Anticancer Preparations Research Articles

PLGA, a Hauler for Anticancer Drugs: Review

Abstract: Polymers are the mainstay of drug delivery systems. They may be natural, semisynthetic, or synthetic and used to program the release of drugs as per requirement. They are used to enhance the bioavailability and hence solubility, stability, and site specificity, or to release to drug either in a controlled, pulsatile, sustained, immediate release pattern. In the present review, we have discussed the recent prose and patents of poly(lactic-co-glycolic acid) and PLGA applicability in preparing formulations against cancer. Synthetic polymer, PLGA comprises monomers of glycolide and lactide available in various grades with varying physicochemical properties thus serving the formulators to fabricate preparations having designed release patterns. In this review, current literature and patents of poly(lactic-co-glycolic acid); PLGA using anticancer preparations have been covered. PLGA has demonstrated its potential as a polymer to program the release of drugs as a coating polymer and the development of a matrix in various drug delivery systems. It can augment the bioavailability of the drug reducing the toxicity/side effects and delivering the drug at the target site. The potential of PLGA to transfer the drug may unclutter novel ways for therapeutic interventions in various tumors.

Ethylcellulose- An Amazing Polymer For Anticancer Formulations

Background: A cellulose derivative known as ethyl cellulose has gained a lot of interest because of its special qualities and prospective uses in systems for the controlled administration of medications. This study concentrates on patents that examine the use of ethyl cellulose for anticancer preparations. Polymeric drug delivery methods are gaining significant research due to their potential to enhance therapeutic effectiveness, improve bioavailability, and reduce toxicity Objective: The primary objective of incorporating ethyl cellulose into anticancer preparations is to develop safe, effective, and targeted therapies for the treatment of cancer. This study aims to provide a comprehensive overview of recent patents that specifically explore the use of ethyl cellulose in the prevention and treatment of different cancers. Methods: The patent review methodology employed an extensive search across multiple patent databases to identify relevant patents on the utilization of ethyl cellulose in anticancer preparations. Results: The formulations described in these patents demonstrated sustained and controlled drug release profiles, which resulted in improved therapeutic efficacy while minimizing potential adverse effects. Our comprehensive review revealed multiple patents that utilized ethyl cellulose as a polymer in the creation of anticancer preparations. The studies conducted in these patents showcased enhanced drug release kinetics, improved cellular uptake, and increased anticancer activity compared to conventional formulations. Conclusion: The analysis of these patents strongly indicates that ethyl cellulose exhibits substantial potential as a versatile polymer for anticancer preparations. The findings strongly suggest that incorporating ethyl cellulose into drug delivery systems can significantly enhance the effectiveness of anticancer drugs, thus benefiting patients.

The Action Mechanisms, Anti-Cancer and Antibiotic-Modulation Potential of Vaccinium myrtillus L. Extract.

Herbal medicinal products containing Vaccinium myrtillus L. (bilberry) fruits and fruit extracts are widely available in the market. Although bilberry leaves and stems are considered as bio-waste, they contain much higher levels of phenolic compounds than fruits. The study aimed to investigate the antimicrobial and anticancer potential of aerial part extracts from Vaccinium myrtillus L. (V. myrtillus, VM) plants harvested at high altitudes in Armenian landscape and characterize the bioactive phytochemicals. For evaluation of antioxidant properties, chemical-based tests (total phenolic and flavonoid content, and antiradical activity in 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) tests) and cellular antioxidant activity (CAA) assay were applied. Genotoxicity and anticancer properties of the extract alone and in combination with fluorouracil were explored in human cancer and normal cell lines. Antibacterial properties of V. myrtillus extract alone and in combination with antibiotics, as well as their effect on proton-flux rate through cell membrane were explored on bacterial strains. The characterization of active phytochemicals was done using Liquid Chromatography-Quadrupole-Orbitrap High-Resolution Mass Spectrometry (LC-Q-Orbitrap HRMS). The V. myrtillus aerial part extract demonstrated promising antioxidant properties in all tests. The selective cytotoxic activity was documented against various cancer cell lines (human colon adenocarcinoma (HT29), human breast cancer (MCF-7) and human cervical carcinoma (HeLa)), while it did not inhibit the growth of tested human normal primary renal mixed epithelial cells (HREC) even at 10-fold higher concentrations. The extract did not have genotoxic properties in comet assay making it a potential source for the development of anticancer preparations. The investigated extract did not directly inhibit the growth of Escherichia coli (E. coli) and Salmonella typhimurium (S. typhimurium) strains at up to 1 mg/mL concentration. However, V. myrtillus extract enhanced the kanamycin intake and increased its efficiency against E. coli strain. The phytochemical characterization of the extract showed the presence of different groups of phenolics. Based on obtained data, we suggest the aerial parts of the V. myrtillus plant as an alternative source of bioactive natural products for food supplements, nutraceuticals, functional foods and medicine.

