... Swarna latha Dugasani a , Madhu Katyayani Balijepalli b and Mallikarjuna Rao, Pichika. International MedicalUniversity,Bukit Jalil,Kuala Lumpur,Malaysia. ... Phytochemistry, 30: 541-543. Apparao, M., Kjer, A., Olsen, O., Venkata Rao,...
more... Swarna latha Dugasani a , Madhu Katyayani Balijepalli b and Mallikarjuna Rao, Pichika. International MedicalUniversity,Bukit Jalil,Kuala Lumpur,Malaysia. ... Phytochemistry, 30: 541-543. Apparao, M., Kjer, A., Olsen, O., Venkata Rao, E., Rasmussen, KW and Sorensen, H. (1981). ...
Novel 3D-biomaterial is constructed having a combination of a new quaternary ammonium silane (k21) antimicrobial impregnated in three-dimensional 3D collagen printed scaffolds cross linked with Riboflavin in presence of d-alpha-tocopheryl...
moreNovel 3D-biomaterial is constructed having a combination of a new quaternary ammonium silane (k21) antimicrobial impregnated in three-dimensional 3D collagen printed scaffolds cross linked with Riboflavin in presence of d-alpha-tocopheryl poly(ethyleneglycol)-1000-succinate as a potential scaffold. Groups of "0.1% and 0.2% k21", and "0.1% and 0.2% Chlorhexidine (CHX)" were prepared. k21/CHX with neutralized collagen was printed with BioXTM . Riboflavin was photo-activated and examined using epifluorescence for Aggregatibacter actinomycetemcomitans (7-days). Collagen was examined using TEM and measured for porosity, and shape-fitting. Raman and Tandem Mass/solid-state were performed with molecular-docking and circular dichroism. X-ray diffractions were conducted with rheological tests, contact angle and ninhydrin assay. k21 samples demonstrated collagen aggregates while 0.1%CHX and 0.2%CHX showed irregularities. Porosity of control and "0.1% and 0.2% k21" scaffolds showed no differences. Low contact angle, improved elastic-modulus, rigidity, and smaller strain in k21 groups were seen. Bacteria were reduced and strong organic intensities seen in k21 scaffolds. Simulation showed hydrophobicity and electrostatic interaction. Crosslinking was observed in 0.2%CHX/79% ± 9.9 and 0.2%k21/80% ± 12.3. Circular dichroism for k21 were suggestive of triple helix. XRD patterns appeared at d = 5.97, 3.03, 2.78, 2.1 and 2.90 Ao . 3D-printing of collagen impregnated with quaternary ammonium silane produced a promising scaffold with antimicrobial potency and structural stability. This article is protected by copyright. All rights reserved.
: With multi-drug-resistant tumours continuously evolving, developing new drugs with enhanced efficacy is essential. This study aims to synthesise flavonoid Mannich bases and evaluate their cytotoxic activity. The flavonoids isolated from...
more: With multi-drug-resistant tumours continuously evolving, developing new drugs with enhanced efficacy is essential. This study aims to synthesise flavonoid Mannich bases and evaluate their cytotoxic activity. The flavonoids isolated from the leaves of Muntingia calabura were used as reactants for the synthesis. Twenty flavonoid Mannich bases were synthesised via the Mannich reaction. Cytotoxic activity of the parent compounds and synthesised compounds were evaluated against two breast cancer cell lines, i.e., MCF-7, MDA-MB-231, and one normal breast cell line, MCF-10A, via MTT assay. Cytotoxic activity against the MDA-MB-231 cancer cell line showed that flavonoid Mannich bases exhibited greater activity than their parent compounds. 5,7-dihydroxy-8-(4-methoxybenzylamine)-2-phenyl-4H-chromen-4-one (4f) showed the highest cytotoxic activity against MDA-MB-231 cell with IC50 of 5.75±0.82 µM. For the MCF-7 cell line, the parent compounds and Mannich bases showed moderate activity with the IC50 range of 9.17-68.5 µM. For cytotoxic activity against the MCF-10A cell line, the parent compound, 5,7-dihydroxyflavone (4), showed the highest toxicity against MCF-10A with IC50 of 10.55±1.05 µM. The results suggest synthetic modifications have produced compounds with improved anticancer activity and selectivity against breast cancer cells.
