Applications of Organic Chemistry in Nano-Medicine

Author(s):  
Asif Ahmad Malik ◽  
Nisar A. Dangroo ◽  
Rabia Amin ◽  
Zubaid Ul Khazir ◽  
Tabassum Ara

Nanotechnology offers multiple benefits. Nanomedicine and nanodelivery systems are relatively new areas in nanotechnology. There are number of outstanding applications of the nanomedicine in diagnosing diseases, delivering drugs to its target location, and thus treating human diseases. Here materials in the nanoscale range are employed to serve as means of diagnostic tools and also to deliver precise medicines to specific targeted sites in a controlled manner. Also, metal nanoparticles offer great interest in modern chemistry and materials research because of their applications in diverse fields such as photochemistry, nanoelectronics, optics, and catalysis. Chemistry provides various nanostructured materials either synthetic or isolated from natural sources offers opportunities and challenges in drug delivery and their applications including biomedical imaging, biosensing, diagnostic, and therapy. Thymoquinone, a bioactive compound in Nigella sativa, after encapsulation in lipid nanocarrier, has been found to show six-fold increase in bioavailability in comparison to free thymoquinone. In addition to this, organic nanomaterials have recently become of great interest for photovoltaic applications also.

2020 ◽  
Vol 11 (2) ◽  
pp. 1505-1510
Author(s):  
Durga B ◽  
Durga B ◽  
Dass Prakash M V ◽  
Julius A

In recent days, the thirst for the identification of the potential bioactive compounds from the natural sources like medicinal plants is on continuous demand. Among scientists and academicians, it has created many interdisciplinary platforms for research in establishing new drugs from the natural sources. According to many recent studies, Nigella sativa is believed to be the rich source of quinone, an effective bioactive compound with lots of medicinal values. The purpose of this study was to isolate and estimate the quinone in Nigella sativa seed extracts (aqueous and ethanol). Based on the qualitative and quantitative determination, the extracts were further focused for isolation of quinone from both aqueous and ethanolic  extracts of Nigella sativa. The isolated compound is identified by thin layer chromatography and purity is analyzed in High performance liquid chromatography. From the results we obtained, it was very clear that among the aqueous and ethanolic extracts of Nigella sativa, the ethanolic extract has been found with the highest quantity of quinine. This would be predicting that the ethanol extract of Nigella sativa may have good efficacy of pharmacological and therapeutic potentials like antidiabetic, anticancer, antimicrobial, anti-inflammatory properties when compared with the aqueous extract due to the presence of more quinone.


2021 ◽  
Vol 19 (7) ◽  
pp. 156-164
Author(s):  
Ennas Abdul Hussein ◽  
Asraa H. Aljbory ◽  
Sadiq J. Baqir ◽  
Ameera Hassan Hamed ◽  
Azal Shakir Waheeb ◽  
...  

Water pollution is one of the biggest problems facing us, so it requires the need to develop a very high-efficiency and inexpensive absorbent material from natural surfaces and compare it with expensive commercial sorbents. Where in this study an absorbent substance was prepared from the natural surfaces of Syzgium Aromaticum Flower Bud (SAFB), Nigella Sativa (NS) Converted to activated carbon to activated carbon Activated (SAFB), and Activated (NS), as these surfaces are characterized by high porosity, cheap price and very high efficiency in removing dye. The composite was illustrated via different analysis apparatus included FTIR, and FE-SEM, The adsorption result were fitted with Freundlich isotherms. The experimental kinetic result at different primary reactive green dye concentrations, were also analyzed through first model, second model and Elovich model. The obtained data appear that the model pseudo-first model fits the adsorption kinetic result through R2 0.96028, R2 0.9486, R2 0.9016 and R2 0.9620 of SAFB and ACTIVE-SAFB and Nigella Sativa (NS) and Activated (NS) in the same order.


2019 ◽  
Vol 86 (2) ◽  
pp. 217-221 ◽  
Author(s):  
Vittorio Tedde ◽  
Valerio Bronzo ◽  
Giulia Maria Grazia Puggioni ◽  
Claudia Pollera ◽  
Antonio Casula ◽  
...  

