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1.
Article in English | MEDLINE | ID: mdl-38967078

ABSTRACT

Dr. Aloysius Alzheimer, a German neuropathologist and psychiatrist, recognized the primary instance of Alzheimer's disease (AD) for a millennium, and this ailment, along with its related dementias, remains a severe overall community issue related to health. Nearly fifty million individuals worldwide suffer from dementia, with Alzheimer's illness contributing to between 60 and 70% of the instances, estimated through the World Health Organization. In addition, 82 million individuals are anticipated to be affected by the global dementia epidemic by 2030 and 152 million by 2050. Furthermore, age, environmental circumstances, and inherited variables all increase the likelihood of acquiring neurodegenerative illnesses. Most recent pharmacological treatments are found in original hypotheses of disease, which include cholinergic (drugs that show affective cholinergic system availability) as well as amyloid-accumulation (a single drug is an antagonist receptor of Nmethyl D-aspartate). In 2020, the FDA provided approval on anti-amyloid drugs. According to mounting scientific data, this gut microbiota affects healthy physiological homeostasis and has a role in the etiology of conditions that range between obesity and neurodegenerative disorders like Alzheimer's. The microbiota-gut-brain axis might facilitate interconnection among gut microbes as well as the central nervous system (CNS). Interaction among the microbiota-gut system as well as the brain occurs through the "two-way" microbiota-gut-brain axis. Along this axis, the stomach as well as the brain develop physiologically and take on their final forms. This contact is constant and is mediated by numerous microbiota-derived products. The gut microbiota, for instance, can act as non-genetic markers to set a threshold for maintaining homeostasis or getting ill. The scientific community has conducted research and found that bowel dysbiosis and gastrointestinal tract dysregulation frequently occur in Alzheimer's disease (AD) patients. In this review, the effects of the microbiota- gut-brain axis on AD pathogenesis will be discussed.

2.
Article in English | MEDLINE | ID: mdl-35538829

ABSTRACT

BACKGROUND AND PURPOSE: Alzheimer's disease (AD) is a degenerative neurological disorder that impairs memory, cognitive abilities, and the ability to do even most everyday activities. This neurodegenerative disease is growing increasingly common as the world's population ages. Here we reviewed some of the key findings that have shown the function of Aß peptide, oxidative stress, free radical damage Triggering Receptors Expressed on Myeloid Cells 2 (TREM2), Nitric Oxide (NO), and gut microbiota in the aetiology of AD. METHODOLOGY: The potentially relevant online medical databases, namely, PubMed, Scopus, Google Scholar, Cochrane Library, and JSTOR were exhaustively researched. In addition, the data reported in the present study were primarily intervened on the basis of the timeline selected from 1 January 2000 to 31 October 2021. The whole framework was designed substantially based on key terms and studies selected by virtue of their relevance to our investigations. RESULTS: Findings suggested that channels of free radicals, such as transition metal accumulation, and genetic factors are mainly accountable for the redox imbalance that assist to understand better the pathogenesis of AD and incorporate new therapeutic approaches. Moreover, TREM2 might elicit a protective function for microglia in AD. NO causes an increase in oxidative stress and mitochondrial damage, compromising cellular integrity and viability. The study also explored that the gut and CNS communicate with one another and that regulating gut commensal flora might be a viable therapeutic for neurodegenerative illnesses like AD. CONCLUSION: There are presently no viable therapies for Alzheimer's disease, but recent breakthroughs in our knowledge of the disease's pathophysiology may aid in the discovery of prospective therapeutic targets.

3.
Curr Top Med Chem ; 22(6): 425-434, 2022.
Article in English | MEDLINE | ID: mdl-35040402

ABSTRACT

Flavonoids are the secondary plant metabolites with diversities of pharmacological activities like antioxidant, anticancer, anti-inflammatory, hepatoprotective, free radical scavenging activity and antiviral activities. Flavonoids have also been proved as a major contributor to an antimicrobial phytochemical. Being the major substituent of antibiotics, today flavonoids have attained great attention as there is an increase in the persistence of untreatable microbial infections due to microbial resistance. This review demonstrates the screening, isolation of extracts and derivatization of various flavonoids and their evaluation for antimicrobial potency. Recent advancements of various derivatives of flavonoids having antimicrobial activity have also been discussed in this review. This review helps researchers to get vast knowledge about flavonoids and also gives an idea for the current scenario of flavonoids and their applications as an antimicrobial agent.