To formulate a dental bleaching agent with strawberry extract that has potent bleaching properties and antimicrobial efficacy. Enamel specimens (3 × 3 × 2 mm3) were prepared. Quaternary Ammonium Silane (CaC2 enriched) was homogenized with...
moreTo formulate a dental bleaching agent with strawberry extract that has potent bleaching properties and antimicrobial efficacy. Enamel specimens (3 × 3 × 2 mm3) were prepared. Quaternary Ammonium Silane (CaC2 enriched) was homogenized with fresh strawberries: Group 1: supernatant strawberry (10 g) extract < Group 2: supernatant strawberry (10 g) extract + 15%HA (Hydroxyapatite) < Group 3: supernatant strawberry (10 g) extract + 15% (HA-2%k21) < Group 4: supernatant strawberry (20 g) extract only (20 g strawberries) < Group 5: supernatant strawberry (20 g) extract + 15% HA < Group 6: supernatant strawberry (20 g) extract + 15% (HA-2%K21) < Group 7: In-office Opalescence Boost 35%. Single-colony lactobacillus was examined using confocal microscopy identifying bacterial growth and inhibition in presence of bleaching agents using 300 µL aliquot of each bacterial culture. Images were analysed by illuminating with a 488 nm argon/helium laser beam. Colour difference (∆E00)...
Auranamide and patriscabratine are amides from Melastoma malabathricum (L.) Smith. Their anti-inflammatory activity and nuclear factor erythroid 2-related factor 2 (NRF2) activation ability were evaluated using Escherichia coli...
moreAuranamide and patriscabratine are amides from Melastoma malabathricum (L.) Smith. Their anti-inflammatory activity and nuclear factor erythroid 2-related factor 2 (NRF2) activation ability were evaluated using Escherichia coli lipopolysaccharide (LPSEc)-stimulated murine macrophages (RAW264.7) and murine hepatoma (Hepa-1c1c7) cells, respectively. The cytotoxicity of the compounds was assessed using a 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay. The anti-inflammatory activity was determined by measuring the nitric oxide (NO) production and pro-inflammatory cytokines (Interleukin (IL)-1β, Interferon (IFN)-γ, tumour necrosis factor (TNF)-α, and IL-6) and mediators (NF-κB and COX-2). NRF2 activation was determined by measuring the nicotinamide adenine dinucleotide phosphate hydrogen (NADPH) quinone oxidoreductase 1 (NQO1), nuclear NRF2 and hemeoxygenase (HO)-1. In vitro metabolic stability was assessed using the mouse, rat, and human liver microsomes. The ...
Zingiber officinale var. rubrum is known as ‘Halia bara’ in the Southeast Asia region. Many herbal products containing Halia bara are in the market are being used for either cosmetic purposes or well-being. The present study aims to...
moreZingiber officinale var. rubrum is known as ‘Halia bara’ in the Southeast Asia region. Many herbal products containing Halia bara are in the market are being used for either cosmetic purposes or well-being. The present study aims to develop a simple, high-performance liquid chromatography (HPLC) method using a diode array detector for the quantification of predominant gingerols (4-, 6-, 8-, and 10-) and shogaols (6-, 8-, and 10-) in supercritical carbon dioxide extract of Halia bara. The optimum conditions for elution of seven compounds were: column, ODS Genesis; column temperature, 25 C; elution, gradient elution consisting of acetonitrile and aqueous formic acid; detection wavelength, 282 nm; flow rate, 1 mL/min; injection volume, 20 µL; and run-time, 38 min. The optimized HPLC method was validated for linear range, accuracy, precision (repeatability and reproducibility), sensibility (limit of detection and quantification) and recovery. All the validation parameters were within t...
