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The aim of current study was to prepare Linum usitatissimum mucilage (LUM) based nanoparticles, capable of encapsulating hydrophobic drug ezetimibe as nanocarriers. Solvent evaporation and nanoprecipitation techniques were used to develop nanoparticles by encapsulating ezetimibe in the articulated matrix of polysaccharide fractions. Developed nanoparticles were characterized to determine the particle size, zeta potential, polydispersibility index (PDI), and entrapment efficiency (EE). Morphology and physicochemical characterization were carried out through SEM, FTIR, PXRD and thermal analysis. Saturation solubility and in vitro release studies were also performed. Safety assessment of ezetimibe loaded nanoparticles was evaluated via oral acute toxicity study. The mean particle size, zeta potential, PDI and EE for emulsion solvent evaporation were 683.6 nm, -28.3 mV, 0.39, 63.7% and for nanoprecipitation were 637.7 nm, 0.07, -27.1 mV and 80%, respectively. Thermal analysis confirmed enhanced thermal stability, whereas PXRD confirmed amorphous nature of drug. Saturation solubility (p-value <0.05) demonstrated improved solubility of drug when enclosed in linseed nanoparticles. Nanoprecipitation surpasses emulsion solvent evaporation in dissolution test by possessing smaller size. Acute oral toxicity study indicated no significant changes in behavioral, clinical or histopathological parameters of control and experimental groups. The in vitro release of ezetimibe was augmented by enhancing aqueous solubility through devised nanoparticles. Thus, linseed mucilage could act as biopolymer in the fabrication of nanoparticle formulation. The acute oral toxicological investigations provided evidence that LUMNs were safe after oral administration.
Ume Ruqia Tulain; Arshad Mahmood; Sidra Aslam; Alia Erum; Nadia Shamshad Malik; Ayesha Rashid; Rizwana Kausar; Mohammed S Alqahtani. Formulation and Evaluation of Linum usitatissimum Mucilage-Based Nanoparticles for Effective Delivery of Ezetimibe. International Journal of Nanomedicine 2021, ume 16, 4579 -4596.
AMA StyleUme Ruqia Tulain, Arshad Mahmood, Sidra Aslam, Alia Erum, Nadia Shamshad Malik, Ayesha Rashid, Rizwana Kausar, Mohammed S Alqahtani. Formulation and Evaluation of Linum usitatissimum Mucilage-Based Nanoparticles for Effective Delivery of Ezetimibe. International Journal of Nanomedicine. 2021; ume 16 ():4579-4596.
Chicago/Turabian StyleUme Ruqia Tulain; Arshad Mahmood; Sidra Aslam; Alia Erum; Nadia Shamshad Malik; Ayesha Rashid; Rizwana Kausar; Mohammed S Alqahtani. 2021. "Formulation and Evaluation of Linum usitatissimum Mucilage-Based Nanoparticles for Effective Delivery of Ezetimibe." International Journal of Nanomedicine ume 16, no. : 4579-4596.
The oral route is the most common route for drug administration. It is the most preferred route, due to its advantages, such as non-invasiveness, patient compliance and convenience of drug administration. Various factors govern oral drug absorption including drug solubility, mucosal permeability, and stability in the gastrointestinal tract environment. Attempts to overcome these factors have focused on understanding the physicochemical, biochemical, metabolic and biological barriers which limit the overall drug bioavailability. Different pharmaceutical technologies and drug delivery systems including nanocarriers, micelles, cyclodextrins and lipid-based carriers have been explored to enhance oral drug absorption. To this end, this review will discuss the physiological, and pharmaceutical barriers influencing drug bioavailability for the oral route of administration, as well as the conventional and novel drug delivery strategies. The challenges and development aspects of pediatric formulations will also be addressed.
Mohammed S. Alqahtani; Mohsin Kazi; Mohammad A. Alsenaidy; Muhammad Z. Ahmad. Advances in Oral Drug Delivery. Frontiers in Pharmacology 2021, 12, 1 .
AMA StyleMohammed S. Alqahtani, Mohsin Kazi, Mohammad A. Alsenaidy, Muhammad Z. Ahmad. Advances in Oral Drug Delivery. Frontiers in Pharmacology. 2021; 12 ():1.
Chicago/Turabian StyleMohammed S. Alqahtani; Mohsin Kazi; Mohammad A. Alsenaidy; Muhammad Z. Ahmad. 2021. "Advances in Oral Drug Delivery." Frontiers in Pharmacology 12, no. : 1.
Curcumin (CUR) is an attractive polyphenol for its anti-inflammatory, antibacterial, antioxidant, and anticancer properties. Poor solubility in water and sensitivity against sunlight are the most challenging characteristics in the development of CUR for clinical use. The aim is to develop oral lipid-based bioactive self-nanoemulsifying drug delivery systems (Bio-SNEDDSs) for curcumin as a candidate for cancer therapy. Bio-SNEDDSs containing black seed oil, medium-chain mono- and diglycerides, and surfactants were prepared as CUR delivery vehicles. The morphology, droplet size, physical stability, encapsulation efficiency, risk of precipitation, lipid digestion, antioxidant activity, and antimicrobial activity were evaluated for the representative formulations. Finally, an MTT assay was performed on MCF-7 cells to determine the cytotoxic effect of the different formulations. The results showed lower droplet size (28.53 nm) and higher drug-loading (CUR 20 mg, thymoquinone 1.2 mg) for the representative Bio-SNEDDS (black seed oil/Imwitor 988/KolliphorEL (35/15/50) % w/w), along with a transparent appearance upon aqueous dilution. The dynamic dispersion and in-vitro lipolysis data proved that the Bio-SNEDDS was able to keep the CUR in a solubilized form in the gastrointestinal tract. From the antioxidant and antimicrobial studies, it was suggested that the Bio-SNEDDS had the highest activity for disease control. The MTT assay showed that the representative Bio-SNEDDS treatment led to a reduction of cell viability of MCF-7 cells compared to pure CUR and conventional SNEDDSs. A Bio-SNEDDS with elevated entrapment efficiency, antioxidant/antimicrobial activities, and an antiproliferative effect could be the best anticancer drug candidate for potential oral delivery.