Eudragit, a Nifty Polymer for Anticancer Preparations: A Patent Review.

Polymers are the backbone of modern pharmaceutical formulations and drug delivery technologies. Polymers that may be natural, synthetic, or semisynthetic are used to control the release of drugs in a pre-programmed fashion. The drug delivery systems are mainly prepared to enhance the bioavailability, site-specific release, sustained release, controlled release, i.e., to modify the release of drug from dosage form may be a tablet, capsule, etc. Objectives: The objective of the present study is to overview the recent patents concerning the application of eudragit in the prevention of cancer and other ailments. Eudragit polymers are polymethacrylates and may be anionic, cationic, or non-ionic polymers of methacrylic acid, dimethylaminoethyl methacrylates, and methacrylic acid esters in varying ratios. Eudragit is available in various grades with solubilities at different pH, thus helping the formulators design the preparation to have a well-defined release pattern. In this review, patent applications of eudragit in various drug delivery systems employed to cure mainly cancer are covered. Eudragit has proved its potential as a polymer to control the release of drugs as coating polymer and formation of the matrix in various delivery systems. It can increase the bioavailability of the drug by site-specific drug delivery and can reduce the side effects/toxicity associated with anticancer drugs. The potential of eudragit to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

ANTITUMOR DRUGS BASED ON INDOLOCARBAZOL DERIVATIVES

The aim of the work is to generalize the literature data on indolocarbazole derivatives with an antitumor activity.Materials and methods. The objects of the study were the preparations based on indolocarbazole derivatives with the antitumor activity. To search for materials on the problem under study, the following search and information as well as library databases were used: ebibrary, PubMed, CyberLeninka, ResearchGate, the State Register of Medicines, clinical trials registries clinline.ru and clinicaltrials.gov. The search for the following words / phrases was performed: indolocarbazoles, indolocarbazole derivatives, staurosporine, rebeccamycin, staurosporine derivatives. The search was conducted from January 11 until March 1, 2021. The compounds with a biological activity which were undergoing or had undergone preclinical and clinical trials, were taken into account. All the materials from 1977 to January 1, 2021, were taken into account.Results. The materials obtained indicate that indolocarbazole derivatives are promising compounds for the creation of anticancer medicinal preparations due to their properties and peculiarities of the action mechanism. These drugs have a selective action due to the targeted interaction with specific molecular targets: kinases (especially protein kinase C and its isozymes), DNA and DNA topoisomerase. To date, many compounds from the class of indolocarbazoles have been synthesized and investigated. They have shown a high antitumor activity in the treatment of systemic and solid tumors. However, despite this, only one MP based on a staurosporine derivative, registered by the TN of Rydapt® (in the USA and EU countries) and Miticaid® (in the Russian Federation), is approved for use in the clinical practice.Conclusion. Thus, the basic data from scientific publications on promising anticancer medicinal preparations based on compounds from the class of indolocarbazoles, have been summarized. The information is provided, in particular, on their molecular structure, the origin, classification, the main representatives of the class, which are at various stages of the research and are approved for use in the clinic.