Objective: To develop a simple and rapid isocratic reversed-phase high-performance liquid chromatography (RP-HPLC) method and validate as per ICH and USP guidelines for analysis of tiagabine in the presence of its degradation products....
moreObjective: To develop a simple and rapid isocratic reversed-phase high-performance liquid chromatography (RP-HPLC) method and validate as per ICH and USP guidelines for analysis of tiagabine in the presence of its degradation products. Methods: The chromatographic separation was achieved on a Vision HT C 18 column (150 mm × 4.6 mm, 5 µm) with mobile phase comprising of 11.5 mM of sodium dihydrogen phosphate (adjusted to pH 2.0 with orthophosphoric acid):acetonitrile (50:50,v/v) at a flow rate of 1.0 ml/min and the UV detection wavelength set at 254 nm. Stress degradation studies were performed as stated in ICH guidelines on tiagabine bulk drug using acid, base, oxidation, heat and light. Results: Tiagabine was found to degrade under acidic, photolytic, oxidative and thermal conditions, but stable under basic hydrolysis condition. The developed method was found to be linear in the concentration range of 50-150 µg/ml (r 2 = 0.9983) and the percentage recovery for the accuracy was 98.86%-99.35%. The LOD and LOQ obtained were 31.93 µg/ml and 96.76 µg/ml, respectively while the %RSD for precision, robustness, and stability studies were less than 2%. The degradation products formed from the stress study were well separated from tiagabine and hence the method could be regarded as stability indicating. Conclusion: A simple and rapid RP-HPLC method was developed and validated for analysis of tiagabine in the presence of its degradation products and thus, the proposed method can be used in the analysis of tiagabine bulk drug and pharmaceutical formulation in quality control laboratories. Normal 0 false false false EN-US X-NONE X-NONE /* Style Definitions */ table.MsoNormalTable {mso-style-name:"Table Normal"; mso-tstyle-rowband-size:0; mso-tstyle-colband-size:0; mso-style-noshow:yes; mso-style-priority:99; mso-style-parent:""; mso-padding-alt:0in 5.4pt 0in 5.4pt; mso-para-margin-top:0in; mso-para-margin-right:0in; mso-para-margin-bottom:8.0pt; mso-para-margin-left:0in; line-height:107%; mso-pagination:widow-orphan; font-size:11.0pt; font-family:"Calibri","sans-serif"; mso-ascii-font-family:Calibri; mso-ascii-theme-font:minor-latin; mso-hansi-font-family:Calibri; mso-hansi-theme-font:minor-latin;}
6-shogaol is a natural and the most potent bioactive vanilloid in dried Zingiber officinale rhizomes. Many scientific studies have reported the diverse biological activities of 6-shogaol. However, the major drawback of 6-shogaol is its...
more6-shogaol is a natural and the most potent bioactive vanilloid in dried Zingiber officinale rhizomes. Many scientific studies have reported the diverse biological activities of 6-shogaol. However, the major drawback of 6-shogaol is its instability at room temperature. We synthesised new shogaol thiophene compounds (STCs) by replacing the pentyl group in the sidechain with thiophene derivatives. The STCs were tested for their nuclear factor erythroid 2-related factor 2 (NRF2) activation ability in murine hepatoma cells (Hepa1c1c-7) by determining their NAD(P)H quinone oxidoreductase 1 (NQO1) inducing ability and expression of NRF2-associated antioxidant genes. The anti-inflammatory activity of STCs was determined in Escherichia coli lipopolysaccharide (LPSEc)-stimulated NR2-proficient and -silenced mouse microglial cells (BV-2) by measuring the inflammatory markers, cytokines, and mediators. The modes of action (interacting with the Kelch domain of KEAP1, covalent bonding with cystei...
Our previous studies have reported the effect of swietenine (a major bioactive component of Swietenia macrophylla seeds) in reversing and potentiating the effect of metformin in hyperglycemia and hyperlipidaemia in diabetic rats....
moreOur previous studies have reported the effect of swietenine (a major bioactive component of Swietenia macrophylla seeds) in reversing and potentiating the effect of metformin in hyperglycemia and hyperlipidaemia in diabetic rats. Moreover, we reported that the anti-inflammatory effect of swietenine is mediated via the activation of nuclear factor erythroid 2-related factor 2 (Nrf2). This study evaluated the effect of swietenine and its mechanisms in nonalcoholic fatty liver disease (NAFLD) in high-fat diet/streptozotocin-induced diabetic mice. The effect was assessed by determining blood biochemical parameters (glucose, cholesterol, triglycerides, alanine transaminase (ALT), asparate transaminase (AST), alkaline phosphatase (ALP), glutathione (GSH), total antioxidant capacity (TAC), and malondialdehyde (MDA)) and liver biochemical parameters (liver index, cholesterol, and triglycerides). Hepatic lipid accumulation (initial causative factor in NAFLD) was determined by oil-O-red stain...
