Actinidia arguta Extract Containing Myo-Inositol Suppresses TNF-α-Induced VCAM-1 Expression and Monocyte Adhesion to Endothelial Cells via Inhibition of the PTEN/Akt/GSK-3ß and NF-κB Signaling Pathways.

The primary inflammatory process in atherosclerosis, a major contributor to cardiovascular disease, begins with monocyte adhering to vascular endothelial cells. Actinidia arguta (kiwiberry) is an edible fruit that contains various bioactive components. While A. arguta extract (AAE) has been recognized for its anti-inflammatory characteristics, its specific inhibitory effect on early atherogenic events has not been clarified. We used tumor necrosis factor-α (TNF-α)-stimulated human umbilical vein endothelial cells (HUVECs) for an in vitro model. AAE effectively hindered the attachment of THP-1 monocytes and reduced the expression of vascular cell adhesion molecule-1 (VCAM-1) in HUVECs. Transcriptome analysis revealed that AAE treatment upregulated phosphatase and tensin homolog (PTEN), subsequently inhibiting phosphorylation of AKT and glycogen synthase kinase 3ß (GSK3ß) in HUVECs. AAE further hindered phosphorylation of AKT downstream of the nuclear factor kappa B (NF-κB) signaling pathway, leading to suppression of target gene expression. Oral administration of AAE suppressed TNF-α-stimulated VCAM-1 expression, monocyte-derived macrophage infiltration, and proinflammatory cytokine expression in C57BL/6 mouse aortas. Myo-inositol, identified as the major compound in AAE, played a key role in suppressing THP-1 monocyte adhesion in HUVECs. These findings suggest that AAE could serve as a nutraceutical for preventing atherosclerosis by inhibiting its initial pathogenesis.

Explore the active ingredients and potential mechanism of action on Actinidia arguta leaves against T2DM by integration of serum pharmacochemistry and network pharmacology.

BACKGROUND: Actinidia arguta leaves (AAL) are traditionally consumed as a vegetable and as tea in folk China and Korea. Previous studies have reported the anti-diabetic effect of AAL, but its bioactive components and mechanism of action are still unclear. AIM OF THE STUDY: This study aims to identify the hypoglycemic active components of AAL by combining serum pharmacochemistry and network pharmacology and to elucidate its possible mechanism of action. METHODS: Firstly, the effective components in mice serum samples were characterized by UPLC-Q/TOF-MSE. Furthermore, based on these active ingredients, network pharmacology analysis was performed to establish an "H-C-T-P-D" interaction network and reveal possible biological mechanisms. Finally, the affinity between serum AAL components and the main proteins in the important pathways above was investigated through molecular docking analysis. RESULTS: Serum pharmacochemistry analysis showed that 69 compounds in the serum samples were identified, including 23 prototypes and 46 metabolites. The metabolic reactions mainly included deglycosylation, dehydration, hydrogenation, methylation, acetylation, glucuronidation, and sulfation. Network pharmacology analysis showed that the key components quercetin, pinoresinol diglucoside, and 5-O-trans-p-coumaroyl quinic acid butyl ester mainly acted on the core targets PTGS2, HRAS, RELA, PRKCA, and BCL2 targets and through the PI3K-Akt signaling pathway, endocrine resistance, and MAPK signaling pathway to exert a hypoglycemic effect. Likewise, molecular docking results showed that the three potential active ingredients had good binding effects on the five key targets. CONCLUSION: This study provides a basis for elucidating the pharmacodynamic substance basis of AA against T2DM and further exploring the mechanism of action.

Transcriptomic analysis reveals ozone treatment delays kiwifruit postharvest softening by modulating cell wall metabolism.

Kiwifruit ripening and senescence after harvesting are closely related to its economic value. Transcriptome analysis and biochemical parameters were used to investigate the differences in gene expression levels and the potential regulation of cell wall metabolism in kiwifruit treated with ozone, thereby regulating fruit softening and prolonging postharvest life. Compared to the control group, the activities of the cell wall modification enzyme were lower under ozone treatment, the content of polysaccharide in the cell wall of primary pectin and cellulose was higher, and the content of soluble pectin was lower. Meanwhile, ozone treatment delayed the degradation of the cell wall mesosphere during storage. A total of 20 pectinesterase (PE)-related genes were identified by sequencing analysis. The data analysis and quantitative polymerase chain reaction results confirmed that cell wall modifying enzyme genes played an important role in softening and senescence after harvesting, which may reduce or induce the expression of certain genes affecting cell wall metabolism. Ozone treatment not only regulates active genes such as xyloglucan endo glycosyltransferase/hydrolase, cellulose synthase, polygalacturonase, and PE to maintain the quality of fruit after harvest but also acts synergically with cell wall modifying enzymes to inhibit the degradation of cell wall, resulting in changes in the ultrastructure of cell wall, thereby reducing the hardness of kiwifruit. In addition, according to the results of cis-acting elements, cell wall degradation is also related to downstream hormone signaling, especially PE-related genes. These results provide a theoretical basis for studying the mechanism of firmness and cell wall metabolism difference of kiwifruit and also lay a good foundation for further research.