Subject(s)
Anti-Infective Agents , Flavonoids , Anti-Bacterial Agents/pharmacology , Anti-Infective Agents/pharmacology , Antioxidants/pharmacology , Flavonoids/pharmacology , Phytochemicals/pharmacology , Plant Extracts/pharmacology
4.
Biomedicine (Taipei) ; 9(3): 17, 2019 Sep.
Article in English | MEDLINE | ID: mdl-31453798

ABSTRACT

Ba.ckground: Sunscreen formulations primarily offer protection against UV induced damages however nowadays it also maintains skin natural physiological conditions. Current global market is flooded with numerous sunscreen products which offer protection to skin against several UV induced damages. However most of these sunscreen formulations offers narrow spectrum protection against UV and also suffer from stability as well as toxicity related issues. METHODS: Present work aims to isolate mycosporine amino acid (Mgy) from green alga namely Ulva fasciata (U. fasciata) and study its sunscreen potential against widely used domestic marketed formulation. Stability evaluations were also performed for almost 90 days. RESULTS: Results demonstrated that the isolated compound, mycosporine glycine (Mgy) preserved physicochemical properties of the product and offered good stability for all formulations throughout the experimental period. Furthermore, Mgy loaded carbopol gel showed better sunscreen protection against marketed formulation in a concentration dependent manner. (7.709). CONCLUSION: (6.806) Novel Myg loaded gel was proved to demonstrate several quality characteristics that may unlock new prospects for the production of more efficient, safe, and economic skin-care products.

5.
Biomedicine (Taipei) ; 9(1): 3, 2019 Mar.
Article in English | MEDLINE | ID: mdl-30794150

ABSTRACT

BACKGROUND: Current investigation explores the anti-oxidant and antinociceptive potential of edible seaweed namely Porphyra vietnamensis. METHODS: Radical scavenging and antinociceptive potential of ethanolic (EE), aqueous (AE), acetone (ACE) and chloroform (CE) fractions were determined using various models and assays. Writhing, formalin, hot plate, acetic acid induce response models were performed to determine antinociceptive activity whereas different assays have been used to determine antioxidant potential. RESULTS: Among the various fractions, ACE showed maximum biological activity. In DPPH assay half maximal inhibitory concentration (IC50) was found to be 0.470 ug/ml (DPPH assay), 0.381 jug/m/ (H2O2 assay), 0.470 ug/ml (super oxide assay), 0.591ug/ml (lipid peroxidation) and 0.430 ug/ml (nitric oxide assay). However, comparatively the TPC was more in EE (977.0 mg GAE/gm DW). CONCLUSION: It was concluded that acetone fraction of Porphyra showed marked antinociceptive and antioxidant activities, however pharmacological and chemical investigations are required to identify principle compounds responsible for activities and characterize their respective mechanism(s) for respective actions.

6.
Life Sci ; 219: 90-99, 2019 Feb 15.
Article in English | MEDLINE | ID: mdl-30639280

ABSTRACT

Insulin remains a predominant life-saving medication for type 1 and type 2 Diabetes Mellites. Natural insulin secretion limits the fluctuation of the narrow and high surge of blood glucose levels. However, imitating the same by external insulin remains a challenge as a variety of insulin analogs (rapid acting, short acting, intermediate acting and long-acting) have different pharmacokinetic (PK) and pharmacodynamic (PD) properties. Inconsistent reduction in overall hyperglycemia level and nocturnal hypoglycemia due to variable absorption time and time action profile predominantly highlights the need of revisiting the PK/PD of insulin analogs as single analog is not yet sufficed to replace internal insulin exogenously. Combination therapy with basal and prandial insulins or intensification of hypoglycemic therapy with premixed insulins are of prime importance in managing diabetes effectively, imitating the natural insulin secretion. Therefore, the knowledge of PK/PD properties might help a practitioner to design, implement and manage insulin replacement therapy effectively and averting adverse events. Present study reports the comparative analysis of PK/PD profile of various insulin analogs based on the concurrent information about clinical aspects. Moreover, study interlinks the major concerns of therapeutic efficacy of insulin analogs with their respective onset of action and duration of effectiveness and reported adverse drug reaction which explore the scope of improvement.


