The water-soluble chitosan derivative, N-methylene phosphonic chitosan, is an effective fungicide against the phytopathogen Fusarium eumartii

Chitosan has been considered an environmental-friendly polymer. However, its use in agriculture has not been extended yet due to its relatively low solubility in water. In an attempt to improve such chemical characteristics, a chitosan-derivative prepared by adding a phosphonic group to chitosan N-methylene phosphonic chitosan, NMPC, was obtained from shrimp fishing industry waste from Argentinean Patagonia. This study showed that NMPC had a fungicidal effect on the phytopathogenic fungus Fusarium solani f. sp. eumartii (F. eumartii). NMPC inhibited F. eumartti mycelial growth and spore germination with low IC50 values. In vivo studies showed that NMPC affected fungal membrane permeability, ROS production, and cell death. NMPC also exerted antifungal effects against two other phytopathogens, Botrytis cinerea, and Phytophthora infestans. NMPC did not affect tomato cell viability at the same doses applied to these phytopathogens. Furthermore, the selective cytotoxicity of NMPC could give it added value in its application as an antimicrobial agent in agriculture.

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The Water-Soluble Chitosan Derivative, N-Methylene Phosphonic Chitosan, Is an Effective Fungicide against the Phytopathogen Fusarium eumartii

The Plant Pathology Journal ◽

10.5423/ppj.oa.06.2021.0090 ◽

2021 ◽

Vol 37 (6) ◽

pp. 533-542

Author(s):

Florencia Anabel Mesas ◽

María Cecilia Terrile ◽

María Ximena Silveyra ◽

Adriana Zuñiga ◽

María Susana Rodriguez ◽

...

Keyword(s):

Water Solubility ◽

Water Soluble ◽

Phytopathogenic Fungus ◽

Oxygen Species ◽

Chitosan Derivative ◽

Solubility In Water ◽

Environmental Friendly ◽

Antifungal Effects ◽

Species Production ◽

Low Solubility

Chitosan has been considered an environmental-friendly polymer. However, its use in agriculture has not been extended yet due to its relatively low solubility in water. N-Methylene phosphonic chitosan (NMPC) is a water-soluble derivative prepared by adding a phosphonic group to chitosan. This study demonstrates that NMPC has a fungicidal effect on the phytopathogenic fungus Fusarium solani f. sp. eumartii (F. eumartii) judged by the inhibition of F. eumartti mycelial growth and spore germination. NMPC affected fungal membrane permeability, reactive oxygen species production, and cell death. Also, this chitosan-derivative exerted antifungal effects against two other phytopathogens, Botrytis cinerea, and Phytophthora infestans. NMPC did not affect tomato cell viability at the same doses applied to these phytopathogens to exert fungicide action. In addition to water solubility, the selective biological cytotoxicity of NMPC adds value in its application as an antimicrobial agent in agriculture.

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Ultradeformable vesicles: concepts and applications relating to the delivery of skin cosmetics

Therapeutic Delivery ◽

10.4155/tde-2021-0044 ◽

2021 ◽

Author(s):

Andang Miatmoko ◽

Qurrota Ayunin ◽

Widji Soeratri

Keyword(s):

Skin Aging ◽

Water Soluble ◽

In Vivo Studies ◽

Active Ingredients ◽

Self Confidence ◽

Skin Delivery ◽

Cosmetic Ingredients ◽

Insight Into

Skin aging is a phenomenon resulting in reduced self-confidence, thus becoming a major factor in social determinants of health. The use of active cosmetic ingredients can help prevent skin aging. Transfersomes are well known to be capable of deeply penetrating the dermis. This scoping review provides an insight into transfersomes and their prospective use in anti-aging cosmetics. Numerous reports exist highlighting the successful skin delivery of therapeutic agents such as high-molecular-weight, poorly water soluble and poorly permeable active ingredients by means of transfersomes. Moreover, in vitro and in vivo studies have indicated that transfersomes increase the deposition, penetration and efficacy of active ingredients. However, the use of transfersomes in the delivery of active cosmetic ingredients is limited. Considering their similar physicochemical properties, transfersomes should possess considerable potential as a delivery system for anti-aging cosmetics.

