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Journal Article Bollettino Chimico Farmaceutico Get access W. Kenneth Fitch W. Kenneth Fitch Publications Manager The Pharmaceutical Society of Great Britain and former Editor of The Pharmaceutical Journal Search for other works by this author on: Oxford Academic Google Scholar American Journal of Hospital Pharmacy, Volume 18, Issue 11, 1 November 1961, Pages 662–663, https://doi.org/10.1093/ajhp/18.11.662 Published: 01 November 1961
Environmentally friendly alternatives have become sought after upon the development of scientific research and industrial processes. Recent trends suggest biodegradable polymers as the most promising solution for synthetic microcapsule systems. Safety, efficiency, biocompatibility, and biodegradability are some of the properties that biodegradable systems in microencapsulation can provide for a broad spectrum of applications. The controlled release of encapsulated active agents is a research field that, over the years, has been constantly innovating due to the promising applications in the areas of pharmaceutical, cosmetic, textile industry, among others. This article presents an overview of different polymers with potential for microcapsule synthesis, namely, biodegradable polymers. First, natural polymers are discussed, which are divided into two categories: polysaccharide-based polymers (cellulose, starch, chitosan, and alginate) and protein polymers (gelatin). Second, synthetic polymers are described, where biodegradable polymers such as polyesters, polyamides, among others appear as examples. For each polymer, this review presents its origin, relevant properties, applications, and examples found in the literature regarding its use in biodegradable microencapsulation systems.
Cinnamon (Cinnamomum zeylanicum, and Cinnamon cassia), the eternal tree of tropical medicine, belongs to the Lauraceae family. Cinnamon is one of the most important spices used daily by people all over the world. Cinnamon primarily contains vital oils and other derivatives, such as cinnamaldehyde, cinnamic acid, and cinnamate. In addition to being an antioxidant, anti-inflammatory, antidiabetic, antimicrobial, anticancer, lipid-lowering, and cardiovascular-disease-lowering compound, cinnamon has also been reported to have activities against neurological disorders, such as Parkinson's and Alzheimer's diseases. This review illustrates the pharmacological prospective of cinnamon and its use in daily life.
Aim of the Review. To grasp the fragmented information available on the botany, traditional uses, phytochemistry, pharmacology, and toxicology of Olea europaea to explore its therapeutic potential and future research opportunities. Material and Methods. All the available information on O. europaea was collected via electronic search (using Pubmed, Scirus, Google Scholar, and Web of Science) and a library search. Results. Ethnomedical uses of O. europaea are recorded throughout the world where it has been used to treat various ailments. Phytochemical research had led to the isolation of flavonoids, secoiridoids, iridoids, flavanones, biophenols, triterpenes, benzoic acid derivatives, isochromans, and other classes of secondary metabolites from O. europaea. The plant materials and isolated components have shown a wide spectrum of in vitro and in vivo pharmacological activities like antidiabetic, anticonvulsant, antioxidant, anti-inflammatory, immunomodulatory, analgesic, antimicrobial, antiviral, antihypertensive, anticancer, antihyperglycemic, antinociceptive, gastroprotective, and wound healing activities. Conclusions. O. europaea emerged as a good source of traditional medicine for the treatment of various ailments. The outcomes of phytochemical and pharmacological studies reported in this review will further expand its existing therapeutic potential and provide a convincing support to its future clinical use in modern medicine.
Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attentionbecause of its unique bioisosteric properties and an unusually wide spectrum of biological activities.Thus, it is a perfect framework for the novel drug development. After a century since the1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists'attention, leading to the discovery of a few presently accessible drugs containing 1,2,4-oxadiazoleunit. It is worth noting that the interest in a 1,2,4-oxadiazoles' biological application has been doubledin the last fifteen years. Herein, after a concise historical introduction, we present a comprehensiveoverview of the recent achievements in the synthesis of 1,2,4-oxadiazole-based compounds and themajor advances in their biological applications in the period of the last five years as well as briefremarks on prospects for further development.
