Adli AbdAllah Selim
@eaea.org.eg
Egyptian Atomic Energy Authority
Egyptian Atomic Energy Authority
RESEARCH INTERESTS
organic chemistry
radio-chemistry
pharmaceutical chemistry
nuclear medicine
nanotechnology
Scopus Publications
Scholar Citations
Scholar h-index
Scholar i10-index
Scopus Publications
Marwa M. Mehany, Olfat A. Hammam, Adli A. Selim, Galal H. Sayed, and Kurls E. Anwer
Springer Science and Business Media LLC
AbstractPyridine compounds are one of the most important heterocyclic derivatives showing wide ranges in biological and pharmacological activities. Green chemistry eliminates or reduces the generation of hazardous compounds. It prevents pollution at a molecular level. The microwave technique used in heterocyclic compound synthesis is also an important branch of green chemistry techniques. In this study, we report designing and synthesizing a new pyridine-bearing pentose moiety via a one-pot multicomponent reaction using D-glucose and also investigate its behavior and reactivity toward some simple and heterocyclic amino derivatives. The chemical structures of the synthesized compounds were characterized and tested for their cytotoxic activities. Some of the test compounds exhibited slight to high cytotoxic activities against Caco2 (colon cancer) cells, HepG2 (hepatocellular carcinoma) cells and MCF-7 (human breast cancer) cells by MTT assay. The results showed clearly that compound 4 and compound 8 displayed strongest to moderate cytotoxic activity against the HepG2, Caco2 and MCF-7 respectively and compound 1 showed good activity against MCF-7 in comparison to the standard anticancer drug doxorubicin. These data were by cytopathological examination. An in-vivo radioactive tracing study of compound 4 proved its targeting ability to sarcoma cells in a tumor-bearing mice model. Our findings suggest that the synthesized compounds may be promising candidates as novel anticancer agents.
Adli A. Selim, Islam M. Abdelmonem, Mohamed A. Amin, and Basma M. Essa
Springer Science and Business Media LLC
AbstractThis study focuses on tumor therapy using two biocompatible silver nanoplatforms of chamomile extract and its active ingredient apigenin-7-glucoside. Chamomile silver nanoparticles (Ch-AgNPs) and apigenin 7- glucoside silver nanoparticles (Ap-AgNPs) were synthesized and characterized using different analytical techniques. On a stable nanoplatform with spherical nanoparticles in a narrow size range, both Ch-AgNP and Ap-AgNP exhibit potent cytotoxic effects against two different cell lines (HepG2 and MCF7). The synthesized NPs were radiolabeled with 131I giving high radiochemical purity. Biodistribution studies in tumor-bearing Albino mice showed higher accumulation in tumor sites compared to normal muscle. In conclusion, after further preclinical studies, both chamomile silver nanoparticles (Ch-AgNPs) and apigenin-7-glucoside silver nanoparticles (Ap-AgNPs) can be used as potential drugs for tumor theranostics.
Mona A. Shewaiter, Adli A. Selim, Hassan M. Rashed, Yasser M. Moustafa, and Shadeed Gad
Springer Science and Business Media LLC
Abstract Background This work aimed to prepare niosomal formulations of an anticancer agent [mefenamic acid (MEF)] to enhance its cancer targeting. 131I was utilized as a radiolabeling isotope to study the radio-kinetics of MEF niosomes. Methods niosomal formulations were prepared by the ether injection method and assessed for entrapment efficiency (EE%), zeta potential (ZP), polydispersity index (PDI) and particle size (PS). MEF was labeled with 131I by direct electrophilic substitution reaction through optimization of radiolabeling-related parameters. In the radio-kinetic study, the optimal 131I-MEF niosomal formula was administered intravenously (I.V.) to solid tumor-bearing mice and compared to I.V. 131I-MEF solution as a control. Results the average PS and ZP values of the optimal formulation were 247.23 ± 2.32 nm and − 28.3 ± 1.21, respectively. The highest 131I-MEF labeling yield was 98.7 ± 0.8%. The biodistribution study revealed that the highest tumor uptake of 131I-MEF niosomal formula and 131I-MEF solution at 60 min post-injection were 2.73 and 1.94% ID/g, respectively. Conclusion MEF-loaded niosomes could be a hopeful candidate in cancer treatment due to their potent tumor uptake. Such high targeting was attributed to passive targeting of the nanosized niosomes and confirmed by radiokinetic evaluation.