AbstractThis research communication reports the evaluation of cathelicidin in dairy goat milk for its relationship with the somatic cell count (SCC) and microbial culture results. Considering the limited performances of SCC for mastitis monitoring in goats, there is interest in evaluating alternative diagnostic tools. Cathelicidin is an antimicrobial protein involved in innate immunity of the mammary gland. In this work, half-udder milk was sampled bimonthly from a herd of 37 Alpine goats along an entire lactation and tested with the cathelicidin ELISA together with SCC and bacterial culture. Cathelicidin and SCC showed a strong correlation (r = 0.72; n = 360 milk samples). This was highest in mid-lactation (r = 0.83) and lowest in late lactation (r = 0.61), and was higher in primiparous (0.80, n = 130) than in multiparous goats (0.71, n = 230). Both markers increased with stage of lactation, but cathelicidin increased significantly less than SCC. In addition, peak level in late lactation was lower for cathelicidin (5.05-fold increase) than for SCC (7.64-fold increase). Twenty-one (5.8%) samples were positive to bacteriological culture, 20 for coagulase-negative staphylococci and one for Streptococcus spp.; 18 of them were positive to the cathelicidin ELISA (85.71% sensitivity). Sensitivity of SCC >500 000 and of SCC >1 000 000 cells/ml was lower (71.43 and 23.81%, respectively). Therefore, the high correlation of cathelicidin with SCC during the entire lactation, along with its lower increase in late lactation and good sensitivity in detecting intramammary infection (IMI), indicate a potential for monitoring subclinical mastitis in dairy goats. However, based on this preliminary assessment, specificity should be improved (40.41% for cathelicidin vs. 54.57 and 67.85% for SCC >500 000 and >1 000 000 cells/ml, respectively). Therefore, the application of cathelicidin for detecting goat IMI will require further investigation and optimization, especially concerning the definition of diagnostic thresholds.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 811
Author(s):  
Suhair Sunoqrot ◽  
Malek Alfaraj ◽  
Ala’a M. Hammad ◽  
Violet Kasabri ◽  
Dana Shalabi ◽  
...  

Thymoquinone (TQ) is a water-insoluble natural compound isolated from Nigella sativa that has demonstrated promising chemotherapeutic activity. The purpose of this study was to develop a polymeric nanoscale formulation for TQ to circumvent its delivery challenges. TQ-encapsulated nanoparticles (NPs) were fabricated using methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL) copolymers by the nanoprecipitation technique. Formulation variables included PCL chain length and NP architecture (matrix-type nanospheres or reservoir-type nanocapsules). The formulations were characterized in terms of their particle size, polydispersity index (PDI), drug loading efficiency, and drug release. An optimized TQ NP formulation in the form of oil-filled nanocapsules (F2-NC) was obtained with a mean hydrodynamic diameter of 117 nm, PDI of 0.16, about 60% loading efficiency, and sustained in vitro drug release. The formulation was then tested in cultured human cancer cell lines to verify its antiproliferative efficacy as a potential anticancer nanomedicine. A pilot pharmacokinetic study was also carried out in healthy mice to evaluate the oral bioavailability of the optimized formulation, which revealed a significant increase in the maximum plasma concentration (Cmax) and a 1.3-fold increase in bioavailability compared to free TQ. Our findings demonstrate that the versatility of polymeric NPs can be effectively applied to design a nanoscale delivery platform for TQ that can overcome its biopharmaceutical limitations.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2093
Author(s):  
Elisa Landucci ◽  
Francesca Bonomolo ◽  
Chiara De Stefani ◽  
Costanza Mazzantini ◽  
Domenico Edoardo Pellegrini-Giampietro ◽  
...  

Thymoquinone (TQ) is the main constituent of Nigella sativa L. essential oil. In vitro studies have shown its protective effect against H2O2-induced oxidative stress in human retinal pigment epithelium cells, and in vivo experiments have demonstrated its effect in decreasing corneal neovascularization and reducing the inflammation in an experimental dry eye model in mice. Its therapeutic use is limited by poor bioavailability, low solubility, and scarce permeability. In this study, two liposomal formulations have been developed, both of which consist of phosphatidylcholine and Plurol Oleique, a liquid lipid, and one of which is coated with 0.1% w/v hyaluronic acid (HA) to increase both TQ solubility and its ocular therapeutic potential. Each formulation has a size <200 nm and an EE% around 70%, determined by scattering techniques and the HPLC-DAD analytical method, respectively, and they result in a 2-fold increase in TQ solubility. HA-coated liposomes are stable over 2 months at +4 °C, and coated and uncoated liposomes present a gradual and prolonged release of TQ. Two cell lines, human corneal epithelial cells (HCEC-2) and human conjunctival epithelial cells (HConEC) were used to investigate the safety of the liposomal formulations. Uptake studies were also performed using fluorescent liposomes. Both liposomes and, in particular, HA-coated liposomes reduce the TQ toxicity observed at high doses in both HCEC-2 and HConEC cells, and both formulations increase the absorption at the cellular level and especially at the nucleus level, with a more pronounced effect for HA-coated liposomes.


2014 ◽  
Vol 5 (9) ◽  
pp. 1557-1572
Author(s):  
Hekmat Massoud ◽  
A. Hamza ◽  
Shadia Ahmed ◽  
Manal Meligy

Author(s):  
Waleed M. Sweileh ◽  
Adham S. AbuTaha ◽  
Ansam F. Sawalha ◽  
Suleiman Al-Khalil ◽  
Samah W. Al-Jabi ◽  
...  