Traditional knowledge is an important source of obtaining new phytotherapeutic agents. Ethnobotanical survey of medicinal plants was conducted in Nossa Senhora Aparecida do Chumbo District (NSACD), located in Poconé, Mato Grosso, Brazil using semi-structured questionnaires and interviews. 376 species of medicinal plants belonging to 285 genera and 102 families were cited. Fabaceae (10.2%), Asteraceae (7.82%) and Lamaceae (4.89%) families are of greater importance. Species with the greater relative importance were Himatanthus obovatus (1.87), Hibiscus sabdariffa (1.87), Solidago microglossa (1.80), Strychnos pseudoquina (1.73) and Dorstenia brasiliensis, Scoparia dulcis L., and Luehea divaricata (1.50). The informant consensus factor (ICF) ranged from 0.13 to 0.78 encompassing 18 disease categories,of which 15 had ICF greater than 0.50, with a predominance of disease categories related to injuries, poisoning and certain other consequences of external causes (ICF = 0.78) having 65 species cited while 20 species were cited for mental and behavioral disorders (ICF = 0.77). The results show that knowledge about medicinal plants is evenly distributed among the population of NSACD. This population possesses medicinal plants for most disease categories, with the highest concordance for prenatal, mental/behavioral and respiratory problems.
Cinnamon is used to flavor most foods in Arabian countries. The aim of this study was to evaluate the medicinal importance, reflecting an important trend in research. The hepatoprotective activity of aqueous and ethanolic extracts of cinnamon was investigated against carbon tetrachloride (CC1(4)) induced lipid peroxidation and hepatic injury in rats. The elevated serum AST and ALT enzymatic activities induced by CC1(4) were significantly restored to near normal by oral administration of 200 mg/kg of either extracts once daily for 7 days, as compared to untreated rats. There was a significant elevation in the level of liver malondialdhyde (MDA), while the activities of antioxidant enzymes superoxide dismutase and catalase (SOD and CAT) were significantly decreased in CC1(4) intoxicated rats. The results obtained indicated that ethanolic extract has more potent hepatoprotective action than water extract against CC1(4) by lowering the MDA level and elevating antioxidants enzymes activities (SOD and CAT). The possible mechanism of this activity may be free radical-scavenging polyphenol compounds. The hepatoprotective properties were documented by the histopathological data obtained. Consequently, this extract can be used as a therapeutic regime in treatment of some hepatic disorders without any side effects. Further study will be done for separation and identification of active components and for testing antitumor activity.
OBJECTIVES: Enzymatic acetylation of the antitubercular isoniazid (INH) by N-acetyltransferase represents a major metabolic pathway for INH in human beings. Acetylation greatly reduces the therapeutic activity of the drug, resulting in underdosing, decreased bioavailability and acquired INH resistance. Chemical modification of INH with a functional group that blocks acetylation, while maintaining strong antimycobacterial action, may improve clinical outcomes and help reduce the rise of INH resistance. The goal of this study was to probe activities, toxicity and bioavailability of an investigational compound prepared by this chemical modification. METHODS: The investigational compound was chosen from a cohort of lipophilic antitubercular INH Schiff bases based on its strong activity in primary assays. The compound was evaluated in vitro, in vivo in mice, in mutagenicity tests and in rats for bioavailability. RESULTS: The INH Schiff base acts against both intracellular and extracellular organisms in vitro, with a wide range between active and cytotoxic concentrations. The material is active against non-tubercular mycobacteria. The INH Schiff base is non-mutagenic in the Ames test and has excellent bioavailability in Sprague-Dawley rats, achieving early peak plasma concentrations approximately three orders of magnitude above its MIC when administered orally. In tuberculosis-infected mice the compound is well tolerated and in a 4 week study provides 3 log cfu reduction in spleens and 4 log cfu reduction in lungs. CONCLUSION: The results demonstrate that investigational compounds in which N-acetylation of INH is blocked by chemical modification can display strong activity, low toxicity and excellent bioavailability, making them suitable for further exploration.
Liver disease is one of the major causes of morbidity and mortality across the world. According to WHO estimates, about 500 million people are living with chronic hepatitis infections resulting in the death of over one million people annually. Medicinal plants serve as a vital source of potentially useful new compounds for the development of effective therapy to combat liver problems. Moreover herbal products have the advantage of better affordability and acceptability, better compatibility with the human body, and minimal side effects and is easier to store. In this review attempt has been made to summarize the scientific data published on hepatoprotective plants used in Saudi Arabian traditional medicine. The information includes medicinal uses of the plants, distribution in Saudi Arabia, ethnopharmacological profile, possible mechanism of action, chemical constituents, and toxicity data. Comprehensive scientific studies on safety and efficacy of these plants can revitalise the treatment of liver diseases.
