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1.
Int J Biomater ; 2024: 5556838, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38725434

RESUMO

Cancer and bacterial infections are major global health concerns driving the need for innovative medicines. This study investigated alginate nanoparticles loaded with essential oils (EOs) from Cuminum cyminum and Zataria multiflora as potential drug delivery systems. The nanoparticles were comprehensively characterized using techniques such as gas chromatography-mass spectrometry (GC-MS), dynamic light scattering (DLS), zetasizer, attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), and ultraviolet-visible spectroscopy (UV-Vis). Their biological properties against two human skin cancer cell lines (A-375 and A-431) and three bacteria (Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus) were also evaluated. Alginate nanoparticles containing C. cyminum and Z. multiflora EOs exhibited sizes of 160 ± 8 nm and 151 ± 10 nm, respectively. Their zeta potentials and encapsulation efficiencies were -18 ± 1 mV and 79 ± 4%, as well as -27 ± 2 mV and 86 ± 5%, respectively. The IC50 values against the tested cell lines and bacteria revealed superior efficacy for nanoparticles containing Z. multiflora EO. Considering the proper efficacy of the proposed nanoparticles, the straightforward preparation method and low cost suggest their potential for further in vivo studies.

2.
BMC Complement Med Ther ; 24(1): 138, 2024 Apr 02.
Artigo em Inglês | MEDLINE | ID: mdl-38566054

RESUMO

Herbal components are highly useful assets for the advancement of novel antibacterial drugs. Nanotechnology holds great promise as an approach to enhance the effectiveness and develop the composition of these substances. The study developed nanogels incorporating camphor, thymol, and a combination derived from the initial nanoemulsions with particle sizes of 103, 85, and 135 nm, respectively. The viscosity of nanogels and the successful loading of compounds in them were examined by viscometery and ATR-FTIR studies. The bactericidal properties of the nanogels were examined against four bacterial strains. The nanogel containing camphor and thymol at 1250 µg/mL concentration exhibited complete growth suppression against Pseudomonas aeruginosa and Staphylococcus aureus. The thymol nanogel at 1250 µg/mL and the camphor nanogel at 2500 µg/mL exhibited complete inhibition of growth on Listeria monocytogenes and Escherichia coli, respectively. Both nanogels showed favorable effectiveness as antibacterial agents and could potentially examine a wide range of pathogens and in vivo studies.


Assuntos
Cânfora , Polietilenoglicóis , Polietilenoimina , Timol , Timol/farmacologia , Nanogéis , Cânfora/farmacologia , Antibacterianos/farmacologia , Escherichia coli
3.
Int J Clin Pract ; 2024: 1016247, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38239768

RESUMO

Burn injuries are considered an important public health problem in the world. Burns are considered the fourth most common kind of trauma in the world, after traffic accidents, falls, and interpersonal violence. Various biochemical agents are involved in the burn healing process such as cytokines (such as IL-6 and TNF-α), antioxidants, and liver and kidney damage biomarkers. Cichorium intybus L. and milk thistle extracts showed a wide range of pharmacological activities such as significant antimicrobial effect and antioxidant activity, as well as anti-inflammatory, antidiabetic, antiproliferative, antiprotozoal, and hepatoprotective effect. Also, these two herbs possess blood-cleansing, detoxifying, laxative, and invigorating activities. Some research confirmed that the preparations of the extract are very suitable for the treatment of nonalcoholic fatty liver disease. This is a double-blind randomized controlled clinical trial. Patients with 2nd and 3rd degree burns have been selected to participate in the study according to the inclusion criteria. A total of 60 patients were selected and divided into intervention and control groups (30 patients in each group). Patients in the intervention group received chicory seed syrup 10 cc three times a day and 1 placebo capsule, and those in the control group received placebo syrup (10 cc three times a day) and one Livergol (140 mg of silymarin in each capsule) capsule. Lab data such as liver function tests, albumin, creatinine, BUN, and hemoglobin were checked every 3 days and 1 week after discharge. The treatment lasted for 4 weeks. According to the results of the study, although the average of liver enzymes at the end of the study does not show a significant difference between the two groups, the level of liver enzymes in each group decreased on the 15th day of the study compared to the first day. This trial is registered with IRCT20180609040016N1.