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Polyphenols in Food: Cancer Prevention and Apoptosis Induction

Current Medicinal Chemistry ◽

10.2174/0929867324666171006144208 ◽

2018 ◽

Vol 25 (36) ◽

pp. 4740-4757 ◽

Cited By ~ 20

Author(s):

Ashita Sharma ◽

Mandeep Kaur ◽

Jatinder Kaur Katnoria ◽

Avinash Kaur Nagpal

Keyword(s):

Cancer Prevention ◽

Defense Mechanism ◽

Antioxidant Property ◽

The Body ◽

Water Soluble ◽

Stress Factors ◽

In Vivo Studies ◽

Hydroxyl Groups

Polyphenols are a group of water-soluble organic compounds, mainly of natural origin. The compounds having about 5-7 aromatic rings and more than 12 phenolic hydroxyl groups are classified as polyphenols. These are the antioxidants which protect the body from oxidative damage. In plants, they are the secondary metabolites produced as a defense mechanism against stress factors. Antioxidant property of polyphenols is suggested to provide protection against many diseases associated with reactive oxygen species (ROS), including cancer. Various studies carried out across the world have suggested that polyphenols can inhibit the tumor generation, induce apoptosis in cancer cells and interfere in progression of tumors. This group of wonder compounds is present in surplus in natural plants and food products. Intake of polyphenols through diet can scavenge ROS and thus can help in cancer prevention. The plant derived products can also be used along with conventional chemotherapy to enhance the chemopreventive effects. The present review focuses on various in vitro and in vivo studies carried out to assess the anti-carcinogenic potential of polyphenols present in our food. Also, the pathways involved in cancer chemopreventive effects of various subclasses (flavonoids, lignans, stilbenes and phenolic acids) of polyphenols are discussed.

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Ganoderma lucidum Polysaccharides as An Anti-cancer Agent

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520617666171113121246 ◽

2018 ◽

Vol 18 (5) ◽

pp. 667-674 ◽

Cited By ~ 20

Author(s):

Didem Sohretoglu ◽

Shile Huang

Keyword(s):

Ganoderma Lucidum ◽

Water Soluble ◽

In Vivo Studies ◽

Beneficial Effects ◽

Anticancer Effects ◽

Bioactive Component ◽

Cancer Agent ◽

Underlying Mechanisms

The mushroom Ganoderma lucidum (G. lucidum) has been used for centuries in Asian countries to treat various diseases and to promote health and longevity. Clinical studies have shown beneficial effects of G. lucidum as an alternative adjuvant therapy in cancer patients without obvious toxicity. G. lucidum polysaccharides (GLP) is the main bioactive component in the water soluble extracts of this mushroom. Evidence from in vitro and in vivo studies has demonstrated that GLP possesses potential anticancer activity through immunomodulatory, anti-proliferative, pro-apoptotic, anti-metastatic and anti-angiogenic effects. Here, we briefly summarize these anticancer effects of GLP and the underlying mechanisms.

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Anthocyanins in Whole Grain Cereals and Their Potential Effect on Health

Nutrients ◽

10.3390/nu12102922 ◽

2020 ◽

Vol 12 (10) ◽

pp. 2922

Author(s):

Alyssa Francavilla ◽

Iris J. Joye

Keyword(s):

