind this review is to provide a detailed insights about the anticancerous potential of apigenin via modulating numerous cell signaling pathways. An ingestible plant-derived flavonoid called apigenin has been linked to numerous anticancerous potential in numerous experimental and biological studies. Apigenin has been reported to induce cell growth arrest and apoptotic induction by modulating multiple cell signaling pathways in a wider range of human tumors including those of the breast, lung, liver, skin, blood, colon, prostate, pancreatic, cervical, oral, and stomach. Oncogenic protein networks, abnormal cell signaling, and modulation of the apoptotic machinery are only a few examples of diverse molecular interactions and processes that have not yet been thoroughly addressed by scientific research. Thus, keeping this fact in mind, we tried to focus our review towards summarizing the apigenin-mediated modulation of oncogenic pathways in various malignancies that can be further utilized to develop a potent therapeutic alternative for the treatment of various cancers.
Topics: Male; Humans; Apigenin; Apoptosis; Neoplasms; Cell Proliferation; Signal Transduction; Cell Line, Tumor
PubMed: 36746671
DOI: 10.1111/cbdd.14206 -
The Kaohsiung Journal of Medical... Jul 2021The present study aimed to investigate the role of apigenin and the molecular mechanism of miR-152-5p and bromodomain containing 4 (BRD4) in the proliferation, invasion,...
The present study aimed to investigate the role of apigenin and the molecular mechanism of miR-152-5p and bromodomain containing 4 (BRD4) in the proliferation, invasion, and epithelial-mesenchymal transition (EMT) of cervical carcinoma cells. Quantitative real-time PCR was used to detect the transfection efficiency and the expression of miR-152-5p and BRD4. Western blotting was conducted to evaluate the protein level of BRD4, E-cadherin, N-cadherin, and MMP9. Luciferase reporter assay was performed to confirm whether miR-152-5p bound to BRD4. MTT and Transwell invasion assay were applied to determine the cell proliferation and invasion, respectively. MiR-152-5p was downregulated and BRD4 was upregulated in cervical carcinoma tissue. Besides, miR-152-5p could directly bind to BRD4 in Hela and CaSki cells. In addition, apigenin inhibited proliferation, invasion, and EMT of Hela and CaSki cells by regulating miR-152-5p/BRD4 axis. Apigenin suppresses proliferation, invasion, and induced EMT of cervical carcinoma cells by regulation of miR-152-5p/BRD4 axis.
Topics: Apigenin; Carcinoma; Cell Cycle Proteins; Cell Line, Tumor; Cell Movement; Cell Proliferation; Epithelial-Mesenchymal Transition; Female; Gene Expression Regulation, Neoplastic; HeLa Cells; Humans; MicroRNAs; Neoplasm Invasiveness; Nuclear Proteins; Tetrazolium Salts; Thiazoles; Transcription Factors; Uterine Cervical Neoplasms
PubMed: 33611824
DOI: 10.1002/kjm2.12370 -
TheScientificWorldJournal 2021Till date, there is no known antidote to cure diabetes mellitus despite the discovery and development of diverse pharmacotherapeutic agents many years ago. Technological... (Review)
Review
BACKGROUND
Till date, there is no known antidote to cure diabetes mellitus despite the discovery and development of diverse pharmacotherapeutic agents many years ago. Technological advancement in natural product chemistry has led to the isolation of analogs of vitexin and isovitexin found in diverse bioresources. These compounds have been extensively studied to explore their pharmacological relevance in diabetes mellitus. . The present review was to compile results from in vitro and in vivo studies performed with vitexin and isovitexin derivatives relating to diabetes mellitus and its complications. A systematic online literature query was executed to collect all relevant articles published up to March 2020.
RESULTS
In this piece, we have collected data and presented it in a one-stop document to support the multitargeted mechanistic actions of vitexin and isovitexin in controlling diabetes mellitus and its complications.
CONCLUSION
Data collected hint that vitexin and isovitexin work by targeting diverse pathophysiological and metabolic pathways and molecular drug points involved in the clinical manifestations of diabetes mellitus. This is expected to provide a deeper understanding of its actions and also serve as a catapult for clinical trials and application research.
Topics: Animals; Apigenin; Diabetes Complications; Diabetes Mellitus; Humans; Hypoglycemic Agents
PubMed: 33935599
DOI: 10.1155/2021/6641128 -
Molecules (Basel, Switzerland) Jun 2023Non-small cell lung cancer (NSCLC) is one of the leading cancer killers. Apigenin (Api) and Naringenin (Nar) are natural bioactive substances obtained in various...
Non-small cell lung cancer (NSCLC) is one of the leading cancer killers. Apigenin (Api) and Naringenin (Nar) are natural bioactive substances obtained in various vegetables and fruits, possessing anti-tumor effects across multiple studies. This study investigated the latent synergistic antiproliferative functions of Api and Nar in A549 and H1299 NSCLC cells. Cell viability was determined after incubating with different concentrations of Api, Nar, or the combination of Api and Nar (CoAN) for 24 h. Analysis using the CompuSyn software revealed that the CI value of each combined dose was < 1, depicting that the two drugs had a synergistic inhibitory effect. The CoAN (A:N = 3:2) group with the lowest CI value was selected for subsequent experiments. The IC of CoAN (A:N = 3:2) was used to determine the cell cycle, the expression ratio of Bax to Bcl2, Caspase 3 activity, and mitochondrial function to assess oxidative stress and apoptosis. The results established that CoAN treatment caused significant cytotoxicity with cell cycle arrest at G2/M phases. Furthermore, CoAN significantly enhanced mitochondria dysfunction, elevated oxidative stress, and activated the apoptotic pathway versus Api or Nar alone groups. Thus, the CoAN chemotherapy approach is promising and deserves further research.
Topics: Humans; Carcinoma, Non-Small-Cell Lung; Apigenin; Lung Neoplasms; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Synergism
PubMed: 37446609
DOI: 10.3390/molecules28134947 -
Molecular Diversity Dec 2022Sirtuins (SIRTs) overexpression serves as a potential therapeutic target for TNBC because it is associated with bioactivities of cancer stem cells (CSCs), resistance to...
Sirtuins (SIRTs) overexpression serves as a potential therapeutic target for TNBC because it is associated with bioactivities of cancer stem cells (CSCs), resistance to chemotherapy, and metastasis. Irrespective of the availability of synthetic SIRT inhibitors, new SIRT inhibitors with enhanced potency and lesser side effects serve as current unmet needs. Therefore, bioactive dietary compounds; kaempferol (KMP) and apigenin (API) were investigated for their anti-SIRTs potential. We observed KMP and API inhibits cellular proliferation by DNA damage and S-phase cell cycle arrest in TNBC Cells. They also suppress stemness properties in TNBCs as observed in experiments of mammosphere formation and clonogenic potential. Our mechanistic approach indicated that KMP and API inhibited SIRT3 and SIRT6 proteins, as evidenced by our in silico and in vitro experiment. Collectively, our studies suggest that KMP and API are promising candidates to be further developed as sirtuin modulators against TNBCs.
Topics: Humans; Sirtuins; Apigenin; Kaempferols; Triple Negative Breast Neoplasms; Neoplastic Stem Cells; Cell Line, Tumor
PubMed: 35129762
DOI: 10.1007/s11030-022-10384-x