Mohsin Kazi; Fahd A. Nasr; Omar Noman; Abdulrahman Alharbi; Mohammed S. Alqahtani; Fars K. Alanazi. Development, Characterization Optimization, and Assessment of Curcumin-Loaded Bioactive Self-Nanoemulsifying Formulations and Their Inhibitory Effects on Human Breast Cancer MCF-7 Cells. Pharmaceutics 2020, 12, 1107 .
AMA StyleMohsin Kazi, Fahd A. Nasr, Omar Noman, Abdulrahman Alharbi, Mohammed S. Alqahtani, Fars K. Alanazi. Development, Characterization Optimization, and Assessment of Curcumin-Loaded Bioactive Self-Nanoemulsifying Formulations and Their Inhibitory Effects on Human Breast Cancer MCF-7 Cells. Pharmaceutics. 2020; 12 (11):1107.
Chicago/Turabian StyleMohsin Kazi; Fahd A. Nasr; Omar Noman; Abdulrahman Alharbi; Mohammed S. Alqahtani; Fars K. Alanazi. 2020. "Development, Characterization Optimization, and Assessment of Curcumin-Loaded Bioactive Self-Nanoemulsifying Formulations and Their Inhibitory Effects on Human Breast Cancer MCF-7 Cells." Pharmaceutics 12, no. 11: 1107.
The main objective of the present study was to investigate the hemo and immune compatibility of gliadin nanoparticles as a function of particle size. Gliadin nanoparticles of different size were prepared using a modified antisolvent nanoprecipitation method. The hemolytic potential of gliadin nanoparticles was evaluated using in vitro hemolysis assay. Phagocytic uptake of gliadin nanoparticles was studied using rat polymorphonuclear (PMN) leukocytes and murine alveolar peritoneal macrophage (J774) cells. In vivo immunogenicity of gliadin nanoparticles was studied following subcutaneous administration in mice. Gliadin nanoparticles were non-hemolytic irrespective of particle size and hence compatible with blood components. In comparison to positive control zymosan, gliadin nanoparticles with a size greater than 406 ± 11 nm showed higher phagocytic uptake in PMN cells, while the uptake was minimal with smaller nanoparticles (127 ± 8 nm). Similar uptake of gliadin nanoparticles was observed in murine alveolar peritoneal macrophages. Anti-gliadin IgG antibody titers subsequent to primary and secondary immunization of gliadin nanoparticles in mice were in the increasing order of 406 ± 11 nm < 848 ± 20 nm < coarse suspension). On the other hand, gliadin nanoparticles of 127 ± 8 nm in size did not elicit immunogenic response. Phagocytosis and immunogenicity of gliadin nanoparticles are strongly influenced by particle size. The results of this study can provide useful information for rational design of protein-based nanomaterials in drug delivery applications.
Mohammed Alqahtani; Rabbani Syed; Meshal Alshehri. Size-Dependent Phagocytic Uptake and Immunogenicity of Gliadin Nanoparticles. Polymers 2020, 12, 2576 .
AMA StyleMohammed Alqahtani, Rabbani Syed, Meshal Alshehri. Size-Dependent Phagocytic Uptake and Immunogenicity of Gliadin Nanoparticles. Polymers. 2020; 12 (11):2576.
Chicago/Turabian StyleMohammed Alqahtani; Rabbani Syed; Meshal Alshehri. 2020. "Size-Dependent Phagocytic Uptake and Immunogenicity of Gliadin Nanoparticles." Polymers 12, no. 11: 2576.
The emergence of new material platforms, focused on nanotechnology, have resulted in a growing interest in their application to healing skin wounds. The skin forms an effective barrier against the external environment and consequently, rapid healing of wound tissue after injury is essential. Curcumin (diferuloylmethane) is a promising small molecule for the treatment of wounds based on its wound-healing activity and antioxidant and anti-inflammatory properties. However, its therapeutic application is limited by the poor skin permeability and bioavailability due to its poor solubility and low stability. Herein, curcumin loaded LNPs was prepared and characterized for their wound healing activity. Cytotoxicity assays indicated that curcumin-free and loaded nanoparticles were biocompatible with skin keratinocytes with no cytotoxic effects, suggesting that they did not interfere with cell proliferation during wound healing. Curcumin loaded LNPs exhibited potent in vitro antibacterial activity against gram-positive bacterial pathogens, particularly against Staphylococcus aureus, the most common wound bacterium. Fibroblast cell migration was observed using a scratch assay; upon treatment with curcumin loaded LNPs, wounded keratinocytes exhibited increased cell migration, which is a key feature of wound healing. The in vivo results showed that wounded rats treated with curcumin loaded LNPs exhibited enhanced dermal wound closure compared with the untreated control. After 12 days, the wounds treated with curcumin loaded LNPs achieved nearly full wound contraction compared with the untreated control, which had a wound size reduction of approximately 43%. Curcumin-loaded LNPs treated wounds showed advanced granulation tissue formation, characterized by greater collagen deposition. They also had lower myeloperoxidase activity, which is indicative of less inflammatory infiltration. Lower expression of matrix metalloproteinases (MMPs), especially MMP9, was characteristic of wounds treated with curcumin loaded LNPs. Overall, the results from this study highlight the advantages of using lignin as a nanocarrier to accelerate wound healing.
