(177) Open Column Chromatographic Separation of Health-promoting Bioactive Citrus Limonoids

Open column chromatography is an effective and common technique for the separation and purification of chemical constituents. Limonoids are found in significant quantities in citrus fruits. Citrus limonoids have documented anti-cancer activity in several types of cancer, such as breast, colon, skin, and neuroblastoma in animal models and in vitro cell culture studies. Furthermore, limonoids have shown anti-inflammatory properties and inhibitory effects on bone resorption. In addition to many potential health benefits, limonoids have also shown antifungal and insect anti-feedant properties. To meet the large demand of limonoids for bioactivity studies, defatted grapefruit seeds were extracted using acetone and concentrated under vacuum. The dried extract was loaded onto a silica gel column and eluted with mixtures of dichloromethane and ethyl acetate with increasing polarity to obtain three compounds. The purity of the compounds (1–3) have been analyzed by HPLC and the structures have been identified by using NMR spectra and mass spectra as nomilin, limonin, and deacetylnomilin, in respective order of elution. The results will be presented in greater detail on the poster. This project is based upon work supported by the USDA-CSREES under Agreement USDA IFAFS #2001 52102 02294 and USDA #2005-34402-14401 “Designing Foods for Health” through the Vegetable & Fruit Improvement Center.

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Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

Combinatorial Chemistry & High Throughput Screening ◽

10.2174/1386207323999201102141206 ◽

2020 ◽

Vol 23 ◽

Author(s):

Roohi Mohi-ud-din ◽

Reyaz Hassan Mir ◽

Prince Ahad Mir ◽

Saeema Farooq ◽

Syed Naiem Raza ◽

...

Keyword(s):

Chemical Constituents ◽

Pharmacological Activities ◽

Traditional Use ◽

Comprehensive Review ◽

Wide Range ◽

Anti Cancer ◽

Comprehensive Survey ◽

Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

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In Vitro Bioaccessibility of Bioactive Compounds from Citrus Pomaces and Orange Pomace Biscuits

Molecules ◽

10.3390/molecules26123480 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3480

Author(s):

Adriana Maite Fernández-Fernández ◽

Eduardo Dellacassa ◽

Tiziana Nardin ◽

Roberto Larcher ◽

Adriana Gámbaro ◽

...

Keyword(s):

Bioactive Compounds ◽

Total Phenol Content ◽

No Production ◽

Food Ingredient ◽

Potential Health ◽

Raw264.7 Macrophages ◽

In Vitro Bioaccessibility ◽

Health Promoting ◽

Orange Pomace

The present investigation aimed to provide novel information on the chemical composition and in vitro bioaccessibility of bioactive compounds from raw citrus pomaces (mandarin varieties Clemenule and Ortanique and orange varieties Navel and Valencia). The effects of the baking process on their bioaccessibility was also assessed. Samples of pomaces and biscuits containing them as an ingredient were digested, mimicking the human enzymatic oral gastrointestinal digestion process, and the composition of the digests were analyzed. UHPLC-MS/MS results of the citrus pomaces flavonoid composition showed nobiletin, hesperidin/neohesperidin, tangeretin, heptamethoxyflavone, tetramethylscutellarein, and naringin/narirutin. The analysis of the digests indicated the bioaccessibility of compounds possessing antioxidant [6.6–11.0 mg GAE/g digest, 65.5–97.1 µmol Trolox Equivalents (TE)/g digest, and 135.5–214.8 µmol TE/g digest for total phenol content (TPC), ABTS, and ORAC-FL methods, respectively; significant reduction (p < 0.05) in Reactive Oxygen Species (ROS) formation under tert-butyl hydroperoxide (1 mM)-induced conditions in IEC-6 and CCD-18Co cells when pre-treated with concentrations 5–25 µg/mL of the digests], anti-inflammatory [significant reduction (p < 0.05) in nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW264.7 macrophages], and antidiabetic (IC50 3.97–11.42 mg/mL and 58.04–105.68 mg/mL for α-glucosidase and α-amylase inhibition capacities) properties in the citrus pomaces under study. In addition, orange pomace biscuits with the nutrition claims “no-added sugars” and “source of fiber”, as well as those with good sensory quality (6.9–6.7, scale 1–9) and potential health promoting properties, were obtained. In conclusion, the results supported the feasibility of citrus pomace as a natural sustainable source of health-promoting compounds such as flavonoids. Unfractionated orange pomace may be employed as a functional food ingredient for reducing the risk of pathophysiological processes linked to oxidative stress, inflammation, and carbohydrate metabolism, such as diabetes, among others.

