Glechomae Herba, the dried aerial part of Glechoma longituba(Labiatae), has the effects of promoting urination, draining dampness, and relieving stranguria. It has received wide attention in recent years owing to the satisfactory efficacy on lithiasis. Amid the in-depth chemical and pharmacological research, it has been found that Glechomae Herba has antibacterial, anti-inflammatory, antioxidant, antithrombotic, hepatoprotective, cholagogic, antitumor, hypoglycemic, and lipid-lowering effects. The main chemical constituents are volatile oils, flavonoids, terpenoids, phenylpropanoids, and organic acids. This paper summarized the chemical constituents and pharmacological effects of Glechomae Herba. Based on genetic relationship of plants, the characteristics, efficacy, and pharmacokinetics of the chemical constituents, and the potential of these constituents as quality markers(Q-markers), it was summed up that ursolic acid, caffeic acid, rosmarinic acid, luteolin-7-O-diglucuronide, apigenin, apigenin-7-O-diglucuronide, apigetrin, and glechone can be the candidate Q-markers of Glechomae Herba.
Apigenin ; Plant Extracts/pharmacology* ; Lamiaceae ; Drugs, Chinese Herbal/pharmacology* ; Flavonoids/pharmacology*

Vitexin, a naturally occurring flavone glycoside in plants, has many pharmacological effects, which is widely distributed in nature. This paper reviewed the research progress of the distribution of vitexin in the plant resources and its pharmacological effects, and summarized its application prospects, aiming to provide a useful reference for the development of vitexin-enriched plant resources.
Animals ; Antineoplastic Agents ; pharmacology ; Antioxidants ; pharmacology ; Apigenin ; pharmacology ; Humans ; Hypoglycemic Agents ; pharmacology ; Myocardial Infarction ; drug therapy ; Plant Dispersal

OBJECTIVETo explore the effect of apigenin on semen parameters in male mice.

METHODSTotally 100 healthy male mice of Kunming strain were randomly divided into 5 groups according to the body weight: negative control, solvent control, low-dose apigenin, median-dose apigenin and high-dose apigenin, the latter three groups given intragastric apigenin at a fixed time every day for 7 and 14 days. At 35 days after the first medication, all the mice were killed and detected for the sperm motion parameters by computer aided sperm analysis (CASA).

RESULTSThere were no statistically significant differences in sperm motion parameters, density and motility between the negative control and the three apigenin groups after 7-day medication. At 14 days, the high-dose apigenin group showed remarkable decreases in average path velocity (VAP), straight line velocity (VSL), straightness (STR), wobbliness (WOB), the percentage of grade b sperm and sperm motility, and a significant increase in beat cross frequency (BCF) as compared with the negative control group (P < 0.05).

CONCLUSIONApigenin affects sperm motility in male mice to a certain extent.

Animals ; Apigenin ; pharmacology ; Male ; Mice ; Mice, Inbred Strains ; Semen ; drug effects ; Sperm Motility ; drug effects

OBJECTIVETo study chemical constituents of Incarvillea arguta and their accelerating PC-12 cell differentiation.

METHODThe constituents were isolated and repeatedly purified on silica gel column chromatography, and were identified on the basis of physicochemical and spectroscopic analysis. The neurotrophic activity of different portion and all purified compounds from I. arguta was determined on the model of PC-12 cell.

RESULTFive compounds were isolated from BuOH portion of alcohol extraction of I. arguta. Their structures were identified as plantarenaloside (I), 5-hydroxy-4', 6 7-trimethoxy-flavone (II), 4', 5-dihydroxy-6, 7-dimethoxyflavone (III), 4', 5-dihydroxy-7-methoxyflavone (IV), 5-dydroxy-4', 7-dimethoxyflavone (V).

CONCLUSIONCompound I is isolated from the plant for the first time and it has neurotrophic activity for PC-12 cell. Compounds II approximately V are isolated from the genus Incarvillea for the first time.

Animals ; Apigenin ; isolation & purification ; pharmacology ; Bignoniaceae ; chemistry ; Cell Transformation, Neoplastic ; drug effects ; Flavones ; isolation & purification ; pharmacology ; PC12 Cells ; Rats

OBJECTIVETo investigate the antitumor effect of apigenin on human lung cancer cells.

METHODSThe anti-proliferation and sensitization effects of apigenin on human lung cancer cells was accessed by counting cells after Trypan blue staining and MTS assay.

RESULTS(1) Apigenin significantly suppressed the proliferation of four types of human lung cancer cells (A549:P=0.041, H460:P=0.050, LTEP-a2:P=0.039, H292:P=0.016); (2) Apigenin significantly increased the susceptibility of human lung cancer cells to antitumor drugs (P<0.05 or P<0.01) in a synergistic way (almost all of the combination index values are less than 1).

CONCLUSIONApigenin widely inhibits cell proliferation of various lung cancer cell lines in a dose-dependent manner and the combination treatment of apigenin and antitumor drugs is very effective in human lung cancer cells, and Nrf2-ARE pathway may contribute to the mechanism.

Antineoplastic Agents ; pharmacology ; Apigenin ; pharmacology ; Cell Line, Tumor ; drug effects ; Cell Proliferation ; drug effects ; Drug Synergism ; Humans ; Lung Neoplasms ; pathology

Animals ; Apigenin ; pharmacology ; Female ; Follicle Stimulating Hormone ; blood ; Gonadotropin-Releasing Hormone ; blood ; Luteinizing Hormone ; blood ; Phytoestrogens ; pharmacology ; Rats

OBJECTIVETo study on the chemical constituents of Lobelia chinensis.