Mohammed S. Alqahtani; Ali Alqahtani; Mohsin Kazi; Muhammad Z. Ahmad; Abdullah Alahmari; Mohammad A. Alsenaidy; Rabbani Syed. Wound-healing potential of curcumin loaded lignin nanoparticles. Journal of Drug Delivery Science and Technology 2020, 60, 102020 .
AMA StyleMohammed S. Alqahtani, Ali Alqahtani, Mohsin Kazi, Muhammad Z. Ahmad, Abdullah Alahmari, Mohammad A. Alsenaidy, Rabbani Syed. Wound-healing potential of curcumin loaded lignin nanoparticles. Journal of Drug Delivery Science and Technology. 2020; 60 ():102020.
Chicago/Turabian StyleMohammed S. Alqahtani; Ali Alqahtani; Mohsin Kazi; Muhammad Z. Ahmad; Abdullah Alahmari; Mohammad A. Alsenaidy; Rabbani Syed. 2020. "Wound-healing potential of curcumin loaded lignin nanoparticles." Journal of Drug Delivery Science and Technology 60, no. : 102020.
Vaccination is the most effective strategy of preventing and treating infectious diseases and the most significant issue in the development of potent vaccines is the sufficient immunogenicity and safety of vaccines. The main goal of the present study is to develop a potent and safe vaccine adjuvant that can also stabilize antigen formulations during preparation and storage. In this study, the model antigen ovalbumin (OVA) was encapsulated in polymeric nanoparticles based on lignin (OVA-LNPs). The nanoparticles had a particle size of 216 nm and a low polydispersity index. The nanoparticles were negatively charged (−26.7 mV) with high encapsulation efficiency 81.6% of OVA antigen. In vitro studies of the nanoparticles were tested against dendritic cells (DCs), specialized antigen-presenting cells (APCs). The results showed no cytotoxic effect from LNPs and a significantly higher percentage of dendritic cells have taken up the antigen when encapsulated inside LNPs in contrast to free OVA. The nanoparticle was administered intradermally to BALB/c mice and the resulting time-dependent systemic immune responses towards OVA were assessed by measuring the OVA-specific IgG titers using an enzyme-linked immunosorbent assay (ELISA). In vivo immunization with OVA-LNPs induced a stronger IgG antibody response than that induced by free OVA or alum adjuvanted OVA. Enhanced immunization by OVA-LNPs was attributed to the observed efficient uptake of the antigen by dendritic cells. These findings demonstrate that LNPs are promising to be used as vaccine adjuvant and delivery system for the induction of long-term immune responses.
Mohammed S. Alqahtani; Mohsin Kazi; Muhammad Z. Ahmad; Rabbani Syed; Mohammad A. Alsenaidy; Salem A. Albraiki. Lignin nanoparticles as a promising vaccine adjuvant and delivery system for ovalbumin. International Journal of Biological Macromolecules 2020, 163, 1314 -1322.
AMA StyleMohammed S. Alqahtani, Mohsin Kazi, Muhammad Z. Ahmad, Rabbani Syed, Mohammad A. Alsenaidy, Salem A. Albraiki. Lignin nanoparticles as a promising vaccine adjuvant and delivery system for ovalbumin. International Journal of Biological Macromolecules. 2020; 163 ():1314-1322.
Chicago/Turabian StyleMohammed S. Alqahtani; Mohsin Kazi; Muhammad Z. Ahmad; Rabbani Syed; Mohammad A. Alsenaidy; Salem A. Albraiki. 2020. "Lignin nanoparticles as a promising vaccine adjuvant and delivery system for ovalbumin." International Journal of Biological Macromolecules 163, no. : 1314-1322.
The current pandemic of 2019 novel coronavirus disease (COVID-19) caused by a novel virus strain, 2019-nCoV/SARS-CoV-2 have posed a serious threat to global public health and economy. It is largely unknown how the human immune system responds to this infection. A better understanding of the immune response to SARS-CoV-2 will be important to develop therapeutics against COVID-19. Here, we have used transcriptomic profile of human alveolar adenocarcinoma cells (A549) infected with SARS-CoV-2 and employed a network biology approach to generate human-virus interactome. Network topological analysis discovers 15 SARS-CoV-2 targets, which belongs to a subset of interferon (IFN) stimulated genes (ISGs). These ISGs (IFIT1, IFITM1, IRF7, ISG15, MX1, and OAS2) can be considered as potential candidates for drug targets in the treatments of COVID-19. We have identified significant interaction between ISGs and TLR3 agonists, like poly I: C, and imiquimod, and suggests that TLR3 agonists can be considered as a potential drug for drug repurposing in COVID-19. Our network centric analysis suggests that moderating the innate immune response is a valuable approach to target COVID-19.
Kartikay Prasad; Fatima Khatoon; Summya Rashid; Nemat Ali; Abdullah AlAsmari; Mohammad Z. Ahmed; Ali S. Alqahtani; Mohammed Alqahtani; Vijay Kumar. Targeting hub genes and pathways of innate immune response in COVID-19: A network biology perspective. International Journal of Biological Macromolecules 2020, 163, 1 -8.
AMA StyleKartikay Prasad, Fatima Khatoon, Summya Rashid, Nemat Ali, Abdullah AlAsmari, Mohammad Z. Ahmed, Ali S. Alqahtani, Mohammed Alqahtani, Vijay Kumar. Targeting hub genes and pathways of innate immune response in COVID-19: A network biology perspective. International Journal of Biological Macromolecules. 2020; 163 ():1-8.