Kurls E. Anwer, Galal H. Sayed, Basma M. Essa, and Adli A. Selim
Springer Science and Business Media LLC
AbstractNew derivatives of heterocyclic bearing pyrazole moiety were synthesized (eight new compounds from 2 to 9) via green synthesis methods (microwave-assisted and grinding techniques). 4,6-Diamino-1,3-diphenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (2) shows high anti-cancer activity against both HepG2 and HCT-116 with IC50 of 9.2 ± 2.8 and 7.7 ± 1.8 µM, respectively, which referenced to 5-Fu which is showing activity of 7.86 ± 0.5 and 5.35 ± 0.3 against both HepG2 and HCT-116, respectively. The cytotoxic activity against HCT-116 and HepG2 was slightly decreased and slightly increased, respectively, by a different pyrazole moiety (compound 5). Pharmacokinetics of compound 2 was carried out using the radioiodination technique in tumour-bearing Albino mice which shows good uptake at the tumour site. The biodistribution showed high accumulation in tumour tissues with a ratio of 13.7% ID/g organ after one hour in comparison with 2.97% ID/g organ at normal muscle at the same time point. As I-131 has maximum beta and gamma energies of 606.3 and 364.5 keV, respectively, therefore the newly synthesized compound 2 may be used for chemotherapy and TRT.
Esraa Taha, Samia A. Nour, Wael Mamdouh, Adli A. Selim, Mohamed M. Swidan, Ahmed B. Ibrahim, and Marianne J. Naguib
Elsevier BV
Adli A. Selim, Tamer M. Sakr, and Basma M. Essa
Springer Science and Business Media LLC
Rana M. El-Masry, Basma M. Essa, Adli A. Selim, Soad Z. El-Emam, Khaled O. Mohamed, Tamer M. Sakr, Hanan H. Kadry, Azza T. Taher, and Sahar M. Abou-Seri
MDPI AG
A new series of 5-(4-chlorophenyl)-1,3,4-thiadiazole-based compounds featuring pyridinium (3), substituted piperazines (4a–g), benzyl piperidine (4i), and aryl aminothiazoles (5a–e) heterocycles were synthesized. Evaluation of the cytotoxicity potential of the new compounds against MCF-7 and HepG2 cancer cell lines indicated that compounds 4e and 4i displayed the highest activity toward the tested cancer cells. A selectivity study demonstrated the high selective cytotoxicity of 4e and 4i towards cancerous cells over normal mammalian Vero cells. Cell cycle analysis revealed that treatment with either compound 4e or 4i induced cell cycle arrest at the S and G2/M phases in HepG2 and MCF-7 cells, respectively. Moreover, the significant increase in the Bax/Bcl-2 ratio and caspase 9 levels in HepG2 and MCF-7 cells treated with either 4e or 4i indicated that their cytotoxic effect is attributed to the ability to induce apoptotic cell death. Finally, an in vivo radioactive tracing study of compound 4i proved its targeting ability to sarcoma cells in a tumor-bearing mice model.
Eman M. M. Ebrahem, Galal H. Sayed, Gehan N. A. Gad, Kurls E. Anwer, and Adli A. Selim
Springer Science and Business Media LLC
Abstract Background Hepatocellular carcinoma (HCC) is one of the most dangerous cancers in all the world. This study focused on prevention and therapy of hepatocellular carcinoma (HCC) using Moringa oleifera extract combined with vitamin C and selenium in a nanoplatform (MO/asc.-Se-NPs). Results Full characterization of MO/asc.-Se-NPs was performed by using different analytical techniques (TEM, DLS, zeta-sizer), and its antioxidant capacity was measured by DPPH assay. Biodistribution study was performed with the aid of radiolabeling technique using technetium-99m in normal albino mice. HCC was induced in Wister albino rats to evaluate the efficiency of MO/asc.-Se-NPs in the treatment of HCC. The biomarker analysis (ALT, AST and ALB) shows improvement in its values in prevention and treated groups by using MO/asc.-Se NP. The levels of inflammatory marker interleukin 6 (IL6 tissue homogenate) was improved by decreasing its values in these two groups also. Histology section of tissue liver showed alleviation in treated and prevention groups. Conclusions In conclusion, MO/asc.-Se-NPs can be used as a potential agent for prevention and treatment of HCC after further preclinical studies.