A Casearia sylvestris (Flacourtiaceae) é uma planta popularmente conhecida como "guaçatonga" e é usada por povos indígenas da América do sul (Brasil, Peru e Bolivia) no tratamento de muitas doenças, incluindo câncer. Estudos citotóxicos mostraram que esta planta apresenta um possível e interessante potencial antitumoral devido à presença de moléculas chamadas casearinas. Além disso, a composição do óleo essencial mostrou uma alta concentração de sesquiterpenos de alto potencial citotóxico. Neste trabalho, nós verificamos que o óleo essencial da C. sylvestris apresentou uma boa citotoxicidade seletiva contra as linhagens de células tumorais HeLa, A-549 and HT-29 (CD50 63,3, 60,7 e 90,6 µg.ml-1, respectivamente) quando comparada às células não-tumorais Vero (CD50 210,1 µg.ml-1) e macrófagos de camundongos (CD50 234,0 µg.ml-1). Além disso, o óleo causou hemólise em sete diferentes tipos de eritrócitos, indicando que a C. sylvestris precisa ser usada com cuidado. Também foram testados padrões de β-cariofileno e α-humuleno que mostraram citotoxicidade similar àquelas apresentadas pelo óleo, indicando que estes compostos podem ser os responsáveis pelos efeitos tóxicos que foram observados neste estudo.
Ethnobotanical study of the Sannio area, in the province of Benevento (SE-Italy) has been carried out on the basis of both bibliographic sources and interviews in the field. In total 365 species in 59 families were identified. Of these species, 361 are medicinal plants, 82 for anthropic use and 35 for veterinary use.RiassuntoUno studio etnobotanico del Sannio, in provincia di Benevento (SE-Italy), è stato effettuato sia sulla base di fonti bibliografiche che di interviste in campo. In totale, 365 specie di 59 famiglie sono state censite. Di queste specie, 265 sono piante medicinali, 82 per uso antropico e 35 per uso veterinario.
BACKGROUND: Naproxen, a non-steroidal anti-inflammatory drug, is used to treat various painful conditions including postoperative pain, and is often administered as the sodium salt to improve its solubility. This review updates a 2004 Cochrane review showing that naproxen sodium 550 mg (equivalent to naproxen 500 mg) was effective for treating postoperative pain. New studies have since been published. OBJECTIVES: To assess efficacy, duration of action, and associated adverse events of single dose oral naproxen or naproxen sodium in acute postoperative pain in adults. SEARCH STRATEGY: We searched Cochrane CENTRAL, MEDLINE, EMBASE and the Oxford Pain Relief Database for studies to October 2008. SELECTION CRITERIA: Randomised, double blind, placebo-controlled trials of single dose orally administered naproxen or naproxen sodium in adults with moderate to severe acute postoperative pain. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trial quality and extracted data. Pain relief or pain intensity data were extracted and converted into the dichotomous outcome of number of participants with at least 50% pain relief over four to six hours, from which relative risk and number-needed-to-treat-to-benefit (NNT) were calculated. Numbers of participants using rescue medication over specified time periods, and time to use of rescue medication, were sought as additional measures of efficacy. Information on adverse events and withdrawals were collected. MAIN RESULTS: The original review included 10 studies with 996 participants. This updated review included 15 studies (1509 participants); 11 assessed naproxen sodium and four naproxen. In nine studies (784 participants) using 500/550 mg naproxen or naproxen sodium the NNT for at least 50% pain relief over four to six hours was 2.7 (95% CI 2.3 to 3.2). No dose response was demonstrated over the range 200/220 mg to 500/550 mg, but limited data was identified. Median time to use of rescue medication was 8.9 hours for naproxen 500/550 mg and 2.0 hours for placebo. Use of rescue medication was significantly less common with naproxen than placebo. Associated adverse events were generally of mild to moderate severity and rarely led to withdrawal. AUTHORS' CONCLUSIONS: Doses equivalent to 500 mg and 400 mg naproxen administered orally provided effective analgesia to adults with moderate to severe acute postoperative pain. About half of participants treated with these doses experienced clinically useful levels of pain relief, compared to 15% with placebo, and half required additional medication within nine hours, compared to two hours with placebo. Associated adverse events did not differ from placebo.