Chicago/Turabian StyleKartikay Prasad; Fatima Khatoon; Summya Rashid; Nemat Ali; Abdullah AlAsmari; Mohammad Z. Ahmed; Ali S. Alqahtani; Mohammed Alqahtani; Vijay Kumar. 2020. "Targeting hub genes and pathways of innate immune response in COVID-19: A network biology perspective." International Journal of Biological Macromolecules 163, no. : 1-8.
In this study, attempts have been made to identify novel inhibitor(s) of SdiA (a homolog of LuxR transcription regulator) of Klebseilla pneumoniae using various computational techniques. 4LFU was used as a template to model the structure of SdiA. ProCheck, Verify3D, Ramachandran plot scores and ProSA-Web confirmed the good quality of the model as the root mean square deviation (RMSD) between SdiA model, and 4LFU template was estimated to be 0.21 Å. The secondary structural contents of SdiA model were predicted using PDBsum. The only binding site of SdiA was identified (area = 523.083 Å2 and volume = 351.044 Å3) using CASTp. Molecular docking at three different levels (high throughput virtual screening, standard precision (SP) and extra precision (XP) dockings) with increasingly stringent conditions was performed using Glide on Selleck’s express pick library (L3600). A total of 61 ligands were found to bind with high affinities to the active site of SdiA. Further, the effect of solvent on protein-ligand interaction was evaluated by performing molecular mechanics-general born surface area (Prime/MM-GBSA). On the basis of Prime/MM-GBSA score, molecular dynamics simulation (50 ns) was performed on the ligand (WAY-390139-A) showing lowest binding energy to confirm the stability of protein-ligand complex. Docking energy and the corresponding binding affinity of WAY-390139-A towards SdiA were estimated to be -13.005 kcal/mol and 3.46 × 109 M−1, respectively. Our results confirm that WAY-390139-A binds at the autoinducer binding site of SdiA with high affinity and stability, and can be further exploited as potential drug against K. pneumoniae after experimental validation.
Mohammad Z. Ahmed; Ghazala Muteeb; Saif Khan; Ali S. Alqahtani; Pallavi Somvanshi; Mohammed S. Alqahtani; Keshav Lalit Ameta; Shafiul Haque. Identifying novel inhibitor of quorum sensing transcriptional regulator (SdiA) of Klebsiella pneumoniae through modelling, docking and molecular dynamics simulation. Journal of Biomolecular Structure and Dynamics 2020, 39, 3594 -3604.
AMA StyleMohammad Z. Ahmed, Ghazala Muteeb, Saif Khan, Ali S. Alqahtani, Pallavi Somvanshi, Mohammed S. Alqahtani, Keshav Lalit Ameta, Shafiul Haque. Identifying novel inhibitor of quorum sensing transcriptional regulator (SdiA) of Klebsiella pneumoniae through modelling, docking and molecular dynamics simulation. Journal of Biomolecular Structure and Dynamics. 2020; 39 (10):3594-3604.
Chicago/Turabian StyleMohammad Z. Ahmed; Ghazala Muteeb; Saif Khan; Ali S. Alqahtani; Pallavi Somvanshi; Mohammed S. Alqahtani; Keshav Lalit Ameta; Shafiul Haque. 2020. "Identifying novel inhibitor of quorum sensing transcriptional regulator (SdiA) of Klebsiella pneumoniae through modelling, docking and molecular dynamics simulation." Journal of Biomolecular Structure and Dynamics 39, no. 10: 3594-3604.
Bee pollens are rich source of essential amino acids and are often considered as complete food for human beings. Herein, we exploited the potential reducing abilities of Bee pollens extract for the eco-friendly preparation of silver nanoparticles (AgNPs-G). The resulting NPs were characterized using a combination of microscopic and spectroscopic techniques. The analyses confirm the formation of spherical Ag NPs. AgNPs-G obtained from the aqueous extract of bee pollens was used to study their antibacterial properties against Gram-positive and Gram-negative microbes using the Minimum Inhibitory Concentration 50 (MIC50) method. The antibacterial properties of AgNPs-G were compared to the properties of chemically synthesized Ag NPs (AgNPs-C) using sodium borohydride as a reducing agent. The green synthesized nanoparticles (AgNPs-G) exhibited a better antibacterial activity against most of the studied strains when compared to the chemically synthesized Ag NPs (AgNPs-C). In addition, the anti-cancer activity of Ag NPs was also studied against human liver and breast carcinoma cell lines by applying MTT-assay. The Ag NPs demonstrated considerable anticancer activity against the studied cell lines and exhibited high IC50 values in both MCF-7 and HepG2 cell lines.
Hanan M. Al-Yousef; Musarat Amina; Ali S. Alqahtani; Mohammed S. Alqahtani; Abdul Malik; Mohammad Rafe Hatshan; Mohammed Rafiq H. Siddiqui; Mujeeb Khan; Mohammed Rafi Shaik; Mohammad Shamsul Ola; Rabbani Syed. Pollen Bee Aqueous Extract-Based Synthesis of Silver Nanoparticles and Evaluation of Their Anti-Cancer and Anti-Bacterial Activities. Processes 2020, 8, 524 .
AMA StyleHanan M. Al-Yousef, Musarat Amina, Ali S. Alqahtani, Mohammed S. Alqahtani, Abdul Malik, Mohammad Rafe Hatshan, Mohammed Rafiq H. Siddiqui, Mujeeb Khan, Mohammed Rafi Shaik, Mohammad Shamsul Ola, Rabbani Syed. Pollen Bee Aqueous Extract-Based Synthesis of Silver Nanoparticles and Evaluation of Their Anti-Cancer and Anti-Bacterial Activities. Processes. 2020; 8 (5):524.