Development of a polyphenol-enriched whole kiwifruit dietary supplement and its potential in ameliorating hyperlipidemia.

BACKGROUND: Kiwifruit pomace, which contains abundant phenolic compounds, is typically discarded during the juicing process, leading to wastage of valuable resources. To address this issue, various indicators (including total acidity, sugar/acid ratio, vitamin C, total polyphenols, polyphenol monomers, and soluble solids content) of 15 kiwifruit cultivars were evaluated and juiced. Then, a polyphenol-concentrated solution from kiwifruit pomace was backfilled into kiwi juice to prepare whole nutritious compound kiwi juice, and its anti-hyperlipidemic activity on obese model mice was then investigated. RESULTS: Through grey relational analysis and the technique for order preference by similarity to an ideal solution (TOPSIS), Kuimi and Huayou were identified as the predominant varieties for juicing, with weighted relevance scores of 0.695 and 0.871 respectively and TOPSIS scores of 0.6509 and 0.8220 respectively. The polyphenol content of Cuixiang pomace was 43.97 mg g-1 , making it the most suitable choice for polyphenol extraction. By backfilling a polyphenol-concentrated solution derived from Cuixiang pomace into compound kiwi juice of Huayou and Kuimi, the whole nutritious compound kiwi juice with polyphenols was produced and exhibited superior bioactivities, including enhanced hepatic oxidative stress defense, and alleviated serum lipid abnormalities. Furthermore, whole nutritious compound kiwi juice with polyphenols ameliorated host intestinal microbiota dysbiosis by increasing the relative abundance of the phyla Bacteroidota and Verrucomicrobiota. CONCLUSION: A hypolipidemic dietary supplement based on kiwifruit pomace polyphenols has been successfully developed, providing an effective solution for hyperlipidemia intervention. © 2023 Society of Chemical Industry.

Efficient three phase partitioning of actinidin from kiwifruit (Actinidia deliciosa) and its characterization.

Three phase partitioning (TPP) method was effectively utilized for the extraction and purification of milk clotting protease (actinidin) from the kiwifruit pulp. The different purification parameters of TPP such as ammonium sulfate saturation, ratio of the crude kiwifruit extract to tert-butanol, and the pH value of extract were optimized. The 40% (w/v) salt saturation having 1.0:0.75 (v/v) ratio of crude kiwifruit extract to tert-butanol at 6.0 pH value exhibited 3.14 purification fold along with 142.27% recovery, and the protease was concentrated exclusively at intermediate phase (IP). This fraction showed milk-clotting activity (MCA), but there was no such activity in lower aqueous phase (AP). The enzyme molecular weight was found to be 24 kDa from Tricine SDS-PAGE analysis. Recovered protease demonstrated greater stability at pH 7.0 and temperature 50 °C. The Vmax and Km values were 121.9 U/ml and 3.2 mg/ml respectively. Its cysteine nature was demonstrated by inhibition studies. This study highlighted that the TPP is an economic and effective method for extraction and purification of actinidin from kiwifruit, and it could be used as a vegetable coagulant for cheesemaking.

Actinidia arguta (Sieb. et Zucc.) Planch. ex Miq.: A Review of Phytochemistry and Pharmacology.