Assuntos
Queimaduras , Cichorium intybus , Hepatopatia Gordurosa não Alcoólica , Humanos , Antioxidantes , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Queimaduras/tratamento farmacológico , Método Duplo-Cego
4.
Front Genet ; 14: 1297093, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-38094755

RESUMO

Colorectal cancer (CRC) is one of the main fatal cancers. Cell signaling such as Janus kinase/signal transducer and activator of transcription (JAK/STAT) signaling substantially influences the process of gene expression and cell growth. Long non-coding RNAs (lncRNAs) play regulatory roles in cell signaling, cell proliferation, and cancer fate. Hence, lncRNAs can be considered biomarkers in cancers. The inhibitory or activating effects of different lncRNAs on the JAK/STAT pathway regulate cancer cell proliferation or tumor suppression. Additionally, lncRNAs regulate immune responses which play a role in immunotherapy. Mechanisms of lncRNAs in CRC via JAK/STAT regulation mainly include cell proliferation, invasion, metastasis, apoptosis, adhesion, and control of inflammation. More profound findings are warranted to specifically target the lncRNAs in terms of activation or suppression in hindering CRC cell proliferation. Here, to understand the lncRNA cross-talk in CRC through the JAK/STAT signaling pathway, we collected the related in vitro and in vivo data. Future insights may pave the way for the development of novel diagnostic tools, therapeutic interventions, and personalized treatment strategies for CRC patients.

5.
BMC Complement Med Ther ; 23(1): 435, 2023 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-38041055

RESUMO

BACKGROUND: Using nanoparticles containing L. citriodora EO and citral has shown potential in treating skin disorders such as melanoma. METHODS: In this study, GC‒MS was used to analyze the chemical composition of L. citriodora essential oil (EO). The ion gelation method prepared free chitosan nanoparticles and chitosan nanoparticles containing L. citriodora EO and citral. The successful loading of the EO and citral was evaluated using ATR-FTIR. The DPPH assay measured the antioxidant effect of citral, L. citriodora EO, Citral-ChiNPs, L. citriodora-ChiNPs, and Free-ChiNPs. A375 melanoma cell viability was assessed using the MTT assay. The qPCR technique was employed to evaluate the expression of apoptotic genes, and flow cytometry was used to detect apoptosis. RESULTS: This study showed that in equal concentrations, the antioxidant properties of chitosan nanoparticles containing citral were greater than those of chitosan nanoparticles containing L. citriodora. The IC50 values of chitosan nanoparticles containing citral, L. citriodora EO, and their nonformulated states were 105.6, 199.9, 136.9, and 240 µg/ml, respectively. The gene expression results showed that the ratio of the expression of the apoptosis gene to the inhibitory gene was higher than 1 in all the samples, indicating that the conditions for apoptosis were present. Flow cytometry confirmed cell apoptosis, with 93.5 ± 0.3% in chitosan nanoparticles containing citral, 80 ± 0.2% in chitosan nanoparticles containing L. citriodora EO, 63 ± 0.3 in citral, and 42.03% in L. citriodora EO-treated cells. CONCLUSION: The results showed that using the Nano form of L. citriodora and citral increased their efficiency in apoptosis pathways and their toxicity against 375 melanoma cancer cells.