Chicago/Turabian StyleHanan M. Al-Yousef; Musarat Amina; Ali S. Alqahtani; Mohammed S. Alqahtani; Abdul Malik; Mohammad Rafe Hatshan; Mohammed Rafiq H. Siddiqui; Mujeeb Khan; Mohammed Rafi Shaik; Mohammad Shamsul Ola; Rabbani Syed. 2020. "Pollen Bee Aqueous Extract-Based Synthesis of Silver Nanoparticles and Evaluation of Their Anti-Cancer and Anti-Bacterial Activities." Processes 8, no. 5: 524.
Biofilms are bacterial cells, especially planktonic bacteria, structured as a community; they group, grow, and develop together by way of complex chemical and molecular communication. The biochemical communication in a biofilm is termed “quorum sensing,” and constitutes the most vital component of their structural and functional stability. In addition to this constant chemical communication, they also exchange nutrients and sometimes genetic components, giving rise to daughter cells with altered genetic makeup. Bacterial biofilms can occur in different contexts, including dental plaque on teeth and pond scum in the environment. Bacterial biofilms are usually infectious and pose considerable challenges to treat. After sufficient growth and expansion, biofilms start discharging their “virulence” in either of two forms: (1) planktonic shower or (2) fragment detachment. The huge mass of bacterial cells in a biofilm is immensely stronger than the corresponding singular planktonic pattern, and their collective virulence presents a heavy challenge to the host’s immune cells. Biofilm bacteria are usually resistant to most common antibiotics, and present a great threat of ruinous infection. Infectious biofilms can sometimes also demand surgical resection of the infected tissue or organ. In addition to the bacterial biofilms, fungi and viral particles integrate to form large communities, producing concomitantly challenging infections. Many species of fungi including Aspergillus, Cryptococcus, Trichosporon, and Pneumocystis are all capable of forming fungal biofilms and collectively exhibit resistance to antifungal therapies. However, biofilms are not always menacing to human life. Their beneficial effects and biotechnological applications are very active fields of research. Nonetheless, biofilms of bacterial, fungal, and viral origin all constitute major platforms for chronic infections and diseases. As a mechanistic approach, scientists believe that the destruction or inhibition of “quorum sensing” can enable disruption of bacterial biofilms. Research also supports that pyruvate is essential for the construction and maintenance of biofilms, and its depletion can degrade their strength. This chapter will explain in detail the molecular signaling, construction, and maintenance of biofilms, their potential threats and beneficial applications, and current research goals.
Rabbani Syed; Mohammed Alqahtani; Ayesha Mateen; Fawaz Alasmari; Youssef Sari. Understanding Biofilm Dynamics: In Vitro and In Vivo Models. Model Organisms for Microbial Pathogenesis, Biofilm Formation and Antimicrobial Drug Discovery 2020, 509 -526.
AMA StyleRabbani Syed, Mohammed Alqahtani, Ayesha Mateen, Fawaz Alasmari, Youssef Sari. Understanding Biofilm Dynamics: In Vitro and In Vivo Models. Model Organisms for Microbial Pathogenesis, Biofilm Formation and Antimicrobial Drug Discovery. 2020; ():509-526.
Chicago/Turabian StyleRabbani Syed; Mohammed Alqahtani; Ayesha Mateen; Fawaz Alasmari; Youssef Sari. 2020. "Understanding Biofilm Dynamics: In Vitro and In Vivo Models." Model Organisms for Microbial Pathogenesis, Biofilm Formation and Antimicrobial Drug Discovery , no. : 509-526.
Nuxia oppositifolia is traditionally used in diabetes treatment in many Arabian countries; however, scientific evidence is lacking. Hence, the present study explored the antidiabetic and antioxidant activities of the plant extracts and their purified compounds. The methanolic crude extract of N. oppositifolia was partitioned using a two-solvent system. The n-hexane fraction was purified by silica gel column chromatography to yield several compounds including katononic acid and 3-oxolupenal. Antidiabetic activities were assessed by α-amylase and α-glucosidase enzyme inhibition. Antioxidant capacities were examined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) scavenging assays. Further, the interaction between enzymes (α-amylase and α-glucosidase) and ligands (3-oxolupenal and katononic acid) was followed by fluorescence quenching and molecular docking studies. 3-oxolupenal and katononic acid showed IC50 values of 46.2 μg/mL (101.6 µM) and 52.4 μg/mL (119.3 µM), respectively against the amylase inhibition. 3-oxolupenal (62.3 µg/mL or 141.9 μM) exhibited more potent inhibition against α-glucosidases compared to katononic acid (88.6 µg/mL or 194.8 μM). In terms of antioxidant activity, the relatively polar crude extract and n-butanol fraction showed the greatest DPPH and ABTS scavenging activity. However, the antioxidant activities of the purified compounds were in the low to moderate range. Molecular docking studies confirmed that 3-oxolupenal and katononic acid interacted strongly with the active site residues of both α-amylase and α-glucosidase. Fluorescence quenching results also suggest that 3-oxolupenal and katononic acid have a good affinity towards both α-amylase and α-glucosidase enzymes. This study provides preliminary data for the plant’s use in the treatment of type 2 diabetes mellitus.
Ali S. Alqahtani; Syed Hidayathulla; Tabish Rehman; Ali A. ElGamal; Shaza Al-Massarani; Valentina Razmovski-Naumovski; Mohammed S. Alqahtani; Rabab A. El Dib; Mohamed F. AlAjmi. Alpha-Amylase and Alpha-Glucosidase Enzyme Inhibition and Antioxidant Potential of 3-Oxolupenal and Katononic Acid Isolated from Nuxia oppositifolia. Biomolecules 2019, 10, 61 .