The antidiabetic effects of quercetin and metformin are well known. However, their synergistic effect in reversing the symptoms of diabetes-induced endothelial dysfunction remains unknown. In this study, we have investigated their...
moreThe antidiabetic effects of quercetin and metformin are well known. However, their synergistic effect in reversing the symptoms of diabetes-induced endothelial dysfunction remains unknown. In this study, we have investigated their synergistic effect in streptozotocin (STZ)-nicotinamide induced diabetic rats. Seventy-five rats were divided into five groups; normal control, diabetic control, treatment groups (10 mg/kg quercetin, 180 mg/kg metformin, and combined). The plasma glucose and lipid levels, liver enzymes, ex-vivo studies on aortic rings, histology of liver, kidney, pancreas, abdominal aorta and thoracic aorta, and immunohistochemical studies were carried out. The findings revealed that the combination of quercetin and metformin showed a greater antidiabetic effect than either drug, and rendered protection to the endothelium. The combination effectively reversed the hyperglycemia-induced endothelial dysfunction in diabetic rats. Furthermore, it also reversed the dysregulated ...
Staphylococcus aureus is a highly adaptive human pathogen responsible for serious hospital- and community-acquired infectious diseases, ranging from skin and soft tissue infections, to complicated and life-threatening conditions such as...
moreStaphylococcus aureus is a highly adaptive human pathogen responsible for serious hospital- and community-acquired infectious diseases, ranging from skin and soft tissue infections, to complicated and life-threatening conditions such as endocarditis and toxic shock syndrome (TSS). The rapid development of resistance of this organism to available antibiotics over the last few decades has necessitated a constant search for more efficacious antibacterial agents. Eugenol (4-allyl-2-methoxyphenol) belongs to the class of chemical compounds called phenylpropanoids. It is a pure-to-pale yellow, oily liquid substance, mostly extracted as an essential oil from natural products such as clove, cinnamon, nutmeg, basil, and bay leaf. Eugenol has previously been shown to have antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA). However, the mechanism of action of eugenol against MRSA has not, as yet, been elucidated; hence, the necessity of this study. Global gene ex...
Due to the specific physiological pH throughout the human body, pH-responsive polymers have been considered for aiding drug delivery systems. Depending on the surrounding pH conditions, the polymers can undergo swelling or contraction...
moreDue to the specific physiological pH throughout the human body, pH-responsive polymers have been considered for aiding drug delivery systems. Depending on the surrounding pH conditions, the polymers can undergo swelling or contraction behaviors, and a degradation mechanism can release incorporated substances. Additionally, polyurethane, a highly versatile polymer, has been reported for its biocompatibility properties, in which it demonstrates good biological response and sustainability in biomedical applications. In this review, we focus on summarizing the applications of pH-responsive polyurethane in the biomedical and drug delivery fields in recent years. In recent studies, there have been great developments in pH-responsive polyurethanes used as controlled drug delivery systems for oral administration, intravaginal administration, and targeted drug delivery systems for chemotherapy treatment. Other applications such as surface biomaterials, sensors, and optical imaging probes are...
Precise functioning and fine-tuning of Toll-like receptor 4 (TLR4) signaling is a critical requirement for the smooth functioning of the innate immune system, since aberrant TLR4 activation causes excessive production of pro-inflammatory...
morePrecise functioning and fine-tuning of Toll-like receptor 4 (TLR4) signaling is a critical requirement for the smooth functioning of the innate immune system, since aberrant TLR4 activation causes excessive production of pro-inflammatory cytokines and interferons. This can result in life threatening conditions such as septic shock and other inflammatory disorders. The TRIF-related adaptor molecule (TRAM) adaptor protein is unique to the TLR4 signaling pathway and abrogation of TRAM-mediated TLR4 signaling is a promising strategy for developing therapeutics aimed at disrupting TRAM interactions with other components of the TLR4 signaling complex. The VIPER motif from the vaccinia virus-producing protein, A46 has been reported to disrupt TRAM-TLR4 interactions. We have exploited this information, in combination with homology modeling and docking approaches, to identify a potential binding site on TRAM lined by the BB loop and αC helix. Virtual screening of commercially available small molecules targeting the binding site enabled to short-list 12 small molecules to abrogate TRAM-mediated TLR4 signaling. Molecular dynamics and molecular mechanics calculations have been performed for the analysis of these receptor-ligand interactions.