Since the introduction of cisplatin to oncology in 1978, Pt(II) and Pd(II) compounds have been intensively studied with a view to develop the improved anticancer agents. Polynuclear polyamine complexes, in particular, have attracted special attention, since they were found to yield DNA adducts not available to conventional drugs (through long-distance intra- and interstrand cross-links) and to often circumvent acquired cisplatin resistance. Moreover, the cytotoxic potency of these polyamine-bridged chelates is strictly regulated by their structural characteristics, which renders this series of compounds worth investigating and their synthesis being carefully tailored in order to develop third-generation drugs coupling an increased spectrum of activity to a lower toxicity. The present paper addresses the latest developments in the design of novel antitumor agents based on platinum and palladium, particularly polynuclear chelates with variable length aliphatic polyamines as bridging ligands, highlighting the close relationship between their structural preferences and cytotoxic ability. In particular, studies by vibrational spectroscopy techniques are emphasised, allowing to elucidate the structure-activity relationships (SARs) ruling anticancer activity.
Abstract This study was conducted to evaluate the toxic effects of an azo dye carmoisine widely used in foods and to investigate its relation to carcinogenicity. Carmoisine administered into mice orally in four different doses as control, low, medium, and high equivalent to 0, 4, 200, and 400 mg/kg bw, respectively, for 120 days. The key toxicological endpoint was observed including animal body weight, organ weights, hematology, biochemistry, and molecular biology assessment. The body weights of medium‐ and high‐dose carmoisine‐treated mice group were significantly decreased as compared to the control mice group. Platelet, white blood cell and monocyte counts of treated group were considerably higher, while Hb and red blood cell counts were drastically lower than the control group. The biochemical parameters such as serum alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, total protein, globulin, urea, and creatinine level were significantly increased, while serum cholesterol level was decreased after treatment as compared to the control. RT ‐ PCR results showed that expression of Bcl‐x and PARP gene was intensively increased, whereas expression of p 53 gene was decreased in the mouse liver tissues treated with carmoisine. This study revealed that high‐dose (400 mg/kg bw) treatment of carmoisine was attributable to renal failure and hepatotoxicity. It also would be suspected as a culprit for liver oncogenesis.
Selenium is considered to be one of the most controversial trace elements. On the one hand, it is toxic at high doses and there is a great body of information related to environmental issues of Se contamination. On the other hand, Se deficiency is a global problem related to an increased susceptibility to various diseases of animals and humans and decreased productive and reproductive performance of farm animals. Optimisation of Se nutrition of poultry and farm animals will result in increased efficiency of egg, meat and milk production and even more important, will improve quality. From the data presented in the review it is clear that the main lesson which we have to learn from nature is how to use organic selenium in animal and human diets. Selenium-enriched yeast (Sel-Plex) is the result of such a lesson and it is just a matter of time before animal nutrition moves completely from using ineffective sodium selenite to organic selenium. Other lessons from nature will follow. Recent advances in genomics and proteomics, in association with descriptions of new selenoproteins, will be a driving force in reconsidering old approaches related to Se nutrition. Probably 90% of all Se research has been conducted with sodium selenite and we now understand that the natural form of selenium is different. The main advances in Se status assessment and Se requirements were established based on the activity of glutathione peroxidase (GSH-Px), an enzyme which for many years was considered to be the main selenoprotein. Recently it was discovered that it is only one of at least 25 various selenoproteins. Se research and practical applications are developing quickly and they are very exciting and promising.
Hydrolyzing the amorphous region while keeping the crystalline region unaltered is the key technology for producing nanocellulose. This study investigated if the dissolution properties of the amorphous region of microcrystalline cellulose can be enhanced in the presence of Fe3+ salt in acidic medium. The process parameters, including temperature, time and the concentration of metal chloride catalyst (FeCl3), were optimized by using the response surface methodology (RSM). The experimental observation demonstrated that temperature and time play vital roles in hydrolyzing the amorphous sections of cellulose. This would yield hydrocellulose with higher crystallinity. The factors that were varied for the production of hydrocellulose were the temperature (x1), time (x2) and FeCl3 catalyst concentration (x3). Responses were measured in terms of percentage of crystallinity (y1) and the yield (y2) of the prepared hydrocellulose. Relevant mathematical models were developed. Analysis of variance (ANOVA) was carried out to obtain the most significant factors influencing the responses of the percentage of crystallinity and yield. Under optimum conditions, the percentage of crystallinity and yield were 83.46% and 86.98% respectively, at 90.95 °C, 6 h, with a catalyst concentration of 1 M. The physiochemical characteristics of the prepared hydrocellulose were determined in terms of XRD, SEM, TGA and FTIR analyses. The addition of FeCl3 salt in acid hydrolyzing medium is a novel technique for substantially increasing crystallinity with a significant morphological change.