Subject(s)
Diabetes Mellitus/drug therapy , Insulin/analogs & derivatives , Forecasting , Humans , Insulin/therapeutic use , Insulin Aspart/therapeutic use , Insulin Detemir/therapeutic use , Insulin Glargine/therapeutic use , Insulin Lispro/therapeutic use , Insulin, Long-Acting/therapeutic use
7.
Curr Drug Deliv ; 14(3): 364-376, 2017.
Article in English | MEDLINE | ID: mdl-27834152

ABSTRACT

BACKGROUND: Resveratrol belonging to stilbene family has emerged as a leading candidate for enhancing the health span by potentially decreasing the aging process and reducing chronic diseases. OBJECTIVE: The aim of this review is to focus on various studies related to chemical composition l, pharmacological activities, bioavailability problems associated with resveratrol. In addition, it includes section discussing the challenges associated with drug and strategies to improve resveratrol solubility, stability and bioavailability. Current Scenario: It is being revealed currently in various literature that resveratrol is a potential drug candidate with multi-spectrum pharmacological applications. The poor bioavailability of resveratrol in humans is a matter of great concern for transforming basic science findings into clinical application. Although couple of research projects have emerged from human clinical trials, however results are conflicting, that may partially belong to defined dosing protocols. A number of theoretical methods have been developed to improve the bioavailability of resveratrol, including micronization of particles which are combined with additional phytochemicals, novel delivery systems, and nanotechnology applied formulations. CONCLUSION: If bioavailability is such a limitation in the clinical application of resveratrol, then methods need to be optimized for resveratrol formulations. Drug stability needs to be improved, so that the bioavailability enhances and side-effects of resveratrol reduces. The novel drug delivery systems have been designed to bring this potential molecule to the first line treatment of diseases. This review focuses on the current bioavailability literature, reveals data from humans, and provides suggested actions to be taken for future research.


Subject(s)
Biological Availability , Stilbenes/pharmacology , Chemistry, Pharmaceutical , Drug Delivery Systems , Humans , Resveratrol , Solubility
8.
Article in English | WPRIM (Western Pacific) | ID: wpr-287173

ABSTRACT

Plants are the real basis towards animal life and are also central to people's livelihood. The contributions of the plants in performing varied religious celebrations and in other multiple beneficiaries like medicine, human happiness as well as in treating deadly diseases can never be neglected. In treating diseases, the plants and their constituents are better choice than any other synthetic chemical. The nature has been kind enough to provide the human beings with various types of medicinal plants and in the real sense these form the storehouse of curing almost all the ailments. Consequently, most of the drugs which are being used in preparing formulations have their origin and roots in the plants which form the chief natural source of medicines. Even in modern era, the plant-derived drugs are being extensively used, either in their original or semi-synthetic form. It is because their natural phytoconstituents are highly innocuous posing relatively fewer or no side effects. Based upon their observations, analysis and experience, our ancestors used many plants for medicinal purposes and thus their efforts need to be supported by scientific evidence. Jasminum grandiflorum Linn. is one of such important plants. It has been extensively used by the tribes all over India to treat different diseases which mainly include body pains, toothache, stomach ache, ulcers, and sexual impotency. Chemistry of the plant revealed the presence of mainly secoiridoids, terpenoids, flavonoids and tannins. Not much scientific support was given to the folklore claims for this plant but some of its traditional uses were investigated like spasmolytic, wound healing, antimicrobial, angiotensin converting enzyme inhibitor, antiulcer and antioxidant activities. This article is the review of research works done on the plant Jasminum grandiflorum Linn. to date. As a part of it the local names, morphology, traditional claims, chemistry and pharmacological activities have been discussed.