Food Industry ◽

Potential Effect ◽

Research Field ◽

Water Soluble ◽

Antioxidant Potential ◽

In Vivo Studies ◽

Whole Grain ◽

Grain Products

Coloured (black, purple, blue, red, etc.) cereal grains, rich in anthocyanins, have recently gained a lot of attention in the food industry. Anthocyanins are water-soluble flavonoids, and are responsible for red, violet, and blue colours in fruits, vegetables, and grains. Anthocyanins have demonstrated antioxidant potential in both in vitro and in vivo studies, and the consumption of foods high in anthocyanins has been linked to lower risks of chronic diseases. As such, whole grain functional foods made with coloured grains are promising new products. This paper will review the characteristics of cereal anthocyanins, and assess their prevalence in various commercially relevant crops including wheat, barley, maize, and rice. A brief overview of the antioxidant potential, and current research on the health effects of cereal-based anthocyanins will be provided. Finally, processing of coloured cereals in whole grain products will be briefly discussed. A full understanding of the fate of anthocyanins in whole grain products, and more research targeted towards health outcomes of anthocyanin supplementation to/inclusion in cereal food products are the next logical steps in this research field.

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Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets

Asian Journal of Organic & Medicinal Chemistry ◽

10.14233/ajomc.2019.ajomc-p209 ◽

2019 ◽

Vol 4 (2) ◽

pp. 121-129

Author(s):

Satya Sankar Sahoo ◽

Chandu Babu Rao

Keyword(s):

Patient Compliance ◽

Oral Drug Delivery ◽

Particle Diameter ◽

Water Soluble ◽

In Vivo Studies ◽

Oral Drug ◽

Water Soluble Drugs ◽

Fast Disintegrating Tablets ◽

Lurasidone Hydrochloride

Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.

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Comparison of Anticancer Effects of Carvone, Carvone-Rich Essential Oils, and Chitosan Nanoparticles Containing Each of Them

Biointerface Research in Applied Chemistry ◽

10.33263/briac124.57165726 ◽

2021 ◽

Vol 12 (4) ◽

pp. 5716-5726

Keyword(s):

Essential Oils ◽

Treatment Approach ◽

Chitosan Nanoparticles ◽

Human Melanoma ◽

In Vivo Studies ◽

Mentha Spicata ◽

Anticancer Effects ◽

Common Cancer ◽

Ic50 Values

Cancers were the first cause of death in 2020; breast and skin are two common cancers worldwide. The most common cancer treatment approach is still chemotherapy; however, as side effects and multidrug resistance, the development of green nano drugs has received much attention. In this study, the chemical composition of Mentha spicata and Tanacetum balsamita essential oils was first investigated. The anticancer effects of them and carvone (as their major ingredients) were then evaluated on human melanoma (A375) and breast cancer (MDA-MB468) cells. After that, an attempt was made to improve their efficacies by preparing chitosan nanoparticles containing each of them. The efficacies of nanoformulations showed a significant improvement (p < 0.05) compared to their non-formulated states. The best-observed potency was related to chitosan nanoparticles containing T. balsamita essential oil with a particle size of 195 ± 7 nm; IC50 values against A375 and MDA-MB468 were observed at 85.3 and 240.1 µg/mL. Thus, the nanoformulation with green ingredients could be considered a proper candidate for further consideration in vivo studies.

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Combretastatins: An Overview of Structure, Probable Mechanisms of Action and Potential Applications

Molecules ◽

10.3390/molecules25112560 ◽

2020 ◽

Vol 25 (11) ◽

pp. 2560 ◽

Cited By ~ 1

Author(s):

Gökçe Şeker Karatoprak ◽

Esra Küpeli Akkol ◽

Yasin Genç ◽

Hilal Bardakcı ◽

Çiğdem Yücel ◽

...

Keyword(s):

South African ◽

Water Solubility ◽

The Body ◽

Water Soluble ◽

In Vivo Studies ◽

Lead Compounds ◽

Combretastatin A4 ◽

Potential Applications

Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of Combretum caffrum (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Combretastatin A4 phosphate is the most frequently tested compounds in preclinical and clinical trials. It is a water-soluble prodrug that the body can rapidly metabolize to combretastatin A4, which exhibits anti-tumor properties. In addition, in vitro and in vivo studies on combretastatins have determined that these compounds also have antioxidant, anti-inflammatory and antimicrobial effects. Nano-based formulations of natural or synthetic active agents such as combretastatin A4 phosphate exhibit several clear advantages, including improved low water solubility, prolonged circulation, drug targeting properties, enhanced efficiency, as well as fewer side effects. In this review, a synopsis of the recent literature exploring the combretastatins, their potential effects and nanoformulations as lead compounds in clinical applications is provided.