The objective of this review is to systematically appraise the literature available to date on biological activities ( in vitro and in vivo ) of extracts and constituents from Cinnamomum . An extensive review of the literature available...
moreThe objective of this review is to systematically appraise the literature available to date on biological activities ( in vitro and in vivo ) of extracts and constituents from Cinnamomum . An extensive review of the literature available in various recognised databases including PubMed, Google Scholar and Scopus on the biological activities of various species of the Cinnamomum were undertaken. The literature provided information on biological activities of the species of the genus Cinnamomum . Crude extracts and constituents from about 30 species of Cinnamomum displayed significant antibacterial, antifungal, antiseptic, antiviral, anti-inflammatory, antipyretic, antioxidant, chemopreventive, cytotoxic, antidiabetic, hypolipidemic, antispasmodic, antiulcer, antiplatelet, anodyne, choleretic, immunostimulant, anaesthetic and sedative activities. Essential oil, aqueous/alcoholic extracts, cinnamaldehyde and proanthocyanidins were reported to be mainly responsible for biological activiti...
INTRODUCTION The use of Artificial intelligence (AI) in drug discovery and development (DDD) has gained more traction in the past few years. Many scientific reviews have already been made available in this area. Thus, in this review, the...
moreINTRODUCTION The use of Artificial intelligence (AI) in drug discovery and development (DDD) has gained more traction in the past few years. Many scientific reviews have already been made available in this area. Thus, in this review, the authors have focused on the success stories of AI-driven drug candidates and scientometric analysis of the literature in this field. AREA COVERED The authors explore the literature to compile the success stories of AI-driven drug candidates that are currently being assessed in clinical trials or which have investigational new drug (IND) status. The authors also provide the reader with their expert perspectives for the future developments and their opinions on the field. EXPERT OPINION The partnerships between AI companies and the pharma industry are booming. The early signs of the impact of AI in DDD is encouraging and the pharma industry is hoping for breakthroughs. AI can be a promising technology to unveil the greatest successes, but it has yet to be proven as AI is still at the embryonic stage.
The transcription factor Nuclear factor erythroid-2-related factor 2 (NRF2) and its principal repressive regulator, the E3 ligase adaptor Kelch-like ECH-associated protein 1 (KEAP1), are critical in the regulation of inflammation, as well...
moreThe transcription factor Nuclear factor erythroid-2-related factor 2 (NRF2) and its principal repressive regulator, the E3 ligase adaptor Kelch-like ECH-associated protein 1 (KEAP1), are critical in the regulation of inflammation, as well as maintenance of homeostasis. Thus, NRF2 activation provides cytoprotection against numerous inflammatory disorders. N-nicotinoylquinoxaline-2-carbohdyrazide (NQC) was designed by combining the important pharmacophoric features of bioactive compounds reported in the literature. NQC was synthesised and characterised using spectroscopic techniques. The compound was tested for its anti-inflammatory effect using LPSEc induced inflammation in mouse macrophages (RAW 264.7 cells). The effect of NQC on inflammatory cytokines was measured using ELISA. The Nrf2 activity of the compound NQC was determined using ‘Keap1:Nrf2 Inhibitor Screening Assay Kit’. To obtain the insights on NQC’s activity on Nrf2, molecular docking studies were performed using Schrodin...
Zingiber officinale var. rubrum (red ginger) is widely used in traditional medicine in Asia. Unlike other gingers, it is not used as a spice in cuisines. To date, a total of 169 chemical constituents have been reported from red ginger....
moreZingiber officinale var. rubrum (red ginger) is widely used in traditional medicine in Asia. Unlike other gingers, it is not used as a spice in cuisines. To date, a total of 169 chemical constituents have been reported from red ginger. The constituents include vanilloids, monoterpenes, sesquiterpenes, diterpenes, flavonoids, amino acids, etc. Red ginger has many therapeutic roles in various diseases, including inflammatory diseases, vomiting, rubella, atherosclerosis, tuberculosis, growth disorders, and cancer. Scientific evidence suggests that red ginger exhibits immunomodulatory, antihypertensive, antihyperlipidemic, antihyperuricemic, antimicrobial, and cytotoxic activities. These biological activities are the underlying causes of red ginger’s therapeutic benefits. In addition, there have been few reports on adverse side effects of red ginger. This review aims to provide insights in terms the bioactive constituents and their biosynthesis, biological activities, molecular mechanis...