Subject(s)
Animals , Humans , Clinical Trials as Topic , Jasminum , Chemistry , Phytotherapy , Plant Extracts , Chemistry , Pharmacology
9.
Pharm Dev Technol ; 18(2): 313-22, 2013.
Article in English | MEDLINE | ID: mdl-21699389

ABSTRACT

CONTEXT: Colchicine (CLC) causes cell death by destabilizing the tubulin unit. However, it ionizes at physiological pH resultant low bioavailability and therapeutic efficacy. OBJECTIVES: We have attempted to augment the bioavailability of CLC by fabricating the inclusion complex with hydroxypropyl-ß-cyclodextrin (HP-ß-CD). MATERIALS AND METHODS: CLC-HP-ß-CD inclusion complex was prepared and evaluated with Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy, (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy and rotating frame overhauser enhancement spectroscopy (ROESY). Oral bioavailability of CLC-HP-ß-CD inclusion complex was analyzed using high performance liquid chromatography method. RESULTS AND DISCUSSION: Our phase-solubility data indicated the formation of a stable complex with K(c) ~0.31 mM(-1) at pH 7.4. (1)H NMR ascertains that NHCOCH(3) moiety of CLC enters in the HP-ß-CD cavity and deshielded the H-3 and H-5 protons. ROESY also correlates the H(f) and H(g) of CLC with H-3 and H-5 protons of HP-ß-CD and indicates that H(f) and H(g) protons of CLC are present either as cis and/or trans form in CLC-HP-ß-CD inclusion complex. Pharmacokinetic studies showed a 1.82-fold increase in absolute bioavailability of CLC upon complexation. CONCLUSION: CLC-HP-ß-CD inclusion complex may potentially be used as a viable formulation of CLC.


Subject(s)
Colchicine/chemistry , Colchicine/pharmacokinetics , beta-Cyclodextrins/chemistry , 2-Hydroxypropyl-beta-cyclodextrin , Animals , Biological Availability , Calorimetry, Differential Scanning/methods , Chemistry, Pharmaceutical/methods , Colchicine/administration & dosage , Female , Hydrogen-Ion Concentration , Magnetic Resonance Spectroscopy/methods , Male , Mice , Protons , Random Allocation , Solubility , Spectroscopy, Fourier Transform Infrared/methods , X-Ray Diffraction/methods , beta-Cyclodextrins/administration & dosage , beta-Cyclodextrins/pharmacokinetics
10.
J Ayurveda Integr Med ; 4(4): 211-5, 2013 Oct.
Article in English | MEDLINE | ID: mdl-24459387

ABSTRACT

BACKGROUND: The genus Amaranthus has potential activity as a hepatoprotective agent. OBJECTIVE: The present pharmacological investigation focuses on evaluation of the efficacy of aqueous extract of roots of Amaranthus tricolor Linn. for their protection against paracetamol (PCM) overdose induced hepatotoxicity. MATERIALS AND METHODS: The aqueous extract of roots of A. tricolor Linn. was prepared and phytochemical screening was done. The biochemical investigation viz. serum glutamic oxaloacetate transaminase (SGOT), serum glutamic pyruvate transaminase (SGPT), alkaline phosphatase (ALP) and total Bilirubin (TB) was done against PCM-induced hepatotoxicity in wistar albino rats. The histopathological studies of liver were also done. RESULTS: The phytochemical screening of the aqueous extract showed the presence of alkaloids, carbohydrates, flavanoids, amino acids, proteins, fixed oil, saponins and tannins, and phenolic compounds. Pretreatment with the aqueous extract of root significantly prevented the physical, biochemical, histological, and functional changes induced by paracetamol in the liver. The extract showed significant hepatoprotective effects as evidenced by decreased serum enzyme activities like SGPT, SGOT, ALP, and TB, which was supported by histopathological studies of liver. The aqueous extract showed significant hepatoprotective activity comparable with standard drug silymarin as well as hepatotoxin drug PCM. CONCLUSION: From these results, it is concluded that the A. tricolor has potential effectiveness in treating liver damage in a dose dependent manner.