PENGAMBANGAN SISTEM NANOSTRUCTURED LIPID CARRIER (NLC) DAUN Chrysanthemum cinerariifolium (Trev.) Vis DENGAN VARIASI KONSENTRASI LIPID

Ethanol extract 96% of Chrysanthemum cinerariifolium (Trev.) Vis leaves are proven to have anticancer activity. However, these compounds have low solubility in water and fat. To improve the bioavailability of preparations, the development of drug design in the form of Nanostructured Lipid Carrier (NLC) is carried out.The aim this study was to determine the effect of differences in lipid concentration of Monostearin and Oleic Acid in the formulation of the NLC system of Chrysanthemum cinerariifolium (Trev.) Vis leaves, which produced good physicochemical characteristics including organoleptic characteristics, pH, viscosity, particle size, and drug entrapment efficiency. Making is done using the High Shear Homogenization method. Organoleptic tests showed ideal results for the Nanostructured Lipid Carrier (NLC) system, the resulting pH values in formula 1 (7.0 ± 0.12), formula 2 (6.7 ± 0.17) and formula 3 (6.8 ± 0.2)), the viscosity value of formula 1 (55.66 ± 2.84 cPs), formula 2 (28.86 ± 3.91 cPs), and formula 3 (28.57 ± 16.85 cPs). Particle size of formula 1 (5530 ± 320.47 nm), formula 2 (5337 ± 671.44 nm) and formula 3 (4676 ± 2215.75 nm)). The entrapment efficiency value of formula 1 drugs (33.55%), formula 2 (38.77%), formula 3 (83.75%). Based on the characterization result, the best formula was obtained at a lipid concentration of 10%, which was used for the formula of the NLC system of Chrysanthemum cinerariifolium (Trev.) Vis leaves for oral anticancer preparations

A review of biologic anti-cancer medicines

Biologic medicines prepared using living organisms by the process of biotechnology have demonstrated improved bioavailability, specificity and effectiveness in the treatment of various diseases especially cancer. Cancer is caused due to malfunctioning of the immune system, and biologic therapy can repair, stimulate, or enhance the immune response. Biologic antibodies prepared in laboratory can bind to the surface of cancer cells and target them in a specific way. They can also work synergistically with chemotherapy to improve the outcome. Since biologics utilize the immune system, it may be advantageous to use them before the immune system is compromised. In spite of these advantages, high cost of these products may limit their use. The first biologic approved for therapeutic use was biosynthetic “human” insulin made by recombinant DNA technology in 1982. Since then, biologics have had a profound effect on rheumatology, dermatology, gastroenterology, oncology, and other medical disciplines. Conventional treatments like surgery and radiotherapy are effective in case of localized tumors, but may not be effective for disseminated disease or tumors located in non-invasive areas that are difficult or dangerous to reach. Despite the potency of cytotoxic chemotherapy and the specificity of immunotherapy, neither method alone has been sufficient to eradicate the disease. There is evidence that standard chemotherapy may work in synergy with active immunization for more effective antitumor immunity, and there is great potential for the combination of these treatment modalities. This review aims to enumerate the various biologic anti-cancer preparations available in market along with their mechanism of action and intended medical use.

Recent Patents on Anti-Cancer Potential of Helenalin.

Arnica montana, containing helenalin as its principal active constituent, is the most widely used plant to treat various ailments. Recent studies indicate that Arnica and helenalin provide significant health benefits, including anti-inflammatory, neuroprotective, antioxidant, cholesterol-lowering, immunomodulatory, and most important, anti-cancer properties. The objective of the present study is to overview the recent patents of Arnica and its principal constituent helenalin, including new methods of isolation, and their use in the prevention of cancer and other ailments. Current prose and patents emphasizing the anti-cancer potential of helenalin and Arnica, incorporated as anti-inflammary agents in anti-cancer preparations, have been identified and reviewed with particular emphasis on their scientific impact and novelty. Helenalin has shown its anti-cancer potential to treat multiple types of tumors, both in vitro and in vivo. It has also portrayed synergistic effects when given in combination with other anti- cancer drugs or natural compounds. New purification/isolation techniques are also developing with novel helenalin formulations and its synthetic derivatives have been developed to increase its solubility and bioavailability. The promising anti-cancer potential of helenalin in various preclinical studies may open new avenues for therapeutic interventions in different tumors. Thus clinical trials validating its tumor suppressing and chemopreventive activities, particularly in conjunction with standard therapies, are immediately required.