Mona A. Shewaiter, Adli A. Selim, Yasser M. Moustafa, Shadeed Gad, and Hassan M. Rashed
Elsevier BV
Safa A. Aljuhr, Gamal Abdelaziz, Adli A. Selim, Wafaa A. Zaghary, and Tamer M. Sakr
Elsevier BV
Basma M. Essa, Adli A. Selim, Galal H. Sayed, and Kurls E. Anwer
Elsevier BV
Adli A. Selim, M. A. Motaleb, and Hend A. Fayez
Springer Science and Business Media LLC
Hend Fayez and Adli Abdallah Selim
Informa UK Limited
Background zoledronate suppresses human sarcomas by blocking the formation of geranylgeranyl diphosphate (GGPP) via inhibiting GGPP synthase.Objectives Designing of new derivative of dronic acid (1-hydroxy-2-(4-nitro-1H-imidazol-1-yl)ethan-1,1-diyl)bis phosphonic acid), structurally related to zoledronate to be used for osteosarcoma therapy.Methods 1-hydroxy-2-(4-nitro-1H-imidazol-1-yl)ethan-1,1-diyl)bis(phosphonic acid) was synthesized in one pot reaction with a yield of 65 ± 4%. The synthesized nitro-zoledronate compound was successfully radiolabeled with 99mTc with a radiochemical purity of 92.05%. Docking accuracy and scoring reliability for the new nitro-zoledronate with human GGPPS using MOE software has been presented.Results and Conclusion The nitro-zoledronate successfully coupled with technetium-99m at high yield to investigate its in-vivo biodistribution which indicated highly selective uptake in the skeletal system and rapid clearance from soft tissues. The in-vitro cytotoxicity of the nitro-zoledronate was evaluated and potently inhibited the osteosarcoma cell line (MG-63) after 72 hours with an IC50 value of 10μM. To summarize, our data point to a promising candidate to improve osteosarcoma therapy.
Basma M. Essa, Adli A. Selim, O. A. El-Kawy, and Gamal Abdelaziz
Informa UK Limited
BACKGROUND
Nanomedicine offers great potential for scintigraphic diagnostic imaging with lower risk and higher quality compared to other traditional techniques.
OBJECTIVES
This work aimed to develop and evaluate gold nanoparticles combined with gallic acid (gallic-AuNPs) and [131I]iodocolchicine as a scintigraphic probe for inflammation.
METHODS
[131I]iodocolchicine-gallic-AuNPs were synthesized via chemical reduction method where gallic acid was used as reducing agent and [131I]iodocolchicine was used as stabilizing agent. Then a characteristic profile for the synthesized nano-platform was performed including size analysis, zeta potential, radiochemical yield and in-vivo biodistribution in inflammation bearing mice.
RESULTS AND CONCLUSION
This platform was successfully synthesized with good stability, appropriate particle size (10 nm diameter for AuNPs), and high radiochemical purity for [131I]iodocolchicine (96.79%). The in-vivo study indicated that [131I]iodocolchicine-gallic-AuNPs accumulated with a high target to non-target ratio in intravenous injection and high retention value in intra-inflammation injection in inflammation model. The obtained data supported the usefulness of the new platform ([131I]iodocolchicine-gallic-AuNPs) as a tracer for the detection and localization of inflammation.
Adli A. Selim, Basma M. Essa, Islam M. Abdelmonem, Mohamed A. Amin, and Mona O. Sarhan
Elsevier BV
Khellin was successfully extracted from Ammi visnaga fruits with a recovery percent of 96.15%. Next radio-iodination of Khellin was successfully achieved with a high yield. The biodistribution study of [131I]iodo-khellin in tumour bearing mice revealed that khellin preferentially localization at tumour tissue. Target prediction study for [131I]iodo-khellin revealed that PI3K and VEGFR are potential targets for iodo-khellin with good affinity. The results of this study potentiate [131I]iodo-khellin as a good theranostic agent for tumour imaging and therapy.
Hanan Gaber Abdulwahab, Marwa F. Harras, Nagwan Galal El Menofy, Amany M. Hegab, Basma M. Essa, Adli AbdAllah Selim, Tamer M. Sakr, and Heba S.A. El-Zahabi
Elsevier BV
Urease enzyme is a virulence factor that helps in colonization and maintenance of highly pathogenic bacteria in human. Hence, the inhibition of urease enzymes is well-established to be a promising approach for preventing deleterious effects of ureolytic bacterial infections. In this work, novel thiobarbiturate derivatives were synthesized and evaluated for their urease inhibitory activity. All tested compounds effectively inhibited the activity of urease enzyme. Compounds 1, 2a, 2b, 4 and 9 displayed remarkable anti-urease activity (IC50 = 8.21-16.95 μM) superior to that of thiourea reference standard (IC50 = 20.04 μM). Moreover, compounds 3a, 3g, 5 and 8 were equipotent to thiourea. Among the tested compounds, morpholine derivative 4 (IC50 = 8.21 µM) was the most potent one, showing 2.5 folds the activity of thiourea. In addition, the antibacterial activity of the synthesized compounds was estimated against both standard strains and clinical isolates of urease producing bacteria. Compound 4 explored the highest potency exceeding that of cephalexin reference drug. Moreover, biodistribution study using radiolabeling approach revealed a remarked uptake of 99mTc-compound 4 into infection induced in mice. Furthermore, a molecular docking analysis revealed proper orientation of title compounds into the urease active site rationalizing their potent anti-urease activity.