11.
J Adv Pharm Technol Res ; 3(2): 82, 2012 Apr.
Article in English | MEDLINE | ID: mdl-22837954
12.
Anticancer Drugs ; 23(8): 836-45, 2012 Sep.
Article in English | MEDLINE | ID: mdl-22407250

ABSTRACT

We have synthesized and characterized doxorubicin (DOX)-loaded galactosylated gelatin nanovectors using in vitro and in vivo for targeting liver cells including hepatocarcinoma cells. Galactosylated and nongalactosylated gelatin nanovectors (GL-GN-DOX and GN-DOX) were spherical in shape and had mean sizes of about 95.1 and 88.3 nm, respectively. In-vitro release of DOX from nanovectors followed first-order kinetics and was pH dependent. Galactosylated formulation released 95.2% of DOX compared with 86.6% by nongalactosylated formulation at pH 5.8. However, the release rate was suppressed at pH 7.4. Further, we showed that GL-GN-DOX had greater growth inhibitory effect on HepG2 in terms of low inhibitory concentration (IC(50); 0.35 µg/ml) compared with GN-DOX (0.75 µg/ml) and induced caspase-3-mediated apoptosis in HepG2 cells. This might be due to efficient internalization of galactosylated nanovectors by HepG2 cells compared with unmodified formulation. Pharmacokinetic and biodistribution analyses show that galactosylated formulation deposits 24.5 µg/g of DOX in targeted tissue (liver) in comparison with heart (0.3 µg/g) at a single dose of 10 mg/kg. These results suggest that DOX-loaded galactosylated gelatin nanovectors warrant future in-depth antitumor study to scale-up technology and may be used for the management of hepatocarcinoma.


Subject(s)
Antibiotics, Antineoplastic/pharmacology , Carcinoma, Hepatocellular/drug therapy , Doxorubicin/pharmacology , Liver Neoplasms/drug therapy , Animals , Antibiotics, Antineoplastic/administration & dosage , Antibiotics, Antineoplastic/pharmacokinetics , Apoptosis/drug effects , Carcinoma, Hepatocellular/pathology , Caspase 3/metabolism , Cell Proliferation/drug effects , Doxorubicin/administration & dosage , Doxorubicin/pharmacokinetics , Drug Delivery Systems , Galactose/chemistry , Gelatin/chemistry , Hep G2 Cells , Humans , Hydrogen-Ion Concentration , Inhibitory Concentration 50 , Liver Neoplasms/pathology , Male , Mice , Nanospheres , Particle Size , Tissue Distribution
13.
Braz. j. microbiol ; 42(4): 1569-1573, Oct.-Dec. 2011. graf, tab
Article in English | LILACS | ID: lil-614623

ABSTRACT

Murraya koenigii, family Rutaceae, commonly known as Curry leaf plant is a highly valued plant for its medicinal value and characteristic aroma. The plant is a rich source of carbazole alkaloids. The petroleum ether, chloroform, ethyl acetate and ethanol extracts of roots of the plant were screened for phytochemical properties and antimicrobial activity for Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. Phytochemical screening showed the presence of carbohydrates, alkaloids, steroids and flavonoids in the root extracts of the plant. The study shows that all the extracts possess remarkable antibacterial activity. Additionally, petroleum ether and chloroform extracts also had antifungal activity.


Subject(s)
Alkaloids/analysis , Chloroform/analysis , Murraya/microbiology , Plants, Medicinal , Rutaceae , Methods , Methods
14.
Anticancer Drugs ; 22(8): 774-82, 2011 Sep.
Article in English | MEDLINE | ID: mdl-21799471