Silane-based/fully hydrolyzed, endodontic irrigant exhibiting antimicrobial properties, is prepared, and is hypothesized to control macrophage polarization for tissue repair. Albino wistar rats were injected with 0.1 ml root canal...
moreSilane-based/fully hydrolyzed, endodontic irrigant exhibiting antimicrobial properties, is prepared, and is hypothesized to control macrophage polarization for tissue repair. Albino wistar rats were injected with 0.1 ml root canal irrigant, and bone marrow cells procured. Cellular mitochondria were stained with MitoTracker green along with Transmission Electron Microscopy (TEM) performed for macrophage extracellular vesicle. Bone marrow stromal cells (BMSCs) were induced for M1 and M2 polarization and Raman spectroscopy with scratch assay performed. Cell counting was used to measure cytotoxicity, and fluorescence microscopy performed for CD163. Scanning Electron Microscopy (SEM) was used to investigate interaction of irrigants with Enterococcus faecalis. K21 specimens exhibited reduction in epithelium thickness and more mitochondrial mass. EVs showed differences between all groups with decrease and increase in IL-6 and IL-10 respectively. 0.5%k21 enhanced wound healing with more fib...
Precise functioning and fine-tuning of Toll-like receptor 4 (TLR4) signaling is a critical requirement for the smooth functioning of the innate immune system, since aberrant TLR4 activation causes excessive production of pro-inflammatory...
morePrecise functioning and fine-tuning of Toll-like receptor 4 (TLR4) signaling is a critical requirement for the smooth functioning of the innate immune system, since aberrant TLR4 activation causes excessive production of pro-inflammatory cytokines and interferons. This can result in life threatening conditions such as septic shock and other inflammatory disorders. The TRIF-related adaptor molecule (TRAM) adaptor protein is unique to the TLR4 signaling pathway and abrogation of TRAM-mediated TLR4 signaling is a promising strategy for developing therapeutics aimed at disrupting TRAM interactions with other components of the TLR4 signaling complex. The VIPER motif from the vaccinia virus-producing protein, A46 has been reported to disrupt TRAM-TLR4 interactions. We have exploited this information, in combination with homology modeling and docking approaches, to identify a potential binding site on TRAM lined by the BB loop and αC helix. Virtual screening of commercially available small...
Background This study evaluated the mode of action of Cinnamomum impressicostatum on Methicillin Resistant Staphylococcus aureus (MRSA). Cinnamon is one of the most popular spices used by mankind to enhance the flavour of his cuisine. In...
moreBackground This study evaluated the mode of action of Cinnamomum impressicostatum on Methicillin Resistant Staphylococcus aureus (MRSA). Cinnamon is one of the most popular spices used by mankind to enhance the flavour of his cuisine. In addition, cinnamon contains medicinally important essential oils in its leaves, stems, twigs, fruits and inner and outer bark. Many species of cinnamon are widely used in traditional medicinal systems around the world for the treatment of a wide variety of infectious diseases including tuberculosis and salmonellosis.Methods The crude stem – bark water extract of C.impressicostatum was generated using sequential soxhlet extraction. The antibacterial activity of the extract was investigated by performing broth microdilution assays and determination of the Minimum Inhibitory Concentration (MIC). A time kill study was performed to determine the killing efficiency of the extract. Potential bacteriolytic activity of the extract against MRSA was evaluated....
Molecules possessing harmine moiety are reported to exhibit marked fungicidal and bactericidal activities. In this study, various quinozilinium tetrafluoroborate salts were synthesized using acylic and cyclic oxoketene dithioacetals...
moreMolecules possessing harmine moiety are reported to exhibit marked fungicidal and bactericidal activities. In this study, various quinozilinium tetrafluoroborate salts were synthesized using acylic and cyclic oxoketene dithioacetals followed by cycloaromatization from Harmine. All of these synthesized compounds were characterized by 1 H NMR, 13 C NMR, Mass and CHN analysis. This methodology would find wide usage in the preparation of indolo quinozilinium -based library of small molecules useful for medicinal chemistry and in drug discovery. Graphic abstract
In the past decades, plants have been exploited as traditional therapeutic agents. This has led to recent studies which had been carried out on plants for investigations of their medicinal uses. The objective of this study was to evaluate...