Anticancer Drug Delivery Systems Based on Curcumin Nanostructures: A Review

In recent years, the application of nanostructures in biomedical and pharmaceutical fields has increased. The special designs and compositions make nanocomposites very useful alternatives to conventional materials. Curcumin is a promising anti-cancer agent that has a positive and significant effect on chemotherapeutic achievements. The anticancer properties of curcumin have been widely investigated in different forms such as nanoparticles and nanocomposite structures. Chitosan-based nanocomposites, magnetic nanoparticles, polymer nanocomposites and blends, and montmorillonite- and alginate-based nanocomposites have been used in loading curcumin for various purposes. The anticancer preparations of curcumin nanoparticles and drug release systems employing curcumin-loaded nanoparticles, electrospun nanofibers, and hydrogel nanocomposites have been investigated. This review provides a summary of the applications of nanostructures containing curcumin, especially in controlled drug release systems. The curcumin nanoparticles and nanocomposites are suitable candidates for anticancer applications. On the nano-scale, curcumin has better aqueous solubility and, if used in a nanocomposite, there is a good ability for manipulating the drug delivery system properties.

RESULTS OF IMPORT SUBSTITUTION ANALYSIS OF ANTI-CANCER MEDICATIONS IN THE RUSSIAN FEDERATION (2013–2018)

The aim. Due to the social importance of anticancer drugs, the aim of the study is to conduct a comparative analysis of the range of domestic and foreign anticancer medications included in the Lists of Vital and Essential Drugs in 2013 and 2018 in the aspect of import substitution.Materials and methods. The study was conducted by comparing the data on the registered anticancer preparations included in the list of Vital and Essential Drugs in the State Register of Medicines in 2013 and 2018. Statistical processing of the data was carried out on the basis of Fisher Z-test method.Results. All in all, there were 286 trade names of anticancer drugs registered in the Russian Federation in 2013. 94 of them, i.e. 33%, were Russian-made. In 2013, there were 19 pharmaceutical substances of domestic production in the analyzed group, which accounted for 27% of 71 INNs (International nonproprietary name). As for 71 INNs, in 2018 there were 393 registered trade names of anticancer drugs. 162 drugs, i.e. 41%, were Russian-made. From 2013 to 2018, a statistically significant positive trend of the increase in the number of domestic anticancer drugs by 8% was revealed.Conclusion. In order to increase the volume of import substitution in the production of anticancer drugs, it is necessary to provide state support to Russian manufacturers, who register domestic analogues for the first time. A particular attention should be paid to the production of domestic pharmaceutical substances, without which it is impossible to ensure the drug safety of the country.

Polymer Derivatives of Anticancer Drugs: Features of Synthesis and Biological Activity