ABSTRACT

Topical 5-fluorouracil (5-FU) is used for the treatment of actinic keratosis and nonmelanoma skin cancer. Unfortunately, 5-FU per se shows a poor percutaneous permeation, thus reducing its anticancer effectiveness after topical administration. Therefore, we have constructed transfersomes, liposomes, and niosomes of 5-FU for topical applications in this investigation. Transfersomes were prepared by the solvent evaporation method, whereas liposomes and niosomes were constructed by reverse-phase evaporation method. The nanovesicles were characterized for particle size, shape, zeta potential, viscosity, entrapment efficiency, deformability, in-vitro permeation release, and kinetics and retention. Cytotoxicity study was carried out on HaCaT cells. Transfersomes (153.2 ± 10.3 nm), liposomes (120.3 ± 9.8 nm), and niosomes (250.4 ± 8.6 nm) were produced with a maximum entrapment efficiency of 82.4 ± 4.8, 45.4 ± 3.3, and 43.4 ± 3.2%, respectively. Moreover, transmission electron microscopy and atomic force microscopy assure the smooth and spherical shape of nanovesicles. Skin permeation and retention showed better permeability and retention than the nonvesiculized dosage form. The IC50 value of transfersomes (1.02 µmol/l), liposomes (6.83 µmol/l), and niosomes (9.91 µmol/l) was found to be far less than 5-FU (15.89 µmol/l) at 72 h. 5-FU-loaded transfersomes were found to be most cytotoxic on the HaCaT cell line in comparison with liposomes and niosomes. We concluded that vesiculization of 5-FU not only improves the topical delivery, but also enhances the cytotoxic effect of 5-FU. We have presented here a viable formulation of 5-FU for the management of actinic keratosis and nonmelanoma skin carcinoma.


Subject(s)
Antimetabolites, Antineoplastic/administration & dosage , Drug Delivery Systems , Fluorouracil/administration & dosage , Skin Neoplasms/drug therapy , Administration, Cutaneous , Animals , Antimetabolites, Antineoplastic/pharmacokinetics , Antimetabolites, Antineoplastic/pharmacology , Cell Line, Tumor , Fluorouracil/pharmacokinetics , Fluorouracil/pharmacology , Humans , Liposomes , Male , Particle Size , Permeability , Rats , Skin Absorption , Skin Neoplasms/pathology , Viscosity
15.
Anticancer Drugs ; 22(6): 543-55, 2011 Jul.
Article in English | MEDLINE | ID: mdl-21471809

ABSTRACT

Noscapine, the tubulin-binding anticancer agent, when administered orally, requires high ED(50) (300-600 mg/kg), whereas intravenous administration (10 mg/kg) results in rapid elimination of the drug with a half-life of 0.39 h. Hence, the development of long-circulating injectable nanoparticles can be an interesting option for designing a viable formulation of noscapine for anticancer activity. Noscapine-enveloped gelatin nanoparticles and poly(ethylene glycol)-grafted gelatin nanoparticles were constructed and characterized. Data indicate that smooth and spherical shaped nanoparticles of 127 ± 15 nm were engineered with maximum entrapment efficiency of 65.32 ± 3.81%. Circular dichroism confirms that nanocoacervates retained the α-helical content of gelatin in ethanol whereas acetone favored the formation of a random coil. Moreover, the Fourier transform infrared and powder X-ray diffraction pattern prevents any significant change in the noscapine-loaded gelatin nanoparticles in comparison with individual components. In-vitro release kinetic data suggest a first-order release of noscapine (85.1%) from gelatin nanoparticles with a release rate constant of 7.611×10(-3). It is to be noted that there is a 1.43-fold increase in the area under the curve up to the last sampling point for the noscapine-loaded poly(ethylene glycol)-grafted gelatin nanoparticles over the noscapine-loaded gelatin nanoparticles and a 13.09-fold increase over noscapine. Cytotoxicity analysis of the MCF-7 cell line indicated that the IC(50) value of the noscapine-loaded poly(ethylene glycol)-grafted gelatin nanoparticles was equivalent to 20.8 µmol/l, which was significantly (P<0.05) lower than the IC(50) value of the noscapine-loaded gelatin nanoparticles (26.3 µmol/l) and noscapine (40.5 µmol/l).Noscapine-loaded poly(ethylene glycol)-grafted gelatin nanoparticles can be developed as a promising therapeutic agent for the management of breast cancer.


Subject(s)
Angiogenesis Inhibitors/administration & dosage , Nanoparticles , Noscapine/administration & dosage , Amines/chemistry , Angiogenesis Inhibitors/pharmacokinetics , Angiogenesis Inhibitors/pharmacology , Animals , Area Under Curve , Cell Line, Tumor , Circular Dichroism , Drug Compounding , Drug Delivery Systems/methods , Drug Stability , Electrochemistry , Excipients , Female , Gelatin , Humans , Mice , Microscopy, Atomic Force , Microscopy, Electron , Microscopy, Electron, Transmission , Nanoparticles/chemistry , Noscapine/pharmacokinetics , Noscapine/pharmacology , Particle Size , Polyethylene Glycols , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared , X-Ray Diffraction
16.
Braz J Microbiol ; 42(4): 1569-73, 2011 Oct.
Article in English | MEDLINE | ID: mdl-24031791