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In Vitro Screening for Cytotoxic, Anti-bacterial, Anti-HIV1-RT Activities and Chemical Constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii

The Natural Products Journal ◽

10.2174/2210315511666210119125611 ◽

2021 ◽

Vol 11 ◽

Author(s):

Charina Worarat ◽

Wilart Pompimon ◽

Phansuang Udomputtimekakul ◽

Sukee Sukdee ◽

Punchavee Sombutsiri ◽

...

Keyword(s):

Ethyl Acetate ◽

Ethyl Acetate Extract ◽

Biological Activities ◽

Chemical Constituents ◽

Bacterial Activity ◽

Cytotoxic Activities ◽

Separation And Purification ◽

Crude Extracts ◽

Cytotoxicity Activities

Background: Although the chemical constituents and biological activities of a large number of plants in the Croton genus have been studied, there are still recently discovered plants to be investigated. Objective: 1. To investigate the anti-bacterial, anti-HIV1-RT, and cytotoxicity activities of crude extracts from these plants. 2. To investigate the chemical constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii. Method: The anti-bacterial, anti-HIV1-RT, and cytotoxicity of the three plants were evaluated by standard techniques. Extraction, separation, and purification of extracts from the three plants were undertaken. Results: The ethyl acetate extract of C. fluviatilis showed low anti-bacterial activity against E. aerogenes, E. coli 0157: H7, and P. mirabilis, together with the ethyl acetate extract of C. acutifolius displayed low anti-bacterial activity against E. aerogenes, while all the crude extracts of C. thorelii were inactive. The ethyl acetate extracts of C. thorelii, and C. fluviatilis showed strong inhibited HIV1-RT, whereas the ethyl acetate extract of C. acutifolius, and the hexane extract of C. fluviatilis displayed moderate inhibited HIV1-RT. Cytotoxic properties of three Croton plants were specific to KKU-M213, MDA-MB-231, A-549, and MMNK-1. Especially, the ethyl acetate extract of C. acutifolius exhibited strong cytotoxic activities against MDA-MB-231, A-549, and MMNK-1. Furthermore, the ethyl acetate extract of C. thorelii showed high cytotoxic activities against KKU-M213, and MDA-MB-231. Compounds 1, and 4 were found in C. fluviatilis. Compounds 2 and 4 were also found in C. acutifolius. Moreover, compound 3 was only found in C. thorelii. Conclusion: The present study revealed that the three Croton species are good sources of flavonoid compounds and further investigation of the chemical constituents from these plants may prove to be fruitful to discover more active compounds to be tested as potential medicines.

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Chemical Constituents from Scindapsus officinalis (Roxb.) Schott. and Their Anti–Inflammatory Activities

Molecules ◽

10.3390/molecules23102577 ◽

2018 ◽

Vol 23 (10) ◽

pp. 2577 ◽

Cited By ~ 2

Author(s):

Hongjing Dong ◽

Yanling Geng ◽

Xueyong Wang ◽

Xiangyun Song ◽

Xiao Wang ◽

...