AMA StyleAli S. Alqahtani, Syed Hidayathulla, Tabish Rehman, Ali A. ElGamal, Shaza Al-Massarani, Valentina Razmovski-Naumovski, Mohammed S. Alqahtani, Rabab A. El Dib, Mohamed F. AlAjmi. Alpha-Amylase and Alpha-Glucosidase Enzyme Inhibition and Antioxidant Potential of 3-Oxolupenal and Katononic Acid Isolated from Nuxia oppositifolia. Biomolecules. 2019; 10 (1):61.
Chicago/Turabian StyleAli S. Alqahtani; Syed Hidayathulla; Tabish Rehman; Ali A. ElGamal; Shaza Al-Massarani; Valentina Razmovski-Naumovski; Mohammed S. Alqahtani; Rabab A. El Dib; Mohamed F. AlAjmi. 2019. "Alpha-Amylase and Alpha-Glucosidase Enzyme Inhibition and Antioxidant Potential of 3-Oxolupenal and Katononic Acid Isolated from Nuxia oppositifolia." Biomolecules 10, no. 1: 61.
In this current study, we demonstrated the green synthesis and characterization of silver nanoparticles using Myrtus communis L. plant extract (Ag-MC) and its evaluation of anticancer and antimicrobial activities. The green synthesis of (Ag-MC), was assessed by numerous characterization techniques such as ultraviolet-visible spectroscopy (UV-VIS), Fourier-transform infrared spectroscopy (FT-IR), X-ray powder diffraction (XRD) transmission electron microscopy (TEM) and energy dispersive x-ray spectroscopy (EDX). The anti-cancer activity of the green synthesized silver nanoparticles was evaluated by the median inhibitory dose (IC50) on human liver carcinoma cell lines (HepG2). These results suggested that SN-NPs can be used as effective anticancer cell lines, as well as antibacterial and antiseptic agents in the medical field. This study showed that overexpression of aldose reductase (AR) in the human liver carcinoma cell line, HepG2, was down regulated by administration of SN-MC. The down regulation of AR was associated with abrogation of Pl3k/Akt, ERK and NF-kB pathways and the inhibition of cancer hallmarks, however, the target molecule for SN-MC was not practically established. Thus it is still unknown if the consequences were due to AR inhibition or direct Ag-MC interaction with AR.
Abdulwahab Ali Abuderman; Rabbani Syed; Abdullah A. Alyousef; Mohammed S. Alqahtani; Mohammad Shamsul Ola; Abdul Malik. Green Synthesized Silver Nanoparticles of Myrtus communis L (AgMC) Extract Inhibits Cancer Hallmarks via Targeting Aldose Reductase (AR) and Associated Signaling Network. Processes 2019, 7, 860 .
AMA StyleAbdulwahab Ali Abuderman, Rabbani Syed, Abdullah A. Alyousef, Mohammed S. Alqahtani, Mohammad Shamsul Ola, Abdul Malik. Green Synthesized Silver Nanoparticles of Myrtus communis L (AgMC) Extract Inhibits Cancer Hallmarks via Targeting Aldose Reductase (AR) and Associated Signaling Network. Processes. 2019; 7 (11):860.
Chicago/Turabian StyleAbdulwahab Ali Abuderman; Rabbani Syed; Abdullah A. Alyousef; Mohammed S. Alqahtani; Mohammad Shamsul Ola; Abdul Malik. 2019. "Green Synthesized Silver Nanoparticles of Myrtus communis L (AgMC) Extract Inhibits Cancer Hallmarks via Targeting Aldose Reductase (AR) and Associated Signaling Network." Processes 7, no. 11: 860.
Lignin nanoparticles (LNPs) were prepared with the objective of evaluating their application as a novel oral drug delivery system.
Mohammed S. Alqahtani; Ali Alqahtani; Abdullah Al-Thabit; Monzurul Roni; Rabbani Syed. Novel lignin nanoparticles for oral drug delivery. Journal of Materials Chemistry B 2019, 7, 4461 -4473.
AMA StyleMohammed S. Alqahtani, Ali Alqahtani, Abdullah Al-Thabit, Monzurul Roni, Rabbani Syed. Novel lignin nanoparticles for oral drug delivery. Journal of Materials Chemistry B. 2019; 7 (28):4461-4473.
Chicago/Turabian StyleMohammed S. Alqahtani; Ali Alqahtani; Abdullah Al-Thabit; Monzurul Roni; Rabbani Syed. 2019. "Novel lignin nanoparticles for oral drug delivery." Journal of Materials Chemistry B 7, no. 28: 4461-4473.
The goal of this study was to develop bioadhesive food protein nanoparticles using zein (Z), a hydrophobic corn protein as the core and whey protein (WP) as the shell for oral pediatric drug delivery applications. Lopinavir (LPV), an anti-retroviral drug and fenertinide, an investigational anti-cancer agent used were used as model drugs in the study. The particle size of ZWP nanoparticles was in the range of 200-250 nm and the drug encapsulation efficiency was > 70%. The nanoparticles showed sustained drug release in simulated gastrointestinal fluids. ZWP nanoparticles enhanced the permeability of LPV and fenretinide across Caco-2 cell monolayers. In both ex-vivo and in-vivo studies, ZWP nanoparticles were found to be strongly bioadhesive. ZWP nanoparticles enhanced the oral bioavailability of LPV and fenretinide by 4 and 7-fold respectively. ZWP nanoparticles also significantly increased the half-life of both drugs. The nanoparticles did not show any immunogenicity in mice. Overall, the study for the first time demonstrates the feasibility of developing a safe and effective food protein-based nanoparticles for pediatric oral drug delivery.