Actinidia arguta (Siebold & Zucc.) Planch ex Miq. (A. arguta) is a highly valued vine plant belonging to the Actinidia lindl genus. It is extensively utilized for its edible and medicinal properties. The various parts of A. arguta serve diverse purposes. The fruit is rich in vitamins, amino acids, and vitamin C, making it a nutritious and flavorful raw material for producing jam, canned food, and wine. The flowers yield volatile oils suitable for essential oil extraction. The leaves contain phenolic compounds and can be used for tea production. Additionally, the roots, stems, and leaves of A. arguta possess significant medicinal value, as they contain a wide array of active ingredients that exert multiple pharmacological and therapeutic effects. These effects include quenching thirst, relieving heat, stopping bleeding, promoting blood circulation, reducing swelling, dispelling wind, and alleviating dampness. Comprehensive information on A. arguta was collected from scientific databases covering the period from 1970 to 2023. The databases used for this review included Web of Science, PubMed, ProQuest, and CNKI. The objective of this review was to provide a detailed explanation of A. arguta from multiple perspectives, such as phytochemistry and pharmacological effects. By doing so, it aimed to establish a solid foundation and propose new research ideas for further exploration of the plant's potential applications and industrial development. To date, a total of 539 compounds have been isolated and identified from A. arguta. These compounds include terpenoids, flavonoids, phenolics, phenylpropanoids, lignin, organic acids, volatile components, alkanes, coumarins, anthraquinones, alkaloids, polysaccharides, and inorganic elements. Flavonoids, phenolics, alkaloids, and polysaccharides are the key bioactive constituents of A. arguta. Moreover, phenolics and flavonoids in A. arguta exhibit remarkable antioxidant, anti-inflammatory, and anti-tumor properties. Additionally, they show promising potential in improving glucose metabolism, combating aging, reducing fatigue, and regulating the immune system. While some fundamental studies on A. arguta have been conducted, further research is necessary to enhance our understanding of its mechanism of action, quality evaluation, and compatibility mechanisms. A more comprehensive investigation is highly warranted to explore the mechanism of action and expand the range of drug resources associated with A. arguta. This will contribute to the current hot topics of anti-aging and anti-tumor drug research and development, thereby promoting its further development and utilization.

In vitro anticholinergic and antiglycaemic properties of frost-hardy Actinidia fruit extracts and their polyphenol profile, L-ascorbic acid content and antioxidant capacity.

The aim of this study was to investigate the inhibitory effects of Actinidia arguta ('Weiki', 'Skarlet September Kiwi') and Actinidia kolomikta ('Lande') fruit extracts against advanced glycation end-products (AGEs) formation and acetylcholinesterase (AChE) activity. The extracts were also tested regarding polyphenol profile and Lascorbic acid content (UHPLC-DAD-MS), and antioxidant capacity (DPPH, ABTS). 'Scarlet September Kiwi' showed the strongest anti-AGEs activity studied with BSAGLU (IC50 = 2.68) and BSA-MGO (IC50 = 18.06) models. The highest anti-AChE activity was found for the 'Lande' extract (IC50 = 4.56). 'Lande' showed the highest L-ascorbic acid content (8271.96 µg/g dw), ABTS (312.42 µmol TE/g dw) and DPPH (282.01 µmol TE/g dw) values. 'Scarlet September Kiwi' revealed the highest individual phenolics concentration (2321.43 µg/g dw). The contents of (+)-catechin and L-ascorbic acid were significantly correlated with anti-AChE activity. This research sheds new light on the bioactivity of Actinidia arguta and Actinidia kolomikta fruit elucidating the role of (+)-catechin and L-ascorbic acid in prevention of Alzheimer's disease.

Nontargeted metabolomic analysis of four different parts of Actinidia arguta by UPLC-Q-TOF-MSE.

Actinidia arguta, an edible berry plant with high nutritional values, has been widely used in Asian countries as a food and traditional medicinal herb. The well-recognized health-promoting properties of A. arguta were associated with its bioactive components in its different botanical parts. To rapidly screen and identify chemical components and simultaneously determine the potential metabolites from different parts of A. arguta, UPLC-Q-TOF-MSE coupled with UNIFI platform and multivariate statistical analysis approach was established in this study. As a result, a total of 107 components were identified from the four different parts of A. arguta, in which 31 characteristic chemical markers were discovered among them, including 12, 8, 6, and 5 compounds from the fruits, leaves, roots, and stems, respectively. These results suggested that the combination of UPLC-Q-TOF-MSE and metabolomic analysis is a powerful method to rapidly screen characteristic markers for the quality control of A. arguta.

Dwarf Kiwi (Actinidia arguta Miq.), a Source of Antioxidants for a Healthy and Sustainable Diet.