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Design, Synthesis and Biological Evaluation of a Novel Series of Thiadiazole-Based Anticancer Agents as Potent Angiogenesis Inhibitors

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621666201231143535 ◽

2020 ◽

Vol 21 ◽

Author(s):

Burcugül Altuğ-Tasa ◽

Betül Kaya-Çavuşoğlu ◽

Ayşe T. Koparal ◽

Gülhan Turan ◽

Ali S. Koparal ◽

...

Keyword(s):

Cell Line ◽

Cell Lines ◽

Anticancer Agents ◽

Human Cancer ◽

Biological Evaluation ◽

Tube Formation ◽

In Vivo Studies ◽

Human Cancer Cell Lines ◽

Ic50 Values

Background: Thiadiazole has attracted a great deal of interest as a versatile heterocycle for the discovery and development of potent anticancer agents. Thiadiazole derivatives exert potent antitumor activity against a variety of human cancer cell lines through various mechanisms. Objective: The goal of this work was to design and synthesize thiadiazole-based anticancer agents with anti-angiogenic activity. Methods: N-aryl-2-[(5-(aryl)amino-1,3,4-thiadiazol-2-yl)thio]acetamides (4a-r) were synthesized via the reaction of 5-(aryl)amino-1,3,4- thiadiazole-2(3H)-thiones with N-(aryl)-2-chloroacetamides in the presence of potassium carbonate. The compounds were investigated for their cytotoxic effects on three cancer (A549, HepG2, SH-SY5Y), two normal (HUVEC and 3T3-L1) cell lines using MTT and WST1 assays. In order to examine whether the compounds have anti-angiogenic effects or not, HUVEC were cultured on matrigel matrix to create a vascular-like tube formation. Results: Compounds 4d, 4m and 4n were more effective on A549 human lung adenocarcinoma cells than cisplatin. The IC50 values of compounds 4d, 4m and 4n for A549 cell line were found to be 7.82±0.4, 12.5±0.22, 10.1±0.52 µM, respectively when compared with cisplatin (IC50= 20±0.51 µM), whilst their IC50 values for HUVEC cell line were determined as 138.7±0.84, 78±0.44, 177.6±0.2 µM, respectively after 48 h treatment. The concentrations (10-20-50 µM) of compounds 4d, 4e, 4l, 4m, 4n, 4q and 4r were found to inhibit vascular like tube formation. Conclusion: According to their anticancer and anti-angiogenic effects, compounds 4d, 4m and 4n may be potential anticancer agents for further in vivo studies.

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NEGATIVE EFFECTS OF VITAMIN K PREPARATIONS ON GLUCURONYL TRANSFERASE ACTIVITY

PEDIATRICS ◽

10.1542/peds.40.6.993 ◽

1967 ◽

Vol 40 (6) ◽

pp. 993-999

Author(s):

Barbara Jones

Keyword(s):

Vitamin K ◽

Inhibitory Effect ◽

Water Soluble ◽

In Vivo Studies ◽

Transferase Activity ◽

Negative Effects ◽

Glucuronyl Transferase ◽

Glucuronide Conjugation

In vitro studies using a mouse liver microsome system failed to demonstrate that menadiol sodium diphosphate, menadione sodium bisulfite, or phytonadione enhanced or inhibited the quantity of ortho-aminophenol glucuronide produced. In vivo studies in young rats with these vitamin K analogues also failed to show an effect on glucuronide conjugation. Based on this data, it is concluded that the hyperbilirubinemia seen in prematures after large doses of water-soluble vitamin K analogues is probably not due to an inhibitory effect of glucuronyl transferase. The evidence suggesting that it may be due in part to hemolysis is briefly reviewed.

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