Legumes are indispensable for human diet in respect to their valuable and nutritive bioactive molecules. Legumes and derivative foodstuffs are rich in fiber, proteins, vitamins and some valuable phytochemicals, which exhibit important biological activities. Due to their remarkable molecular content, they are receiving great attention by researchers. Recent developments in genomics and bioinformatics led to cumulative data about legume genomes. These data could provide important information to accelerate breeding and to develop new traits for biofortification. The main focus of this review is to present their distinctive genomic properties by summarizing significant studies conducted with relatively newly developed techniques revealing the beneficial effects of bioactive molecules from legumes on human health.
Organic acid hydrazides include a vast group of organic derivatives of hydrazines containing the active functional group (-C(=O)NHNH2). Acid hydrazones were important bidentate ligands and show keto-enol (amido-iminol) tautomerism. They usually exist in keto form in the solid-state while in equilibrium between keto and enol forms in solution state. Such hydrazones were synthesized in the laboratory by heating substituted hydrazides or hydrazines with corresponding aldehydes or ketones in different organic solvents such as ethanol, methanol, butanol, tetrahydrofuran, etc., and some cases with the ethanol-glacial acetic acid or acetic acid alone. Hydrozones are very important intermediates for the synthesis of heterocyclic compounds and also have different biological activities. The organic chemist would have more interest in the synthesis of acid hydrazides and their derivatives because of their properties. These derivatives having wide applications as chemical preservers for plants, drugs, for manufacturing polymers, glues, etc., in industry and many other purposes. These acid hydrazides and their derivatives were found to be useful synthons for various heterocyclic five, six or seven-membered rings with one or more heteroatoms that were exhibited great biological, pharmacological and industrial applications. This paper will present a review of the chemistry and pharmacological potentials of hydrazide-hydrazones. The various synthetic routes for hydrazone, as well as antibacterial, antifungal and antiviral potentials, have been elaborated in brief.
The objective of the present study was to design ophthalmic delivery systems based on polymeric carriers that undergo sol-to-gel transition upon change in temperature or in the presence of cations so as to prolong the effect of HP- β -CD Voriconazole (VCZ) in situ gelling formulations. The in situ gelling formulations of Voriconazole were prepared by using pluronic F-127 (PF-127) or with combination of pluronic F-68 (PF-68) and sodium alginate by cold method technique. The prepared formulations were evaluated for their physical appearance, drug content, gelation temperature (T gel), in vitro permeation studies, rheological properties, mucoadhesion studies, antifungal studies, and stability studies. All batches of in situ formulations had satisfactory pH ranging from 6.8 to 7.4, drug content between 95% and 100%, showing uniform distribution of drug. As the concentration of each polymeric component was increased, that is, PF-68 and sodium alginate, there was a decrease in T gel with increase in viscosity and mucoadhesive strength. The in vitro drug release decreased with increase in polymeric concentrations. The stability data concluded that all formulations showed the low degradation and maximum shelf life of 2 years. The antifungal efficiency of the selected formulation against Candida albicans and Asperigillus fumigatus confirmed that designed formulation has prolonged effect and retained its properties against fungal infection.
Flavonoid content was determined spectrophotometrically, and organic acid concentrations by HPLC. The content of the studied compounds varied greatly. Interspecific differences in the amount of flavonoids and ascorbic acid were highly significant. The most common species, Rosa canina, showed low average content of vitamin C (0.51 g/100 g of dry matter) and flavonoids (41 mg/100 g DM) and high content of citric acid (3.48 g/100 g DM). Ascorbic acid was highest in R. villosa hips (avg. 2.25 g/100 g DM), flavonoids were highest in R. rubiginosa (72 mg/100 g DM), and citric acid was highest in R. tomentosa (4.34 g/100 g DM). Flavonoid level correlated negatively with the amount of citric acid (r=-0.47, p<0.001). Cluster analysis of rose species based on the content of the investigated compounds confirmed the validity of the division of sect. Caninae into three subsections: Rubiginosae, Vestitae and Rubrifoliae. The phytochemical variation of these roses reflects their probable phylogenetic relationships as determined from morphology.