The feasibility of using dwarf kiwi fruits (Actinia arguta Miq.) as a healthy and sustainable food, compared to other types of commercial kiwi fruits, was evaluated in the present study. The overall antioxidant capacity of these fruits was assessed by either extraction-dependent methods (ABTS, ORAC) or the direct method called Quick, Easy, New, CHEap, Reproducible (QUENCHER) (DPPH, FRAP, Folin-Ciocalteu), applied for the first time to analyze kiwi fruits. With this methodology, all the molecules with antioxidant capacity are measured together in a single step, even those with high molecular weight or poor solubility in aqueous extraction systems, such as antioxidant dietary fiber. The effect of kiwi extracts on physiological and induced intracellular reactive oxygen species (ROS) production on IEC-6 cells was also analyzed, as well as total phenolic content (TPC) by Fast Blue BB, flavonols, hydroxycinnamic acids, and hydroxybenzoic acids. A. arguta fruits showed the highest values in all the antioxidant assays, being remarkably higher than the other kiwi species for Q-FRAP and Q-DPPH. Dwarf kiwi showed the highest potential in reducing physiological ROS and the highest values of TPC (54.57 mgGAE/g), being hydroxybenzoic acids the main phenolic family found (2.40 mgGAE/g). Therefore, dwarf kiwi fruits are a natural source of antioxidants compared to conventional kiwi fruits, being a sustainable and healthy alternative to diversify fruits in the diet.

One-time ozone treatment improves the postharvest quality and antioxidant activity of Actinidia arguta fruit.

The major aim of this study was to check the effect of one-time ozonation on selected quality parameters and antioxidant status of Actinidia arguta fruit. For this purpose, A. arguta fruit was ozonated with gas at a concentration of 10 and 100 ppm, which was carried out successively for 5, 15 and 30 min. Next, the selected quality attributes, antioxidants level as well as NADPH and mitochondrial energy metabolism in mini-kiwi fruit after ozonation were analysed. Our research has shown that ozonation reduced the level of yeast and mould without affecting the content of soluble solids or acidity. In turn, ozonation clearly influenced the antioxidant activity and the redox status of the fruit. The ozonated fruit was characterised by a lower level of ROS due to the higher level of low molecular weight antioxidants, as well as the higher activity of superoxide dismutase and catalase. In addition, improved quality and antioxidant activity of the fruit were indirectly due to improved energy metabolism and NADPH level. The ozonated fruit showed a higher level of ATP, due to both higher activity of succinate dehydrogenase and higher availability of NADH. Moreover, the increased level of NAD+ and the activity of NAD+ kinase and glucose-6-phosphate dehydrogenase contributed to higher levels of NADPH in the fruit.

Actinidin diversity: discovery of common and selective substrates for actinidin isoforms and Actinidia cultivars.

The actinidin proteinase family has a striking sequence diversity; isoelectric points range from 3.9 to 9.3. The biological drive for this variation is thought to be actinidin's role as a defense-related protein. In this study we map mutations in the primary sequence onto the 3D structure of the protein and show that the region with the highest diversity is close to the substrate binding groove. Non-conservative substitutions in the active site determine substrate preference and therefore create problems for quantification of actinidin activity. Here we use a peptide substrate library to compare two actinidin isoforms, one from the kiwiberry cultivar 'Hortgem Tahi' (Actinidia arguta), and the other from the familiar kiwifruit cultivar 'Hayward' (Actinidia chinensis var. deliciosa). Among 360 octamer substrates we find one substrate (RVAAGSPI) with the useful property of being readily cleaved by all the functionally active actinidins in a set of A. arguta and A. chinensis var. deliciosa isoforms. In addition, we find that two substrates (LPPKSQPP & ILRDKDNT) have the ability to differentiate different isoforms from a single fruit. We compare actinidins from 'Hayward' and A. arguta for their ability to digest the allergenic gluten peptide (PFPQPQLPY) but find the peptide to be indigestible by all sources of actinidin. The ability to inactivate salivary amylase is shown to be a common trait in Actinidia cultivars due to proteolysis by actinidin and is particularly strong in 'Hortgem Tahi'. A mixture of 10% 'Hortgem Tahi' extract with 90% saliva inactivates 100% of amylase activity within 5 minutes. Conceivably, 'Hortgem Tahi' might lower the glycaemic response in a meal rich in cooked starch.

Oral care tablet containing kiwifruit powder affects tongue coating microbiome.