Hend Fayez, Mohamed Abd El-Motaleb, and Adli Abdullah Selim
Wiley
The combined action of shikonin and silver nanoparticles (AgNPs) for apoptosis in human cancer cells has not been elucidated. Hence, we investigated the synergistic combinatorial effect of shikonin and AgNPs in human lung cancer cells. Shikonin was used as a reducing and capping agent for AgNPs synthesis as a green method avoiding the hazards of chemical methods. Radiolabeling of Shikonin-AgNPs with radioactive iodine forming [131 I]I-Shikonin-AgNPs was carried out to enable the intracellular tracking of nanoparticles. The antitumor effect of a combined treatment (shikonin-AgNPs) was evaluated using tissue culture assay. The 50% inhibitory concentration (IC50 ) of SHK-AgNPs on A549 cells after 24h determined by an MTT assay is 2.4 ± 0.11μg/mL. As a deduction this study revealed that the combination of shikonin and AgNPs treatment significantly inhibited cell viability and proliferation of A549 cells (human lung carcinoma cell line) with a great potential than the monotherapy.
G. Abdelaziz, M. M.A., N. Farouk and A. A. Selim
Egypts Presidential Specialized Council for Education and Scientific Research
The aim of this study was to synthesis an imaging agent for tumor targeting. New recombinant insulin analogue was successfully produced from E. coli by recombinant DNA technique, and was well labeled with Technetium-99m with a high radiochemical yield of 93.3 ± 2.1 %. Moreover, it showed good in-vitro stability in both saline and human serum. Preclinical evaluation of Technetium-99m [ 99m Tc] Tc-insulin in solid tumor-bearing mice showed high accumulation in tumor tissues. The T/NT (target to non-target ratio) was of 5.4, after 60 min. of post injection (p.i). The direct intra-tumoral (I.T) injection of [ 99m Tc] Tc-insulin showed good retention in tumor tissues with a ratio more than 50 % after 15 min. As a result of the promising bio-distribution studies; the newly recombinant insulin showed good uptake in tumor site, which assured high concentration of insulin receptor on tumor cell surface, accompanied with high cell density of tumor cells as well. This work affords a potential radio-carrier that could be used as a good tumor marker and imaging probe via SPECT (Single Photon Emission Computed Tomography) technique, after further preclinical studies.
Mohamed A. Motaleb and Adli A. Selim
Elsevier BV
The selective properties of dioxime compounds were discovered and outlined in the beginning of 20th century by Tschugaeff [L.Z. Tschugaeff, Z. Anorg. Allgem. Chem. 46 (1905) 144]. Dioximes have special properties as analytical reagents for transition metals. Dioximes complexation properties with metals were carried out by many investigations and these complexations showed a wide range of applications such as antimicrobial and theranostic agents. This review will provide general synthetic methods of oximes especially dioximes and brief overview on the applications of dioximes (applications of their metal complexes).
M. A. Motaleb, Adli A. Selim, M. El-Tawoosy, M. H. Sanad, and M. A. El-Hashash
Informa UK Limited
Abstract Purpose: Dioxime derivative is reported to exhibit high affinity towards tumor cells. The objective of the present study is to synthesize a new dioxime derivative to be labeled with technetium-99m for using as a solid tumor marker. Materials and methods: ((2E,2′,3E,3′)-3,3′-(cyclohexane-1,2-diylbis (azanylylidene)) bis-(butan-2-one)dioxime) was synthesized by condensation of Butan-2,3-dione monooxime and diaminocyclohexane and labeled with 99mTc. The in-vivo distribution of the agent was studied by carrying out biodistribution in tumor bearing Albino mice. Results: A new cyclohexane dioxime derivative was synthesized with a good yield of 93 ± 2% and its complexation with 99mTc was prepared with 85 ± 4% radiochemical yield under the optimized conditions and the preparation exhibited in-vitro stability up to 6 h. Biodistribution studies showed high uptake in tumor cells with T/NT (target to non-target ratio) = 3.4 ± 0.2 after 0.5 h post injection. Conclusion: As a result of biodistribution studies, the newly synthesized cyclohexane dioxime derivative showed its good uptake in tumor cells, which affords a potential radiopharmaceutical that could be used as a good tumor imaging agent.