The state of the development of polymeric derivatives of anticancer agents for selective delivery is assessed, and relevant directions for further development and improvement in this field are identified. As part of the work, the available data on polymeric derivatives of anticancer preparations was analyzed, and the relevant unsolved problems in this direction were determined. Polymer systems for the selective delivery of anticancer agents, such as polymer micelles, polymer conjugates, polymer complexes, and nanohydrogels, are considered. The analysis was performed with respect to first-line therapy preparations (doxorubicin, cisplatin, 5-fluorouracil). The features of the synthesis of polymer systems for selective delivery are considered. The main directions of binding of the drug to the polymer carrier are determined. The advantage of polymeric carriers is their high molecular weight, which ensures the best pharmacokinetic parameters. The use of water-soluble carriers makes it possible to obtain simple injection systems, and the presence of functional groups in the polymer chain enables the polymer to be modified with various drugs and vectors for tumor cells. Such systems may also contain components (vectors) that “recognize” tumor cells, which increases the level of specific drug interactions with the target cell. Folic acid can be such a vector, since the expression of its receptors is higher for some tumor cells than for normal ones. Another example is steroid hormone residue; there are a sufficient number of its receptors on the surface of cancer cells. These compounds, which are used as cancer cell vectors, are poorly soluble in water. These substances become chemically attached to a water-soluble polymer carrier at a specific concentration. The system then becomes water-soluble. There are practically no studies on the search for and use of carrier polymers with their own pharmacological activity, including antitumor and immunostimulating. Polymethacrylates are a class of anionic polymers with their own potential pharmacological activity, which is associated with activation of the immune system. There are promising areas of research in this field: the determination of the optimal conditions for the synthesis of a water-soluble anionic polymer carrier based on methacrylic acid with the characteristics of a given molecular weight; the determination of the cytotoxicity of potential polymeric carriers in an in vitro cell culture and of the dependence of the cytotoxic effect on the molecular-weight characteristics of the polymer; the production of polymeric conjugates of doxorubicin, 5-fluorouracil, cisplatin, and their combinations; the study of the effect of molecular-weight characteristics, the structure of the polymer chain, and the degree of chemical modification of (co)polymers on the release of drugs from the polymer system under conditions simulating biosystems and on the cytotoxicity of polymer conjugates in vitro and in vitro; and the determination of their own immunostimulating properties (the study of the activation of macrophages under the action of polymers) of polymeric carriers with respect to the molecular weight, polydispersity, and the presence of hydrophilic anionic groups.

α-Glucosidase Inhibitor Isolated from Blechum pyramidatum

Blechum pyramidatum (Lam.) Urb. is a species of extensive medicinal use in the American continent. In fact, antidiabetic and anticancer preparations from this plant have been patented in Mexico, even though their active constituents are not yet known. It was recently discovered that B. pyramidatum inhibits the action of the α-glucosidase enzyme, thereby corroborating the antidiabetic properties attributed to this plant. The primary purpose of this study was to identify and characterize the α-glucosidase inhibitors from this species. Bioassay-guided fractionation of a crude extract of B. pyramidatum led to the isolation of a main α-glucosidase inhibitor, Palmitic acid (IC50 237.5). This compound was identified by both spectroscopic and spectrometric analysis. Its inhibitory activity was similar to that of the antidiabetic drug acarbose (IC50 241.6 μM), which was used as a positive control in our bioassay. Kinetic analysis established that palmitic acid acted as a competitive inhibitor. Docking analysis predicted that this compound binds to the same site as acarbose does in the human intestinal α-glucosidase (PDB: 3TOP). The presence of palmitic acid in B. pyramidatum and its potent inhibitory activity against α-glucosidase enzyme provides solid evidence to support the antidiabetic use of this plant in traditional medicine.

Effect of Target Therapy on the Content of Transcription and Growth Factors, Protein Kinase TOR, and Activity of Intracellular Proteases in Patients with Metastatic Renal Cell Carcinoma.

We analyzed the dynamics of the expression of transcription factors, VEGF and its receptor VEGFR2, serine-threonine protein kinase mTOR and activity of proteasome and calpain in patients with metastatic renal cancer during therapy with tyrosine kinase inhibitor Votrient and mTOR blocker Afinitor. The expression of hypoxic nuclear factor HIF-1α in the tumor tissue decreased during therapy with the target preparations. The decrease of VEGF and its receptor VEGFR2 was observed only in patients treated with mTOR inhibitor. The increase in calpain activity in the tumor tissue was observed in both groups. These findings extend our understanding of the mechanism of action of target anticancer preparations as allow considering the studied markers as predictors in choosing optimal therapy.