OBJECTIVES: Tongue coating, a kind of biofilm formed on the tongue dorsum, is the cause of various clinical conditions, such as oral halitosis and periodontal diseases, because Fusobacterium nucleatum acts as a bridge between other oral bacteria and periodontopathogenic bacteria in biofilm formation. Our previous clinical study revealed that taking oral care tablets containing kiwifruit powder significantly reduced not only tongue-coating index and volatile sulfur compounds but also total bacteria and F. nucleatum in tongue coating. In this study, we analyzed the microbiome of tongue coating samples obtained before and after oral care tablets intake to clarify whether this tablet is a useful tool for daily tongue care. METHODS: Thirty-two healthy young adults were enrolled, and a crossover clinical trial was conducted. We instructed subjects to remove tongue coating by tongue brush for intervention I, to keep the oral care tablet containing kiwifruit powder on the tongue dorsum and to let it dissolve naturally for intervention II. Microbial DNA was isolated from the collected tongue coating samples in each subject, then 16S rRNA next-generation sequencing, operational taxonomic unit clustering, and statistical analysis were performed. RESULTS: The microbiome analysis revealed that the oral care tablet in intervention II prompted a significant change in the tongue microbiota composition, a significant reduction in the relative abundance of Prevotella and Porphyromonas, and an increase in Firmicutes/Bacteroidetes ratio when compared to that in intervention I. CONCLUSION: These results suggested that the oral care tablet might contribute to the improvement of the oral condition due to its good influence on the tongue coating microbiome.

Changes in metabolites and antioxidant activities of green 'Hayward' and gold 'Haegeum' kiwifruits during ripening with ethylene treatment.

Fruit ripening involves changes in physical, physiological, biochemical, and metabolic activities through the actions of enzymes and regulatory genes. In this study, we elucidate primary and secondary metabolites and antioxidant activities of green 'Hayward' and gold 'Haegeum' kiwifruit cultivars during ripening by comparing ethylene-treated fruit to the control. A total of 36 primary metabolites (20 amino acids, 9 fatty acids, 4 organic acids, and 3 sugars) were identified to be altered significantly during the ripening of both cultivars. Significant changes in secondary metabolites such as total phenols, flavonoids, and vitamin C were also observed during the ripening of both cultivars. Moreover, antioxidant activity assays showed that ripening either maintains or increases the antioxidant activity of kiwifruit cultivars. These findings could assist the fruit industry in developing metabolic markers for indication of the optimum kiwifruit ripening quality and postharvest decisions for storage, distribution, and marketing.

Actinidia chinensis Planch Root extract suppresses the growth and metastasis of hypopharyngeal carcinoma by inhibiting E2F Transcription Factor 1-mediated MNX1 antisense RNA 1.

Increasing evidence has shown that traditional Chinese medicines and their bioactive components exert an anti-tumor effect, representing a novel treatment strategy. Actinidia chinensis Planch Root extracts (acRoots) have been reported to repress cancer cell proliferation and metastasis. The effect of acRoots on hypopharyngeal carcinoma progression was explored in this study. Firstly, data from MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and colony formation assays showed that incubation with accRoots reduced cell proliferation of hypopharyngeal carcinoma cells. Moreover, acRoots promoted the cell apoptosis of hypopharyngeal carcinoma. Secondly, cell migration and invasion of hypopharyngeal carcinoma cells were suppressed by acRoots. Thirdly, E2F1 (E2F Transcription Factor 1) and lncRNA MNX1-AS1 (MNX1 antisense RNA 1) were up-regulated in hypopharyngeal carcinoma tissues, and reduced in hypopharyngeal carcinoma cells post acRoots incubation. Overexpression of E2F1 attenuated acRoots-induced decrease in MNX1-AS1 in hypopharyngeal carcinoma cells. Lastly, administration with acRoots retarded in vivo hypopharyngeal carcinoma growth through down-regulation of E2F1-mediated MNX1-AS1. In conclusion, acRoots exerted tumor-suppressive role in hypopharyngeal carcinoma through inhibition of E2F1-mediated MNX1-AS1.

Correction of Temperature Variation with Independent Water Samples to Predict Soluble Solids Content of Kiwifruit Juice Using NIR Spectroscopy.