moreIn the past decades, plants have been exploited as traditional therapeutic agents. This has led to recent studies which had been carried out on plants for investigations of their medicinal uses. The objective of this study was to evaluate and determine antimicrobial activity of different extracts from the stem bark and leaves of Dillenia obovata against five Gram-positive and six Gram-negative bacteria, seven yeasts and three fungi. Using disc diffusion method followed by broth microdilution, the results highlighted the most potent activity of hexane, ethyl acetate and methanol extracts of leaves were against Bacillus cereus with a minimum inhibition concentration of 0.0625mg/mL. Hexane, methanol, ethyl actetate and water extracts of stem bark and leaves exhibited broadest spectrum of antimicrobial activity against Gram-positive bacteria: Staphylococcus aureus, Bacillus cereus and Bacillus subtilis. Our findings suggest that D. obovata has the potential to be a good alternative to t...
This study’s objective was to examine L-arginine (L-arg) supplementation’s effect on mono-species biofilm (Streptococcus mutans/Streptococcus sanguinis) growth and underlying enamel substrates. The experimental groups were 1%, 2%, and 4%...
moreThis study’s objective was to examine L-arginine (L-arg) supplementation’s effect on mono-species biofilm (Streptococcus mutans/Streptococcus sanguinis) growth and underlying enamel substrates. The experimental groups were 1%, 2%, and 4% arg, and 0.9% NaCl was used as the vehicle control. Sterilised enamel blocks were subjected to 7-day treatment with test solutions and S. mutans/S. sanguinis inoculum in BHI. Post-treatment, the treated biofilms stained for live/dead bacterial cells were analysed using confocal microscopy. The enamel specimens were analysed using X-ray diffraction crystallography (XRD), Raman spectroscopy (RS), and transmission electron microscopy (TEM). The molecular interactions between arg and MMP-2/MMP-9 were determined by computational molecular docking and MMP assays. With increasing arg concentrations, bacterial survival significantly decreased (p < 0.05). The XRD peak intensity with 1%/2% arg was significantly higher than with 4% arg and the control (p &l...
Tuberculosis (TB) is a contagious airborne disease caused by Mycobacterium tuberculosis, which primarily affects human lungs. The progression of drug-susceptible TB to drug-resistant strains, MDR-TB and XDR-TB, has become worldwide...
moreTuberculosis (TB) is a contagious airborne disease caused by Mycobacterium tuberculosis, which primarily affects human lungs. The progression of drug-susceptible TB to drug-resistant strains, MDR-TB and XDR-TB, has become worldwide challenge in eliminating TB. The limitations of conventional TB treatment including frequent dosing and prolonged treatment, which results in patient’s noncompliance to the treatment because of treatment-related adverse effects. The non-invasive pulmonary drug administration provides the advantages of targeted-site delivery and avoids first-pass metabolism, which reduced the dose requirement and systemic adverse effects of the therapeutics. With the modification of the drugs with advanced carriers, the formulations may possess sustained released property, which helps in reducing the dosing frequency and enhanced patients’ compliances. The dry powder inhaler formulation is easy to handle and storage as it is relatively stable compared to liquids and suspen...
A novel series of amide functionalized imidazo[1,2-a]pyridine ( 14a – 14j ) derivatives were synthesized and screened for their anticancer activities against breast (MCF-7 and MDA-MB-231), lung (A549), and prostate (DU-145) cancer cell...
moreA novel series of amide functionalized imidazo[1,2-a]pyridine ( 14a – 14j ) derivatives were synthesized and screened for their anticancer activities against breast (MCF-7 and MDA-MB-231), lung (A549), and prostate (DU-145) cancer cell lines using MTT assay with etoposide as the standard reference drug. Among them, compound 14j showed highest potency in anticancer activities against MCF-7, MDA-MB-231, A549, and DU-145 cell lines with IC 50 values of 0.021 ± 0.0012 µM, 0.95 ± 0.039 µM, 0.091 ± 0.0053 µM, and 0.24 ± 0.032 µM, respectively.