ABSTRACT

Murraya koenigii, family Rutaceae, commonly known as Curry leaf plant is a highly valued plant for its medicinal value and characteristic aroma. The plant is a rich source of carbazole alkaloids. The petroleum ether, chloroform, ethyl acetate and ethanol extracts of roots of the plant were screened for phytochemical properties and antimicrobial activity for Staphylococcus aureus, Micrococcus luteus, Bacillus subtilis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. Phytochemical screening showed the presence of carbohydrates, alkaloids, steroids and flavonoids in the root extracts of the plant. The study shows that all the extracts possess remarkable antibacterial activity. Additionally, petroleum ether and chloroform extracts also had antifungal activity.

17.
Cancer Chemother Pharmacol ; 65(3): 537-48, 2010 Feb.
Article in English | MEDLINE | ID: mdl-19597818

ABSTRACT

PURPOSE: Noscapine (NOS) is a unique class of tubulin-binding anticancer agents. Their potential usefulness as anticancer drugs is however limited by the poor bioavailability, thus necessitating administration of a higher dose regime in the range of 300-600 mg/kg for tumor growth inhibition. To augment bioavailability, we prepared an inclusion complex of NOS in beta-cyclodextrin (beta-CD) and evaluated its physico-chemical characteristics. METHOD AND RESULTS: Our phase-solubility analysis shows a 1:1-complexation (Kc approximately 0.454 mM(-1)) of NOS with beta-CD that offers better dissolution properties. We confirmed complex formation in solid state by differential scanning calorimetry, powder X-ray diffractometry, Fourier-transform infrared spectroscopy, 1H nuclear magnetic resonance spectroscopy, rotating frame Overhauser enhancement spectroscopy and by molecular modeling methods. Based upon theoretical calculations in gas phase, we propose O-CH2-O- in orientation of NOS in the beta-CD cavity. The thermal behavior data also provides complementary evidences of complex formation. The pharmacokinetic studies showed a 1.87-fold increase in bioavailability of NOS upon complexation in the beta-CD inclusion complex state as compared to free NOS. Furthermore, the complex retains the anticancer attributes of NOS. CONCLUSION: Our studies propose for the first time a stable NOS-beta-CD inclusion complex as an effective approach to enhance the solubility and bioavailability of NOS for anticancer therapy.


Subject(s)
Noscapine/chemistry , Noscapine/pharmacokinetics , beta-Cyclodextrins/chemistry , Administration, Oral , Animals , Area Under Curve , Biological Availability , Calorimetry, Differential Scanning , Cell Line, Tumor , Chromatography, High Pressure Liquid , Drug Compounding , Drug Stability , Humans , Magnetic Resonance Spectroscopy , Male , Metabolic Clearance Rate , Mice , Models, Molecular , Molecular Structure , Noscapine/administration & dosage , Solubility , Spectroscopy, Fourier Transform Infrared , Temperature , X-Ray Diffraction
18.
Yao Xue Xue Bao ; 44(11): 1278-84, 2009 Nov.
Article in English | MEDLINE | ID: mdl-21351727

ABSTRACT

The present investigation is aimed to develop a new formulation containing chemically crosslinked guar gum microspheres loaded with 5-fluorouracil for targeting colorectal cancer. The emulsification polymerization method involving the dispersion of aqueous phase of guar gum in castor oil was used to prepare spherical microspheres. Various processing parameters were studied in order to optimize the formulation. Particle size and surface morphology of the microspheres were determined using optical microscopy and scanning electron microscopy. The in vitro drug release studies performed in simulated gastric fluid (SGF) for 2 h followed by intestinal fluid for 3 h, revealed the retention of the drug inside the microspheres from which only (15.27 +/- 0.56) % of the drug was released in 5 h. In vitro release rate studies were also carried out in simulated colonic fluid (SCF) in the presence of rat caecal contents, which showed improved drug release. The drug release from the formulation was found to be (41.6 +/- 3.5) % with 2% (w/v) caecal matter in 24 h as compared to control study where (25.2 +/- 3.5) % of drug was released. The drug release from the formulation with 2% and 4% rat caecal contents medium after 2 days of enzyme induction was found to be (56.3 +/- 4.1) % and (78.9 +/- 2.8) % in 24 h respectively. Similarly, (61.3 +/- 5.4) % and (90.2 +/- 2.9) % drug was released respectively with 2% and 4% rat caecal matter after 4 days of enzyme induction and (72.1 +/- 2.9) % and (90.2 +/- 3.2) % after 6 days of enzyme induction. In this way, 5-fluorouracil loaded guar gum microspheres have shown promising results in the management of colorectal cancer, warranting thorough in vivo study for scale up technology.