M. A. Motaleb, M. H. Sanad, A. A. Selim, M. El-Tawoosy, and M. Abd-Allah
Pleiades Publishing Ltd
Abstract1-Hydroxy-2-(2-pyridyl)ethanedisphosphonic acid monosodium salt (HPEDP) was prepared and labeled with 99mTc using two different reducing agents: SnCl2·2H2O and NaBH4; NaBH4 gave better results. The radiochemical purity of 99mTc(NaBH4)-HPEDP was 96 ± 4%, and the complex was stable in vitro for 6 h. The in vivo biodistribution studies performed in mice show highly selective uptake of the labeled compound in the skeletal system and rapid elimination via the urinary pathway. The maximum bone uptake was 32.3 ± 2.1% ID/organ.
M. A. Motaleb, Adli A. Selim, M. El-Tawoosy, M. H. Sanad, and M. A. El-Hashash
Springer Science and Business Media LLC
A novel dioxime derivative (2E,2′E,3E,3′E)-3,3′-(pyrimidine-4,5-diylbis(azanylylidene))bis(butan-2-one)dioxime was synthesized with a yield of 65%. IR, elemental analysis, mass spectroscopy and 1H-NMR were used to characterize the structure of the synthesized compound. 99mTc-dioxime was radio-synthesized with a high radiochemical yield of 97.8 ± 0.5% and in vitro stability of 6 h under the optimum conditions. The preclinical evaluation of 99mTc-dioxime in solid tumor-bearing mice showed high accumulation in solid tumor cells with a high Target/Non-Target ratio of 5.14 at 30 min post-injection. This study suggests that 99mTc-dioxime derivative is a promising candidate as a new 99mTc-based tumor-imaging agent after further preclinical studies.
Reem Ibrahim Al-Wabli, Tamer Mostafa Mohamed Hafez Sakr, Mohammed Abdou Khedr, Adly Abdallah Selim, Mohamed Abd El-Motaleb Abd El-Rahman, and Wafaa Abdou Zaghary
Springer Science and Business Media LLC
BackgroundOne of the most popular techniques for cancer detection is the nuclear medicine technique. The present research focuses on Platelet-12-lipoxygenase (P-12-LOX) as a promising target for treating and radio-imaging tumor tissues. Curcumin was reported to inhibit this enzyme via binding to its active site.ResultsA novel curcumin derivative was successfully synthesized and characterized with yield of 74%. It was radiolabeled with the diagnostic radioisotope technetium-99m with 84% radiochemical yield and in vitro stability up to 6 h. The biodistribution studies in tumor bearing mice confirmed the high affinity predicted by the docking results with a free binding energy value of (ΔG −50.10 kcal/mol) and affinity (13.64 pki) showing high accumulation in solid tumor with target/non-target ratio >6.ConclusionThe newly synthesized curcumin derivative, as a result of a computational study on platelet-12 lipoxygenase, showed its excellent free binding energy (∆G −50.10 kcal/mol) and high affinity (13.64 pKi). It could be an excellent radio-imaging agent that targeting tumor cells via targeting of P-12-LOX.Graphical abstractThis novel curcumin derivative was successfully synthesized and radiolabeled with technetium-99m and biologically evaluated in tumor bearing mice that showed high accumulation in solid tumor with target/non-target ratio >6 confirming the affinity predicted by the docking results. Predicted binding mode of a new curcumin derivative in complex with 12-LOX active site. b Curcumin itself in the 12-LOX active site biological distribution of 99mTc-curcumin derivative complex in solid tumor bearing Albino mice
M. A. Motaleb, A. S. A. Adli, M. El-Tawoosy, M. H. Sanad, and M. AbdAllah
Wiley
This study aimed to provide an easy method for synthesis of 1-hydroxy-2-(3-pyridyl) ethylidene bisphosphonic acid monosodium (sod. risedronate) with a high yield of 71%. The synthesized risedronate was labeled with technetium-99 m using two different reducing agents (SnCl2 .2H2 O and NaBH4 ) where NaBH4 gave stable complex and higher radiochemical yield more than SnCl2 .2H2 O. The results showed that, the radiochemical purity of (99m) Tc(NaBH4 )-risedronate was 99.2 ± 0.6% and its stability was up to 6 h. Biodistribution study showed high uptake and long retention of (99m) Tc(NaBH4 )-risedronate in bone starting from 15 min (29 ± 2.5% ID/organ) up to 4 h (35.1 ± 3.2 ID/organ) post injection. This research could introduce an easy and effective method for synthesis and labeling of risedrionate and affording a good tracer for bone imaging.