Keyword(s):

Chemical Constituents ◽

2D Nmr ◽

No Production ◽

Inhibitory Effects ◽

Nmr Data ◽

Extensive Analysis ◽

Ic50 Values ◽

Monoterpene Glycoside ◽

Anti Inflammatory

One new monoterpene glycoside (1), one new phenyl glycoside (2), one new caffeoyl derivative (3), were isolated from Scindapsus officinalis (Roxb.) Schott., along with four known compounds (4–7). Structures of the isolated compounds were elucidated by extensive analysis of spectroscopic data, especially 2D NMR data and comparison with literatures. All isolates were evaluated for anti-inflammatory activity against nitric oxide (NO) production in vitro. Compounds 3 and 7 exhibited moderate inhibitory effects on NO production with IC50 values of 12.2 ± 0.8 and 18.9 ± 0.3 μM, respectively.

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Potential Health Benefits of Ropy Exopolysaccharides Produced by Lactobacillus plantarum

Molecules ◽

10.3390/molecules25143293 ◽

2020 ◽

Vol 25 (14) ◽

pp. 3293 ◽

Cited By ~ 1

Author(s):

Tülin Yılmaz ◽

Ömer Şimşek

Keyword(s):

Lactobacillus Plantarum ◽

Immune Modulation ◽

Radical Scavenging ◽

Fermentation Medium ◽

Potential Health ◽

Tnf Α ◽

Medium Level ◽

Probiotic Strains ◽

Health Promoting

The ability of Lactobacillus plantarum to produce exopolysaccharides (EPS) of various structures and properties is effective in showing both starter and probiotic culture qualification. In this study, the potential health promoting functions of the ropy EPS produced by Lactobacillus plantarum strains isolated from tarhana were tested. A stimulation of the pro-inflammatory IL-12 and TNF-α cytokines was observed in the presence of the ropy EPS suggesting an in vitro immune modulation. Similarly, the tested EPS demonstrated promoted the growth of the probiotic strains in fermentation medium. A medium level of radical scavenging activities of ropy EPS was observed whereas the superoxide and hydroxyl scavenging activities were more effective. The ropy EPS also showed α-glucosidase inhibition and cholesterol removal characteristics depending on their concentration. These findings revealed the potential health-promoting functions of ropy EPS from L. plantarum strains and EPS from L. plantarum PFC311 and PFC310 strains demonstrated multiple health-improving effects that can be further evaluated in food and other industries.

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Prebiotic effects of inulin and oligofructose

British Journal Of Nutrition ◽

10.1079/bjn/2002537 ◽

2002 ◽

Vol 87 (S2) ◽

pp. S193-S197 ◽

Cited By ~ 179

Author(s):

S. Kolida ◽

K. Tuohy ◽

G. R. Gibson

Keyword(s):

Food Product ◽

Inhibitory Effects ◽

Food Ingredients ◽

Acute Infections ◽

Health Promoting ◽

Human Large Intestine ◽

Gut Pathogens ◽

Stimulation Of

Prebiotics are non-digestible food ingredients that target certain components within the microbiota of the human large intestine. Efficient prebiotics need to have a specific fermentation therein and thereby have the ability to alter the faecal microflora composition towards a more ‘beneficial’ community structure. This should occur by the stimulation of benign or potentially health promoting genera but not the harmful groups. Because of their positive attributes bifidobacteria and lactobacilli are the most frequent target organisms. Both inulin and oligofructose have been demonstrated to be effective prebiotics. This has been shown through both in vitro and in vivo assessments in different laboratories. Because of their recognised prebiotic properties, principally the selective stimulation of colonic bifidobacteria, both inulin and oligofructose are increasingly used in new food product developments. Examples include drinks, yoghurts, biscuits and table spreads. Because of the recognised inhibitory effects that bifidobacteria can exert against gut pathogens, one of the most important aspects of prebiotic ingestion is fortification of the gut flora to resist acute infections.