A UV-Raman spectrometry method for quality control of anticancer preparations: Results after 18 months of implementation in hospital pharmacy

In France, chemotherapy preparation units of hospital pharmacy compound cytotoxic infusion bags adapted to each patient. The narrow therapeutic index of these preparations led us to implement qualitative and quantitative control for patients’ safety. To this aim, we calibrated an equipment combining UV–vis spectrometry and Raman spectroscopy (QC Prep+®) and monitored 14 different molecule–solvent combinations over a 18 months period. This rapid and specific method allowed the qualitative and quantitative analysis of 1mL sample tests in less than 2min. On 5742 anticancer preparations, we obtained accepted results with more than 99.4% solvent identification, 99.6% drug identification and only 1.52% of preparations not matching quantitative specifications (±15% of theoretical concentration). This quantitative control enabled us to pinpoint some critical points of production for two of the most common preparations. We thus updated the procedures of reconstitution and preparation, increasing the quality of final product. UV-Raman spectrometry is thus an effective tool to control chemotherapy infusions and to improve good practices of preparation.

An ion-pairing, reversed-phase liquid chromatography method to assess the cross-contamination of cancer chemotherapy infusions prepared in a dual-operator aseptic isolator.

Cytotoxics are usually prepared in a centralized pharmacy unit in a controlled hospital environment. Despite the rigorous operating procedures used for such preparations, contamination is theoretically possible - for example due to vial switches. Therefore products ought to be checked in order to determine whether quality control measures are adequate. Numerous strategies have been applied locally to ensure the safety of both patients and operators but the efficacy of these methodologies has not previously been examined. The aim of this study was to develop an analytical method sensitive enough to detect traces of anti-cancer drugs, in order to evaluate cross-contamination between infusions prepared in a dual-operator isolator in the dedicated pharmacy unit. We developed a high performance liquid chromatography (HPLC) method with ultraviolet (UV) detection to identify and quantify the following seven drugs: 5-Fluorouracil, Cytarabine, Gemcitabine, Irinotecan, Doxorubicin, Epirubicin, and Daunorubicin. We assessed the levels of cross-contamination in 20 random preparations. We achieved separation of the seven drugs in less than 28 min, with a lower limit of quantification capable of detecting cross-contamination. An assessment of 20 preparations revealed no cross-contamination. We developed a reproducible and sensitive HPLC method which could be a potentially useful tool for use in practice. We checked the level of cross-contamination in anti-cancer drug infusions and confirmed that the process in current use was safe. This study is the first to assess cross-contamination in anti-cancer preparations. This work is the first step in an extensive programme of quality control, whose aim is to ensure the safety of both patients and operators. Copyright © 2015 John Wiley & Sons, Ltd. Development of a reproducible and sensitive HPLC method capable of detecting seven anticancer drugs. This method could be used alongside MS detection, to check for biological contamination of nursing and pharmacy staff with anticancer drugs. No cross-contamination was detected in cancer chemotherapy infusions prepared in a dual-operator aseptic isolator.

Evaluation of the genome stability and mitochondrial potential of tumor cells in vivo under the action of nanoferromagnetics with different sizes of nanoparticles

The transmembrane potential and genome stability of tumor cells under nanoferromagnetic action with different sizes of nanoparticles were studied in vivo. An evaluation of the genotoxic influence of nanoeferromagnetics on tumor cells and changes in their mitochondrial potential was carried out with the application of a micronuclei test and mitochondrial fluorescent probe JC-1. Nanoferromagnetics with nanoparticle diameters of 40 and 100 nm at a concentration of 3 mg/kg were not found to deminish the trasmembrane mitochondrial potential and the genome of tumor cells and increase the micronucleus frequency of tumor cells to only a small extent. Iron nanoparticles at a concentration of 6 mg/kg were noted to demonstrate an antidromonous character of the changing mitochondrial potential and micronuclei frequency depending on their size. Iron nanoparticles with a smaller diameter were found to provoke an essential rise in the transmembrane potential of tumor cell metachondria on the background of a constant number of micronuclei, and the opposite was true for those with a greater diameter. The data obtained can serve as an important criterion for further studies in experimental oncology to create an optimal system for delivering anticancer preparations to tissue targets.