Background: The year 2015 marked the end of United Nations Millennium Development Goals which was aimed at halting and reversing worldwide tuberculosis (TB). The emergence of drug resistance is a major challenge for worldwide TB control. The aim of this study was to give a bibliometric overview of publications on multi-, extensively, and totally drug-resistant TB. Methods: Scopus database was used to retrieve articles on multidrug resistant (MDR), extensively drug-resistant (XDR), and totally drug-resistant (TDR) tuberculosis for the study period (2006–2015). The number of publications, top productive countries and institutions, citation analysis, co-authorships, international collaboration, active authors, and active journals were retrieved and analyzed. Results: A total of 2260 journal articles were retrieved. The mean ± SD citations per article was 7.04 ± 16.0. The h-index of retrieved data was 76. The number of publications showed a three – fold increase over the study period compared with less than two – fold increase in tuberculosis research during the same study period. Stratified by number of publications, the United States of America ranked first while Switzerland ranked first in productivity per 100 million people, and South Africa ranked first in productivity stratified per one trillion Gross Domestic Product. Three of the High Burden Countries (HBC) MDR-TB (India, China, and South Africa) were present in top productive countries. High percentage of international collaboration was seen among most HBC MDR-TB. Except for Plos One journal, most active journals in publishing articles on MDR, XDR, TDR-TB were in infection – related fields and in general medicine. Top 20 cited articles were published in prestigious journal such as Lancet and New England Journal of Medicine. The themes in top 20 cited articles were diverse, ranging from molecular biology, diagnostic tools, co-infection with HIV, and results of new anti-TB drugs. Conclusion: Publications on MDR, XDR and TDR – TB are increasing in the past decade. International collaboration was common. Many low resourced African and Asian countries will benefit from research leading to new diagnostic and screening technology of TB. The exchange of expertise, ideas and technology is of paramount importance in this field.


Author(s):  
Abid Nordin ◽  
Haziq Kamal ◽  
Muhammad Dain Yazid ◽  
Aminuddin Saim ◽  
Ruszymah Idrus

Abstract Background Nigella sativa or commonly known as black seed or black cumin is one of the most ubiquitous complementary medicine. Epithelial to mesenchymal transition (EMT) of type 2 is defined by the balance between wound healing and tissue fibrosis, which is dependent to the state of inflammation. This systematic review is conducted to provide an overview regarding the reported effect of Nigella sativa and its bioactive compound on the type 2 EMT. Methods A search was done in EBSCOHOST, OVID and SCOPUS database to obtain potentially relevant articles that were published between 1823 and August 2019. This review includes studies that focus on the effect of Nigella sativa and its bioactive compound on the events related to type 2 EMT. Results A total of 1393 research articles were found to be potentially related to the effect of Nigella sativa and its bioactive compound, thymoquinone on Type 2 EMT. After screening was done, 22 research articles met inclusion criteria and were included in this review. Majority of the studies, reported better wound healing rate or significant prevention of tissue inflammation and organ fibrosis following Nigella sativa or thymoquinone treatments. In terms of wound healing, studies included reported progression of EMT related pathological changes after treatment with Nigella sativa or thymoquinone. Alternatively, in terms of fibrosis and inflammation, studies included reported reversal of pathological changes related to EMT after treatment with Nigella sativa or thymoquinone. Conclusion Through this review, Nigella sativa and thymoquinone have been associated with events in Type 2 EMT. They have been shown to promote wound healing, attenuate tissue inflammation, and prevent organ fibrosis via regulation of the EMT process.


Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3271 ◽  
Author(s):  
Onyeabor ◽  
Paik ◽  
Kovvasu ◽  
Ding ◽  
Lin ◽  
...  

Celastrol (CL), a bioactive compound isolated from Tripterygium wilfordii, has demonstrated bioactivities against a variety of diseases including cancer and obesity. However, its poor water solubility and rapid in vivo clearance limit its clinical applications. To overcome these limitations, nanotechnology has been employed to improve its pharmacokinetic properties. Nanoparticles made of biological materials offer minimal adverse effects while maintaining the efficacy of encapsulated therapeutics. Silk fibroin (SF) solution was prepared successfully by extraction from the cocoons of silkworms, and a final concentration of 2 mg/mL SF solution was used for the preparation of CL-loaded SF nanoparticles (CL-SFNP) by the desolvation method. A stirring speed of 750 rpm and storage time of 20 h at −20 °C resulted in optimized product yield. A high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of CL in rat plasma in terms of selectivity, linearity, intra-/inter-day precision and accuracy, and recovery. No interference was observed in rat plasma. Linearity in the concentration range of 0.05–5 µg/mL was observed with R2 of 0.999. Precision and accuracy values were below the limit of acceptance criteria, i.e., 15% for quality control (QC) samples and 20% for lower limit of quantification (LLOQ) samples. Rats were given intravenous (IV) administration of 1 mg/kg of pure CL in PEG 300 solution or CL-SFNP. The pharmacokinetic profile was improved with CL-SFNP compared to pure CL. Pure CL resulted in a maximum concentration (Cmax) value of 0.17 µg mL−1 at 5 min following administration, whereas that for CL-SFNP was 0.87 µg mL−1 and the extrapolated initial concentrations (C0) were 0.25 and 1.09 µg mL−1, respectively, for pure CL and CL-SFNP. A 2.4-fold increase in total area under the curve (AUC0-inf) (µg h mL−1) was observed with CL-SFNP when compared with pure CL. CL-SFNP demonstrated longer mean residence time (MRT; 0.67 h) than pure CL (0.26 h). In conclusion, the preparation of CL-SFNP was optimized and the formulation demonstrated improved pharmacokinetic properties compared to CL in solution following IV administration.


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