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Nigericin Suppresses the Wnt/β-catenin Signaling in Pancreatic Cancer through Targeting pre-miR-374b-PRKCA/HBP1 Axis

10.21203/rs.3.rs-52126/v1 ◽

2020 ◽

Author(s):

Qiaoming Zhi ◽

Wei Li ◽

Dongming Zhu ◽

Daiwei Wan ◽

Ye Han ◽

...

Keyword(s):

Pancreatic Cancer ◽

Tumor Model ◽

Migration And Invasion ◽

Inhibitory Effects ◽

Biochemical Basis ◽

Over Expression ◽

Anti Cancer ◽

Ic50 Values ◽

Anti Tumor Activity

Abstract Background The polyether antibiotic nigericin has been demonstrated recently to have anti-tumor activity in multiple cancers. But the biochemical basis for its anti-cancer effects has not been fully elucidated. The objective of this study was to investigate the potential mechanisms of nigericin in pancreatic cancer (PC) cells. Methods PC cells were exposed to increasing concentrations of nigericin at different time periods, and the corresponding IC50 values were calculated. Then the effects on the biological functions of PC cells were evaluated. Subsequent experiments including the high-throughput RNA sequencing, qRT-PCR, western blot, TOP/FOP-Flash reporter, Co-Immunoprecipitation and luciferase report assays were employed to reveal the potential mechanisms of nigericin. In addition, the inhibitory effects of nigericin on PC cells were also accessed in the subcutaneous tumor model. Results The data showed that nigericin was extremely sensitive to PC cells, and could influence the abilities of cell proliferation, colony formation, apoptosis, migration and invasion. The results in vitro implied that nigericin suppressed the Wnt/β-catenin signaling by up-regulating PRKCA and HBP1 mRNA expressions. Furthermore, the dual strands of pre-miR-374b were proved to down-regulate the PRKCA and HBP1 expressions coordinately, and over-expression of pre-miR-374b partly antagonized the suppressing effects of PC cells induced by nigericin. Meanwhile, the inhibitory effects of nigericin on PC cells were also confirmed in mice. Conclusion These findings demonstrated that suppressing the Wnt/β-catenin signaling pathway by targeting pre-miR-374b-PRKCA/HBP1 axis might represent a novel molecular mechanism of nigericin in PC. Nigericin remained a candidate for a potential pre-clinical application for PC.

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In Vitro and In Vivo Anti-Breast Cancer Activities of Some Newly Synthesized 5-(thiophen-2-yl)thieno-[2,3-d]pyrimidin-4-one Candidates

Molecules ◽

10.3390/molecules24122255 ◽

2019 ◽

Vol 24 (12) ◽

pp. 2255 ◽

Cited By ~ 1

Author(s):

Abd El-Galil E. Amr ◽

Alhussein A. Ibrahimd ◽

Mohamed F. El-Shehry ◽

Hanaa M. Hosni ◽

Ahmed A. Fayed ◽

...

Keyword(s):

Chloroacetic Acid ◽

Aromatic Aldehydes ◽

Mercaptoacetic Acid ◽

Inhibitory Effects ◽

In Vivo Experiments ◽

Schiff Base Derivatives ◽

Anti Cancer ◽

Mcf 7

In this study, some of new thiophenyl thienopyrimidinone derivatives 2–15 were prepared and tested as anti-cancer agents by using thiophenyl thieno[2,3-d]pyrimidinone derivative 2 as a starting material, which was prepared from cyclization of ethyl ester derivative 1 with formamide. Treatment of 2 with ethyl- chloroacetate gave thienopyrimidinone N-ethylacetate 3, which was reacted with hydrazine hydrate or anthranilic acid to afford acetohydrazide 4 and benzo[d][1,3]oxazin-4-one 5, respectively. Condensation of 4 with aromatic aldehydes or phenylisothiocyanate yielded Schiff base derivatives 6,7, and thiosemicarbazise 10, which were treated with 2-mercaptoacetic acid or chloroacetic acid to give the corresponding thiazolidinones 8, 9, and phenylimino-thiazolidinone 11, respectively. Treatment of 4 with ethylacetoacetate or acetic acid/acetic anhydride gave pyrazole 12 and acetyl acetohydrazide 13 derivatives, respectively. The latter compound 13 was reacted with ethyl cycno-acetate or malononitrile to give 14 and 15, respectively. In this work, we have studied the anti-cancer activity of the synthesized thienopyrimidinone derivatives against MCF-7 and MCF-10A cancer cells. Furthermore, in vivo experiments showed that the synthesized compounds significantly reduced tumor growth up to the 8th day of treatment in comparison to control animal models. Additionally, the synthesized derivatives showed potential inhibitory effects against pim-1 kinase activities.