Using the framework of aquaphotomics, we have sought to understand the changes within the water structure of kiwifruit juice occurring with changes in temperature. The study focuses on the first (1300-1600 nm) and second (870-1100 nm) overtone regions of the OH stretch of water and examines temperature differences between 20, 25, and 30 °C. Spectral data were collected using a Fourier transform-near-infrared spectrometer with 1 mm and 10 mm transmission cells for measurements in the first and second overtone region, respectively. Water wavelengths affected by temperature variation were identified. Aquagrams (water spectral patterns) highlight slightly different responses in the first and second overtone regions. The influence of increasing temperature on the peak absorbance of the juice was largely a lateral wavelength shift in the first overtone region and a vertical amplitude shift in the second overtone region of water. With the same data set, we investigated the use of external parameter orthogonalisation (EPO) and extended multiple scatter correction (EMSC) pre-processing to assist in building temperature-independent partial least square regression models for predicting soluble solids concentration (SSC) of kiwifruit juice. The interference component selected for correction was the first principal component loading measured using pure water samples taken at the same three temperatures (20, 25, and 30 °C). The results show that the EMSC method reduced SSC prediction bias from 0.77 to 0.1 °Brix in the first overtone region of water. Using the EPO method significantly reduced the prediction bias from 0.51 to 0.04 °Brix, when applying a model made at one temperature (30 °C) to measurements made at another temperature (20 °C) in the second overtone region of water.

Harnessing the Power of Kiwifruit for Radiosensitization of Melanoma.

BACKGROUND: Melanoma is the deadliest variant of skin cancer and its incidence continues to increase. There are limited treatment options for advanced and metastatic cases of melanoma, despite advances in immunotherapy and chemotherapy. Melanoma is notorious as a radioresistant tumor. Previous studies found that phytochemicals, such as resveratrol and those found in green tea and blueberry, can sensitize various cancer cells, including melanoma, to radiotherapy. Our previous study also revealed that kiwifruit extract (KE) has antitumor activity to melanoma cells. This study was designed to expand upon our previous investigation and determine KE's potential as a radiosensitizer on CRL-11147 melanoma cancer cells and elucidate the possible mechanisms behind its potential. MATERIALS AND METHODS: Proliferation and apoptosis of CRL-11147 melanoma cells under radiation therapy (RT) plus KE versus RT alone were investigated using Proliferative cell nuclear antigen (PCNA) staining, quick cell proliferation assay, clonogenic assay, and caspase-3 activity assay. Reverse transcription-polymerase chain reaction (RT-PCR) and immunohistochemistry (IHC) were then used to investigate the mechanisms behind the observed results. RESULTS: The percentage of CRL-11147 colonies, PCNA staining intensity, and the optic density value of CRL-11147 cells decreased with RT/KE vs. RT alone. Relative caspase-3 activity was increased with RT/KE vs. RT alone. Increased expression of the anti-proliferative molecule p27 and pro-apoptotic molecule TRAILR1 correlated with the anti-tumor effect seen in the RT/KE group versus the RT alone group. CONCLUSION: KE augments radiosensitivity of CRL-11147 by up-regulating both p27 and TRAILR1 to inhibit proliferation and increase apoptosis, respectively.

The bioactive ingredients in Actinidia chinensis Planch. Inhibit liver cancer by inducing apoptosis.

ETHNOPHARMACOLOGICAL RELEVANCE: Actinidia chinensis Planch. (ACP) is a common traditional Chinese medicine, which is mostly used for cancer treatment clinically. Liver cancer is a refractory tumor with a high incidence. Although ACP has been reported in the treatment of liver cancer, its possible mechanism of action is little known. AIM OF STUDY: The aim of this paper was to investigate the active components of ACP in the treatment of liver cancer and the related mechanisms by a network pharmacology approach. METHODS: The active components of ACP and the corresponding targets were obtained from multiple databases. Cytoscape software and STRING database were used to build the "herb-component-target (H-C-T)" network and protein-protein interactions (PPI) network. The key components and targets were further predicted by the Cytohubba plug-in in Cytoscape. Then, experiments were carried out on HepG2 cell line and Huh7 cell line to verify the effects and related mechanisms of the key compounds in ACP. RESULTS: 28 active components in ACP and 1299 related targets were screened out according to two indicators, oral bioavailability (OB) and drug-likeness (DL). The key compounds predicted include rutinum, astragalin, and L-epicatechin, and the main signaling pathways focus on apoptosis. Astragalin, a key compound in ACP, could inhibit the expression of Bcl-2, up-regulate the expression of Bax, cleaved caspase 3, cleaved caspase 8, and cleaved caspase 9, and regulate the apoptosis signaling pathway to inhibit the proliferation of liver cancer cells to play a therapeutic role in anti-liver cancer. CONCLUSIONS: These results suggest that ACP can alleviate the progression of liver cancer through the mechanisms predicted by network pharmacology, and provide a basis for the further understanding of the application of ACP in anti-cancer.