Differential signaling involved in Sutherlandia frutescens-induced cell death in MCF-7 and MCF-12A cells

Ethnopharmacological relevanceThe scientific study of natural products traditionally used in anticancer preparations has yielded several therapeutically relevant compounds. One of these traditional preparations with potentially beneficial properties is aqueous extracts of Sutherlandia frutescens, a shrub indigenous to the Western Cape region of South Africa. The aims of this study were to evaluate in vitro efficacy of these preparations on the MCF-7 breast adenocarcinoma and MCF-12A non-tumorigenic cell lines in terms of cell proliferation, cell morphology and possible induction of cell death. Materials and methodsCrystal violet staining was used to evaluate cell proliferation, light-and fluorescence microscopy were used to investigate both intracellular and extracellular morphological features of apoptosis and autophagy (e.g. membrane blebbing, condensed chromatin and intracellular lysosomes), while flow cytometry quantified cell cycle changes and induction of apoptosis through analysis of the flip-flop translocation of phosphatidylserine. ResultsCrystal violet staining showed a time- and dose specific response to aqueous Sutherlandia frutescens extracts, revealing exposure to 1mg/ml aqueous extract for 48h to be ideal for comparing the differential effects of Sutherlandia frutescens in the MCF-7 and MCF-12A cell lines. Microscopy showed distinct morphological changes with hallmarks of apoptosis being observed in both cell lines. Flow cytometry revealed a decrease in actively cycling cells in both cell lines, and a 4.36% increase in phosphatidylserine translocation in the MCF-7 cell line, indicative of apoptosis induction, while fluorescence microscopy showed evidence of the induction of autophagy. ConclusionsAnalyses revealed the carcinogenic MCF-7 cell line to be more susceptible to the cytostatic and cytotoxic effects of aqueous extracts of Sutherlandia frutescens when compared to the non-tumorigenic MCF-12A cell line, thus warranting further research into the exact cellular mechanisms involved and the possible synergistic activities of Sutherlandia frutescens ingredients.

Stability under heat accelerated condition of Dioscorealide B from the ethanolic extract of Dioscorea membranacea for Cancer Treatment

Hua-Khao-Yen-Tai (Dioscorea membranacea Pierre) have been commonly used among ingredients in Thai traditional anticancer preparations. The rhizome of D. membranacea was found potently cytotoxic and possibly contributed to such a therapeutic effect [1]. Bioassay-guided isolation was used for discovery a selective novel cytotoxic compound, dioscorealides B [2]. In this study, we aimed to determine the stability of dioscorealide B content [3] by HPLC method from ethanol extract under accelerated condition 45, 60, 70 and 80°C, 75% RH and also tested cytotoxic activity of the ethanolic extract of Dioscorea membranacea Pierre against breast human cancer cell line [MCF-7] was also determined. The results of stability of dioscorealide B from the ethanolic extract under heat-accelerated conditions, 45, 60, 70, 80°C, 75% RH for 1 month, also caused dioscorealide B remaining in the end of the exposure time decrease significant, 84.87±1.89, 61.16±3.72, 42.72±0.92 and 22.97±2.35%, respectively. Even though, the cytotoxic activity against MCF-7 of all samples of every condition were not changed significantly.

Synthesis of N-aminoglycoside from the monoethanolamine vinyl ether

It is known that the introduction of carbohydrate fragments into the molecules of physiologically active substances not only increases their solubility in water and considerably decreases their toxicity [1–3], but it also makes it possible to transport a drug into the desired part of living organism cells. The modified derivatives of saccharides are of great scientific and practical interest because many of them possess a pronounced broad-spectrum biological activity [4] and are widely used in medicine, for example, as effective antiviral and anticancer preparations [5, 6]. Vinyl ether of monoethanolamine derivatives are used as intermediates in the syntheses of compounds possessing analgesic, psychtropic [7], and radio-protective properties [8]. In [9] synthetic approaches to glycosides based on monoethanolamine were suggested. Optimal conditions for synthesis and isolation of the desired products were shown. However, aminoglycosides based on the monoethanolamine vinyl ether were not reported. In this work we obtained and described a mono-ethanolamine vinyl ether

Dioscorealides and Dioscoreanone, Novel Cytotoxic Naphthofuranoxepins, and 1,4‐Phenanthraquinone from Dioscorea membranacea Pierre.

AbstractFor Abstract see ChemInform Abstract in Full Text.