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The Anticancer Effect of Sanguinarine: A Review

Current Pharmaceutical Design ◽

10.2174/1381612824666180829100601 ◽

2018 ◽

Vol 24 (24) ◽

pp. 2760-2764 ◽

Cited By ~ 7

Author(s):

Chenxing Fu ◽

Guiping Guan ◽

Hongbing Wang

Keyword(s):

Tumor Cell ◽

In Vivo Studies ◽

Inhibitory Effects ◽

Anticancer Effect ◽

Growth Inhibitory ◽

Cell Proliferation Inhibition ◽

Anti Cancer ◽

Induced Apoptosis

In vitro and in vivo studies have revealed that Sanguinarine has antioxidant, anti-inflammatory, proapoptotic, and growth inhibitory effects on tumor cells of a variety of cancers. Previous research showed that sanguinarine induced apoptosis (cell death) and/or antiproliferative while reducing tumor cell antiangiogenic and anti-invasive properties. This paper describes various sanguinarine anti-cancer mechanisms, including inhibition of erroneously-activated signal transduction pathways, apoptosis, and tumor cell proliferation inhibition.

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“Evaluation of cholesterol lowering efficacy and antibacterial potential of probiotics: An In vitro study”

Anti-Infective Agents ◽

10.2174/2211352518666200423082803 ◽

2020 ◽

Vol 18 ◽

Author(s):

Ayisha Aman ◽

Tooba Shamim ◽

Ayesha Siddiqui ◽

Suad Naheed

Keyword(s):

Antibacterial Activity ◽

Therapeutic Potential ◽

In Vitro Study ◽

Human Beings ◽

Potential Health ◽

Cholesterol Lowering ◽

Fruit Samples ◽

Natural Microflora ◽

Health Promoting

Background and Objectives: Probiotics are nonpathogenic and beneficial viable microorganisms that exhibit potential health welfare for human beings. Probiotics are found in various food products. They also occur as natural microflora in the intestine of mammals. Main goal of this study was to isolate probiotics conferring antibacterial activity and cholesterol lowering ability from different fruits. Materials and Method: Present research reveals the usefulness of probiotics, in which twenty one bacterial cultures were isolated from different fruit samples including figs, coconut water and grapes. These strains were explored for their antibacterial and cholesterol reduction ability by conducting in vitro experiments. Results and Conclusion: Among twenty one isolates, nine probiotic cultures FgC2, FgC7, FgC14, G2C5, G1C,GrC18 and StCW showed maximum antibacterial activity against different human clinical pathogens. This suggests that these microbes produce inhibitory metabolites which are extracellular and diffusible. For cholesterol assimilation assay, six strains FgC2, FgC7,FgC12, FgC13, GrC7 and GrC18 presented remarkable cholesterol lowering efficacy (up to 98%) when grown in the presence of bile salts. Only potential probiotic cultures were identified and characterized as lactic acid bacteria (LAB), on the basis of Bergey’s Manual of Determinative Bacteriology. Thus this study is helpful to exploit the bioactive and therapeutic potential of beneficial microorganisms so that they can be utilized in the generation of functional food and other health promoting products.

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