METHODThe coloumn chromatographic techniques were applied to isolate constituents, and their structures were elucidated by means of spectral data analysis.

RESULTSixteen compounds were isolated and identified as daucosterol (1), diosmetin (2), apigenin (3), chrysoeriol (4), loteolin (5), hesperidin (6), loteolin-7-O-beta-D-glucoside (7), apigenin-7-O-beta-D-glucoside (8), linarin (9), diosmin(10), 5,7-dimethoxy-8- hydroxycoumarin (11), palmitinic acid (12), lacceroic acid (13), stearic acid (14), beta-sitosterol (15), daucosterol (16).

CONCLUSIONAll of these compouds were obtained from L. chinensis for the first time.

Apigenin ; analysis ; Cholestenones ; analysis ; Flavones ; Flavonoids ; analysis ; Glycosides ; analysis ; Hesperidin ; analysis ; Lobelia ; chemistry ; Plant Extracts ; pharmacology ; Sitosterols ; analysis

Cancer is a major health concern and leading burden on economy worldwide. An increasing effort is devoted to isolation and development of plant-derived dietary components as effective chemo-preventive products. Phytochemical compounds from natural resources such as fruits and vegetables are responsible for decreasing the risk of certain cancers among the consuming populations. Apigenin, a flavonoid phytochemical found in many kinds of fruits and vegetables, has been shown to exert significant biological effects, such as anti-oxidant, anti-inflammatory and most particularly anti-neoplastic properties. This review is intended to summarize the most recent advances in the anti-proliferative and chemo-preventive effects of apigenin in different cancer models. Analysis of the data from the studied cancer models has revealed that apigenin exerts its anti-proliferative effects through multiple and complex pathways. This guided us to discover some controversial results about the exact role of certain molecular pathways such as autophagy in the anticancer effects of apigenin. Further, there were cumulative positive evidences supporting the involvement of certain pathways such as apoptosis, ROS and DNA damage and repair. Apigenin possesses a high potential to be used as a chemosensitizing agent through the up-regulation of DR5 pathway. According to these preclinical findings we recommend that further robust unbiased studies should consider the possible interactions between different molecular pathways.
Animals ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; Apigenin ; chemistry ; pharmacology ; Apoptosis ; drug effects ; Autophagy ; drug effects ; Humans ; Neoplasms ; drug therapy ; genetics ; metabolism ; physiopathology ; Phytochemicals ; chemistry ; pharmacology

This study aimed to evaluate the biological effect and mechanism of Vernonia anthelmintica Injection(VAI) on melanin accumulation. The in vivo depigmentation model was induced by propylthiouracil(PTU) in zebrafish, and the effect of VAI on melanin accumulation was evaluated based on the in vitro B16F10 cell model. The chemical composition of VAI was identified according to the high-performance liquid chromatography quadrupole-time-of-flight tandem mass spectrometry(UPLC-Q-TOF-MS). Network pharmaco-logy was applied to predict potential targets and pathways of VAI. A "VAI component-target-pathway" network was established, and the pharmacodynamic molecules were screened out based on the topological characteristics of the network. The binding of active molecules to key targets was verified by molecular docking. The results showed that VAI promoted tyrosinase activity and melanin production in B16F10 cells in a dose-and time-dependent manner and could restore the melanin in the body of the zebrafish model. Fifty-six compounds were identified from VAI, including flavonoids(15/56), terpenoids(10/56), phenolic acids(9/56), fatty acids(9/56), steroids(6/56), and others(7/56). Network pharmacological analysis screened four potential quality markers, including apigenin, chrysoeriol, syringaresinol, and butein, involving 61 targets and 65 pathways, and molecular docking verified their binding to TYR, NFE2L2, CASP3, MAPK1, MAPK8, and MAPK14. It was found that the mRNA expression of MITF, TYR, TYRP1, and DCT in B16F10 cells was promoted. By UPLC-Q-TOF-MS and network pharmacology, this study determined the material basis of VAI against vitiligo, screened apigenin, chrysoeriol, syringaresinol, and butein as the quality markers of VAI, and verified the efficacy and internal mechanism of melanogenesis, providing a basis for quality control and further clinical research.
Animals ; Vernonia/chemistry* ; Melanins/metabolism* ; Zebrafish/metabolism* ; Network Pharmacology ; Molecular Docking Simulation ; Apigenin/pharmacology* ; Drugs, Chinese Herbal/pharmacology* ; Chromatography, High Pressure Liquid

Oxidative stress plays an important role in the pathogenesis of aminoglycoside-induced hearing loss and represents a promising target for treatment. We tested the potential effect of apigenin, a natural flavonoid with anticancer, anti-inflammatory, and antioxidant activities, on neomycin-induced ototoxicity in cochlear hair cells in vitro. Results showed that apigenin significantly ameliorated the loss of hair cells and the accumulation of reactive oxygen species upon neomycin injury. Further evidence suggested that the nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway was activated by apigenin treatment. Disruption of the Nrf2 axis abolished the effects of apigenin on the alleviation of oxidative stress and subsequent apoptosis of hair cells. This study provided evidence of the protective effect of apigenin on cochlear hair cells and its underlying mechanism.
Apigenin/pharmacology* ; Apoptosis ; Hair Cells, Auditory/metabolism* ; Humans ; NF-E2-Related Factor 2/pharmacology* ; Neomycin ; Oxidative Stress ; Reactive Oxygen Species/metabolism* ; Signal Transduction