Subject(s)
Antimetabolites, Antineoplastic/administration & dosage , Colon/metabolism , Drug Delivery Systems , Fluorouracil/administration & dosage , Galactans/chemistry , Mannans/chemistry , Plant Gums/chemistry , Animals , Antimetabolites, Antineoplastic/pharmacokinetics , Cecum/metabolism , Drug Carriers , Drug Compounding , Fluorouracil/pharmacokinetics , Microspheres , Particle Size , Rats
19.
Acta Pharm ; 58(4): 479-87, 2008 Dec.
Article in English | MEDLINE | ID: mdl-19103581

ABSTRACT

Immune suppression resulting from chemoprophylaxis and potential drug interaction were investigated in experimental animals pre-medicated with ampicillin and chloroquine followed by immunization with bovine serum albumin bearing liposomes prepared by the reverse phase evaporation method. The prepared liposomes were evaluated for particle size, entrapment efficiency and in vitro release. Humoral immune response was measured in terms of systemic IgG antibody titre by the ELISA method. The present study showed that 7:3 molar ratio of soya phosphatidylcholine and cholesterol produced liposomes of mean diameter of 235.4 +/- 10.3 nm and entrapment efficiency of 41.3 +/- 3.2%. Ampicillin significantly (p < 0.05) decreased the antibody titre whereas chloroquine did not reduce the antibody titre significantly. The study will help in programming a new drug management and in characterization of vaccine-drug interaction.


Subject(s)
Ampicillin/pharmacology , Antibody Formation/drug effects , Chloroquine/pharmacology , Serum Albumin, Bovine/immunology , Animals , Immunoglobulin G/blood , Liposomes , Male , Rats , Rats, Wistar , Serum Albumin, Bovine/administration & dosage
20.
Yao Xue Xue Bao ; 42(8): 905-10, 2007 Aug.
Article in English | MEDLINE | ID: mdl-17944244

ABSTRACT

The aim is to evaluate the effect of ciprofloxacin and chloramphenicol on anti-BSA antibody production triggered by bovine albumin encapsulated in non-ionic surfactant vesicle, niosomes. Reverse phase evaporation method was adopted to entrap the antigen in colloidal carrier composed of Span 80 and Span 85 followed by simultaneous characterization for particle size, entrapment efficiency and in vitro release. The protein content was determined by Bradford method using UV Visible Spectrophotometer at 595 nm. Humoral immune response was measured in terms of systemic IgG antibody titre by ELISA method. Experimental data indicated that 7 : 3 molar ratio of Span 80 and cholesterol based niosomal formulation possessed maximum (39.8 +/- 2.9)% of soluble protein. Ciprofloxacin markedly (P < 0.05) decreased the antibody titre. In contrast, chloramphenicol did not reduce the antibody titre significantly in comparison to control group (P > 0.05). It is necessary to explore the effect of a vaccine antigen when a candidate is medicated with a therapeutic agent, which might help in programming a new drug management and vaccination programme.


Subject(s)
Antibody Formation/drug effects , Chloramphenicol , Ciprofloxacin , Drug Carriers , Immunoglobulin G/blood , Animals , Chloramphenicol/administration & dosage , Chloramphenicol/pharmacology , Ciprofloxacin/administration & dosage , Ciprofloxacin/pharmacology , Hexoses , Liposomes , Male , Particle Size , Rats , Rats, Wistar , Serum Albumin, Bovine
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