Saiful Islam; Joshua Reineke; Radhey S Kaushik; Tofuko Woyengo; Aravind Baride; Mohammed S. Alqahtani; Omathanu Perumal. Bioadhesive Food Protein Nanoparticles as Pediatric Oral Drug Delivery System. ACS Applied Materials & Interfaces 2019, 11, 18062 -18073.
AMA StyleSaiful Islam, Joshua Reineke, Radhey S Kaushik, Tofuko Woyengo, Aravind Baride, Mohammed S. Alqahtani, Omathanu Perumal. Bioadhesive Food Protein Nanoparticles as Pediatric Oral Drug Delivery System. ACS Applied Materials & Interfaces. 2019; 11 (20):18062-18073.
Chicago/Turabian StyleSaiful Islam; Joshua Reineke; Radhey S Kaushik; Tofuko Woyengo; Aravind Baride; Mohammed S. Alqahtani; Omathanu Perumal. 2019. "Bioadhesive Food Protein Nanoparticles as Pediatric Oral Drug Delivery System." ACS Applied Materials & Interfaces 11, no. 20: 18062-18073.
Fennel (Foeniculum vulgare Mill.) member from the family Umbelliferae (Apiaceae) and has been used in Saudi Arabia as an medicine as of the from the tradition. Our previous work with seed extracts of this plant generated DEAE-ion exchange purified proteins that exhibited antibacterial properties. The current study moves this work forward by using 2-D gel separation and MALDI TOF/TOF to identify proteins in this active extract. Fourteen protein spots were excised, digested, and identified. Several putative functions were identified, including: a copper-trans locating ATPase PAA1 chloroplastic-like isoform X1; a cytosolic enolase; a putative pentatricopeptide repeat-containing protein; an NADP-requiring isocitrate dehydrogenase; two proteins annotated as being encoded downstream from Son-like proteins; three probable nuclear proteins 5-1; and four predicted/ unidentified proteins. Future efforts will further characterize their relevant antimicrobial properties with the aim of cloning and high throughput synthesis of the antimicrobial element(s).
Abdullah A. Alyousef; Ayesha Mateen; Raid Al –Akeel; Abdulaziz Alqasim; Yazeed Al –Sheikh; Mohammed Alqahtani; Rabbani Syed. Screening & analysis of anionic peptides from Foeniculum vulgare Mill by mass spectroscopy. Saudi Journal of Biological Sciences 2018, 26, 660 -664.
AMA StyleAbdullah A. Alyousef, Ayesha Mateen, Raid Al –Akeel, Abdulaziz Alqasim, Yazeed Al –Sheikh, Mohammed Alqahtani, Rabbani Syed. Screening & analysis of anionic peptides from Foeniculum vulgare Mill by mass spectroscopy. Saudi Journal of Biological Sciences. 2018; 26 (4):660-664.
Chicago/Turabian StyleAbdullah A. Alyousef; Ayesha Mateen; Raid Al –Akeel; Abdulaziz Alqasim; Yazeed Al –Sheikh; Mohammed Alqahtani; Rabbani Syed. 2018. "Screening & analysis of anionic peptides from Foeniculum vulgare Mill by mass spectroscopy." Saudi Journal of Biological Sciences 26, no. 4: 660-664.
Due to growing concern towards microbial resistance, ongoing search for developing novel bioactive compounds such as peptides is on rise. The aim of this study was to evaluate antimicrobial effect of Populus trichocarpa extract, chemically identify the active peptide fraction and finds its target in Staphylococcus aureus. In this study the active fraction of P. trichocarpa crude extract was purified and characterized using MS/MS. This peptide PT13 antimicrobial activity was confirmed by in-vitro agar based disk diffusion and in-vivo infection model of G. mellonella. The proteomic expression analysis of S. aureus under influence of PT13 was studied using LTQ-Orbitrap-MS in-solution digestion and identity of target protein was acquired with their quantified expression using label-free approach of Progenesis QI software. Docking study was performed with peptide PT13 and its target YycG protein using CABS-dock. The active fraction PT13 sequence was identified as KVPVAAAAAAAAAVVASSMVVAAAK, with 25 amino acid including 13 alanine having M/Z 2194.2469. PT13 was uniformly inhibited growth S. aureus SA91 and MIC was determined 16 μg/mL for SA91 S. aureus strain. Sensor histidine kinase (YycG) was most significant target found differentially expressed under influence of PT13. G. mellonella larvae were killed rapidly due to S aureus infection, whereas death in protected group was insignificant in compare to control. The docking models showed ten docking models with RMSD value 1.89 for cluster 1 and RMSD value 3.95 for cluster 2 which is predicted to be high quality model. Alanine rich peptide could be useful in constructing as antimicrobial peptide for targeting extracellular Domain of Sensor Histidine Kinase YycG from S. aureus used in the study.
Raid Al Akeel; Ayesha Mateen; Rabbani Syed; Mohammed Alqahtani; Ali S. Alqahtani. Alanine rich peptide from Populus trichocarpa inhibit growth of Staphylococcus aureus via targetting its extracellular domain of Sensor Histidine Kinase YycGex protein. Microbial Pathogenesis 2018, 121, 115 -122.
AMA StyleRaid Al Akeel, Ayesha Mateen, Rabbani Syed, Mohammed Alqahtani, Ali S. Alqahtani. Alanine rich peptide from Populus trichocarpa inhibit growth of Staphylococcus aureus via targetting its extracellular domain of Sensor Histidine Kinase YycGex protein. Microbial Pathogenesis. 2018; 121 ():115-122.