Bioactivities of Phenolic Compounds from Kiwifruit and Persimmon.

Fruit used in the common human diet in general, and kiwifruit and persimmon particularly, displays health properties in the prevention of heart disease. This study describes a combination of bioactivity, multivariate data analyses and fluorescence measurements for the differentiating of kiwifruit and persimmon, their quenching and antioxidant properties. The metabolic differences are shown, as well in the results of bioactivities and antioxidant capacities determined by ABTS, FRAP, CUPRAC and DPPH assays. To complement the bioactivity of these fruits, the quenching properties between extracted polyphenols and human serum proteins were determined by 3D-fluorescence spectroscopy studies. These properties of the extracted polyphenols in interaction with the main serum proteins in the human metabolism (human serum albumin (HSA), α-ß-globulin (α-ß G) and fibrinogen (Fgn)), showed that kiwifruit was more reactive than persimmon. There was a direct correlation between the quenching properties of the polyphenols of the investigated fruits with serum human proteins, their relative quantification and bioactivity. The results of metabolites and fluorescence quenching show that these fruits possess multiple properties that have a great potential to be used in industry with emphasis on the formulation of functional foods and in the pharmaceutical industry. Based on the quenching properties of human serum proteins with polyphenols and recent reports in vivo on human studies, we hypothesize that HSA, α-ß G and Fgn will be predictors of coronary artery disease (CAD).

Potential use of kiwifruit extract for treatment of melanoma.

Skin cancers are the most common cancers in the world and among the different types of skin cancers, melanoma is the deadliest and incidence is rising. Previous studies have shown promising in vitro and human evidence of kiwifruit exhibiting anti-cancer effects. This study was designed to investigate if kiwifruit extract (KE) has any effect on CRL-11147 melanoma cancer cells and to investigate the possible mechanisms behind the results. The effects of KE on CRL-11147 melanoma cell survival, proliferation, and apoptosis was investigated using clonogenic survival assay, cell proliferation, and caspase-3 activity kits. Potential anti-tumor molecular mechanisms were elucidated using RT-PCR and IHC. Addition of KE decreased CRL-11147 cell colonies percentages indicated by a decreased optical density value of cancer cells when compared to control. Furthermore, treatment with KE increased relative caspase-3 activity in cancer cells, which indicated increased apoptosis of cancer cells. The anti-proliferative effect of KE on cancer cells corresponded with decreased expression of the pro-proliferative molecule Cyclin E and CDK4, while increased expression of the pro-apoptotic molecule TRAILR1 corresponded with the pro-apoptotic effect. KE decreases CRL-11147 melanoma cell growth via downregulation of Cyclin E and CDK4 and upregulation in TRAILR1. Our study suggests a potential use for KE in treatment of melanoma.

Effect of selenium-enriched kiwifruit on body fat reduction and liver protection in hyperlipidaemic mice.

This study aimed to investigate the effects and mechanism of selenium-enriched kiwifruit (Se-Kiwi) on lipid-lowering and liver protection in hyperlipidaemic mice induced by consuming a long-term high-fat diet. Selenium-enriched cultivation can significantly improve the contents of vitamins and functional elements in kiwifruits, especially vitamin C, selenium, and manganese, thus enhancing the activity of antioxidant enzymes in Se-Kiwi. Se-Kiwi can significantly improve the activity of antioxidant enzymes in the liver of hyperlipidaemic mice, restore the liver morphology of mice close to normal, reduce the fat content in the liver, and inhibit the accumulation of abdominal fat cells. Meanwhile, the expression levels of inflammation-related factors (TNF-α and NF-κB) and lipid synthesis related genes (SREBP-1c and FAS) are inhibited at the gene transcription and protein expression levels, and the expression levels of energy expenditure related genes (PPAR-α and CPT1) are increased, resulting in lipid reductions and liver protection. In conclusion, our results indicate that the protective mechanism of Se-Kiwi on high-fat diet mice is associated with enhancing the activity of antioxidant enzymes, reducing the degree of the inflammatory reaction, inhibiting the fat synthesis, and accelerating body energy consumption.