Oxidation of carbazole-3-carboxyaldehydes promoted by a 70% aqueous solution of tert-butylhydroperoxide leads to the corresponding carbazole-3-carboxylic acids in good yields. This transition-metal-free oxidation protocol is attractive...
moreOxidation of carbazole-3-carboxyaldehydes promoted by a 70% aqueous solution of tert-butylhydroperoxide leads to the corresponding carbazole-3-carboxylic acids in good yields. This transition-metal-free oxidation protocol is attractive for the synthesis of pharmaceutically important carbazole analogues.
Wounds still pose a huge burden on human health and healthcare systems in many parts of the world. Phytomedicines are being used to heal the wounds since ancient times. Now-a-days also many researchers are exploring the wound healing...
moreWounds still pose a huge burden on human health and healthcare systems in many parts of the world. Phytomedicines are being used to heal the wounds since ancient times. Now-a-days also many researchers are exploring the wound healing activity of phytomedicines. Wound healing is a complex process thus, it is always a question mark regarding the best test model (in vivo, ex vivo and in vitro) model to assess the wound healing activity of phytomedicines. In general, the researchers would opt for in vivo model - probably because of closer physiological relevance to human wounds. However, in vivo experimental models are not suitable for high throughput screening and not ethical in terms of initial screening of the phytomedicines. The in vivo models are associated with difficulties in obtaining the ethical approvals, requires huge budget, and resources. We argue that judicious selection of cell types would serve the purpose of developing a physiologically relevant in vitro experimental model. A lot of progress has been made in molecular biology techniques to bridge the gap between in vitro models and their physiological relevance. The in vitro models are the best suited for high throughput screening and to elucidate the molecular mechanisms. The main aim of this review is to provide insights on selection of the cell types for developing physiologically relevant in vitro wound healing assays, which can be used to improve the value of phytomedicines further.
Two new alkyl (E)-5-(methylsulfinyl) pent-4-enoates were isolated from the seeds of Raphanus sativus L., Brassicaceae. The compounds were identified as methyl-(E)-5-(methylsulfinyl) pent-4-enoate and ethyl-(E)-5-(methylsulfinyl)...
moreTwo new alkyl (E)-5-(methylsulfinyl) pent-4-enoates were isolated from the seeds of Raphanus sativus L., Brassicaceae. The compounds were identified as methyl-(E)-5-(methylsulfinyl) pent-4-enoate and ethyl-(E)-5-(methylsulfinyl) pent-4-enoate using 1D and 2D NMR and HR-EI-MS.
Pulmonary aspergillosis (PA), a pulmonary fungal infection caused by Aspergillus spp., is a concern for immunocompromised populations. Despite substantial research efforts, conventional treatments of PA using antifungal agents are...
morePulmonary aspergillosis (PA), a pulmonary fungal infection caused by Aspergillus spp., is a concern for immunocompromised populations. Despite substantial research efforts, conventional treatments of PA using antifungal agents are associated with limitations such as excessive systemic exposure, serious side effects and limited availability of the therapeutics in the lungs for an adequate duration. To overcome the limitations associated with the conventional regimens, pulmonary delivery of antifungal agents has become a focal point of research because of the superiority of local and targeted drug delivery. Dry powder inhalers and nebulized formulations of antifungal agents have been developed and evaluated for their capability to effectively deliver antifungal agents to the lungs. Moreover, progress in nanotechnology and the utilization of nanocarriers in the development of pulmonary delivery formulations has allowed further augmentation of treatment capability and efficiency. Thus, ...
Background: Breast cancer (BC) is one of the most common and prevalent cancer types among women. It is caused mainly due to mutations in receptors of estrogen or progesterone. There are several conventional treatment strategies available...
moreBackground: Breast cancer (BC) is one of the most common and prevalent cancer types among women. It is caused mainly due to mutations in receptors of estrogen or progesterone. There are several conventional treatment strategies available which include chemotherapy, radiation therapy, and partial or entire mastectomy. These are being most frequently used by most of the healthcare professionals for the treatment of BC. These commonly traditional forms of available treatment therapy, however, were often associated with multiple adverse effects, thus reducing patient compliance. Objective: This review focuses on therapeutic strategies driven by nanotechnology that are recognized as a frontline therapy to enhance therapeutic effectiveness and the unintended side-effects associated with incorporated anticancer drugs in the treatment of breast cancer. Results: Although there are several nanocarriers available, the folic acid conjugated nanocarriers have shown remarkable efficiency of speci...