Chicago/Turabian StyleRaid Al Akeel; Ayesha Mateen; Rabbani Syed; Mohammed Alqahtani; Ali S. Alqahtani. 2018. "Alanine rich peptide from Populus trichocarpa inhibit growth of Staphylococcus aureus via targetting its extracellular domain of Sensor Histidine Kinase YycGex protein." Microbial Pathogenesis 121, no. : 115-122.
The study was aimed at systematically investigating the influence of shell composition on the particle size, stability, release, cell uptake, permeability, and in vivo gastrointestinal distribution of food protein based nanocarriers for oral delivery applications. Three different core–shell nanocarriers were prepared using food-grade biopolymers including zein-casein (ZC) nanoparticles, zein-lactoferrin (ZLF), nanoparticles and zein-PEG (ZPEG) micelles. Nile red was used as a model hydrophobic dye for in vitro studies. The nanocarriers had negative, positive, and neutral charge, respectively. All three nanocarriers had a particle size of less than 200 nm and a low polydispersity index. The nanoparticles were stable at gastrointestinal pH (2–9) and ionic strength (10–200 mM). The nanocarriers sustained the release of Nile red in simulated gastric and intestinal fluids. ZC nanoparticles showed the slowest release followed by ZLF nanoparticles and ZPEG micelles. The nanocarriers were taken up by endocytosis in Caco-2 cells. ZPEG micelles showed the highest cell uptake and transepithelial permeability followed by ZLF and ZC nanoparticles. ZPEG micelles also showed P-gp inhibitory activity. All three nanocarriers showed bioadhesive properties. Cy 5.5, a near IR dye, was used to study the in vivo biodistribution of the nanocarriers. The nanocarriers showed longer retention in the rat gastrointestinal tract compared to the free dye. Among the three formulations, ZC nanoparticles was retained the longest in the rat gastrointestinal tract (≥24 h). Overall, the outcomes from this study demonstrate the structure–function relationship of core–shell protein nanocarriers. The findings from this study can be used to develop food protein based oral drug delivery systems with specific functional attributes.
Mohammed Alqahtani; M. Saiful Islam; Satheesh Podaralla; Radhey S. Kaushik; Joshua Reineke; Tofuko Woyengo; Omathanu Perumal. Food Protein Based Core–Shell Nanocarriers for Oral Drug Delivery: Effect of Shell Composition on in Vitro and in Vivo Functional Performance of Zein Nanocarriers. Molecular Pharmaceutics 2017, 14, 757 -769.
AMA StyleMohammed Alqahtani, M. Saiful Islam, Satheesh Podaralla, Radhey S. Kaushik, Joshua Reineke, Tofuko Woyengo, Omathanu Perumal. Food Protein Based Core–Shell Nanocarriers for Oral Drug Delivery: Effect of Shell Composition on in Vitro and in Vivo Functional Performance of Zein Nanocarriers. Molecular Pharmaceutics. 2017; 14 (3):757-769.
Chicago/Turabian StyleMohammed Alqahtani; M. Saiful Islam; Satheesh Podaralla; Radhey S. Kaushik; Joshua Reineke; Tofuko Woyengo; Omathanu Perumal. 2017. "Food Protein Based Core–Shell Nanocarriers for Oral Drug Delivery: Effect of Shell Composition on in Vitro and in Vivo Functional Performance of Zein Nanocarriers." Molecular Pharmaceutics 14, no. 3: 757-769.
Novel biodegradable micelles were synthesized by conjugating methoxy poly(ethylene glycol) (mPEG) to zein, a biodegradable hydrophobic plant protein. The mPEG–zein micelles were in the size range of 95–125 nm with a low CMC (5.5 × 10–2 g/L). The micelles were nonimmunogenic and were stable upon dilution with buffer as well as 10% serum. Curcumin, an anticancer agent with multiple delivery challenges, was encapsulated in mPEG–zein micelles. The micelles significantly enhanced the aqueous solubility (by 1000–2000-fold) and stability (by 6-fold) of curcumin. PEG–zein micelles sustained the release of curcumin up to 24 h in vitro. Curcumin-loaded mPEG–zein micelles showed significantly higher cell uptake than free curcumin in drug-resistant NCI/ADR-RES cancer cells in vitro. Micellar curcumin formulation was more potent than free curcumin in NCI/ADR-RES cancer cells, as evidenced from the 3-fold reduction in IC50 value of curcumin. Overall, this study for the first time reports a natural protein core based polymeric micelle and demonstrates its application for the delivery of hydrophobic anticancer drugs such as curcumin.
Satheesh Podaralla; Ranjith Averineni; Mohammed Alqahtani; Omathanu Perumal. Synthesis of Novel Biodegradable Methoxy Poly(ethylene glycol)–Zein Micelles for Effective Delivery of Curcumin. Molecular Pharmaceutics 2012, 9, 2778 -2786.
AMA StyleSatheesh Podaralla, Ranjith Averineni, Mohammed Alqahtani, Omathanu Perumal. Synthesis of Novel Biodegradable Methoxy Poly(ethylene glycol)–Zein Micelles for Effective Delivery of Curcumin. Molecular Pharmaceutics. 2012; 9 (9):2778-2786.
Chicago/Turabian StyleSatheesh Podaralla; Ranjith Averineni; Mohammed Alqahtani; Omathanu Perumal. 2012. "Synthesis of Novel Biodegradable Methoxy Poly(ethylene glycol)–Zein Micelles for Effective Delivery of Curcumin." Molecular Pharmaceutics 9, no. 9: 2778-2786.