Assuntos
Quitosana , Lippia , Melanoma , Nanopartículas , Óleos Voláteis , Humanos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Quitosana/farmacologia , Apoptose , Melanoma/tratamento farmacológico
6.
BMC Complement Med Ther ; 23(1): 428, 2023 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-38017466

RESUMO

BACKGROUND: Breast cancer is the most common cancer among women, and melanoma is the most dreadful type of skin cancer. Due to the side effects of chemotherapy drugs, the development of new herbal nano-medicines has been considered. METHODS: This study first investigated the chemical composition of Ferula gummosa essential oil using GC-MS analysis; ß-pinene, with 61.57%, was the major compound. Next, alginate nanoparticles containing ß-pinene and the essential oil with particle sizes of 174 ± 7 and 137 ± 6 nm were prepared. Meanwhile, their zeta potentials were 12.4 ± 0.7 and 28.1 ± 1 mV. Besides, the successful loading of ß-pinene and the essential oil in nanoparticles was confirmed using ATR-FTIR analysis. After that, their effects on viability and apoptotic index of human melanoma and breast cancer cells were investigated in normoxia and normobaric hyperoxia (NBO) conditions. RESULTS: The best efficacy on A-375 and MDA-MB-231 cells was achieved by alginate nanoparticles containing the EO at hyperoxic and normoxia conditions; IC50 76 and 104 µg/mL. Besides, it affected apoptosis-involved genes; as Bax/Bcl-2 ratio was higher than 1, conditions for induction of apoptosis were obtained. Higher sensitivity was observed in the A-375 cell line treated with Alg-EO in the NBO model. CONCLUSIONS: Alginate nanoparticles containing F. gummosa EO could be considered for further investigation in anticancer studies. Also, it may be expected that NBO can be a new strategy for delaying cancer progression and improving nanotherapy efficacy.


Assuntos
Neoplasias da Mama , Ferula , Hiperóxia , Melanoma , Óleos Voláteis , Humanos , Feminino , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Ferula/química , Alginatos , Neoplasias da Mama/tratamento farmacológico , Melanoma/tratamento farmacológico , Proliferação de Células
7.
BMC Res Notes ; 16(1): 261, 2023 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-37814316

RESUMO

OBJECTIVE: Malaria is a vector-borne disease that causes many deaths worldwide; repellents are a practical approach to malaria prevention, especially in endemic regions. RESULTS: Gas chromatography-mass spectrometry analysis was used to identify compounds in Acroptilon repens essential oil (EO). Alpha-copaene (15.67%), α-cubenen (3.76%), caryophyllene oxide (14.00%), 1-heptadecane (5.61%), and δ-cadinene (2.84) were five major compounds. After that, the nanoemulsion containing the EO with a particle size of 46 ± 4 nm, SPAN 0.85, PDI 0.4, and zeta potential - 5.7 ± 0.4 mV was prepared. Then, it was gellified by adding CMC (carboxymethyl cellulose) to the nanoemulsion. Besides, ATR-FTIR analysis (Attenuated Total Reflection-Fourier Transform InfraRed) was used to confirm the EO's successful loading in the nanogel. Finally, the protection time and repellent activity of nanogel compared to DEET (N, N-diethyl-meta-toluamide) were investigated against Anopheles stephensi. Interestingly, the nanogel with a protection time of 310 ± 45 min was significantly more potent than DEET (160 ± 17 min). It could thus be considered for future investigation against other mosquitoes.


Assuntos
Anopheles , Repelentes de Insetos , Malária , Óleos Voláteis , Animais , Humanos , DEET , Óleos Voláteis/farmacologia , Nanogéis , Mosquitos Vetores , Repelentes de Insetos/farmacologia , Malária/prevenção & controle
8.
J Funct Biomater ; 14(9)2023 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-37754867

RESUMO

The gastrointestinal tract (GIT) environment has an intricate and complex nature, limiting drugs' stability, oral bioavailability, and adsorption. Additionally, due to the drugs' toxicity and side effects, renders are continuously seeking novel delivery systems. Lipid-based drug delivery vesicles have shown various loading capacities and high stability levels within the GIT. Indeed, most vesicular platforms fail to efficiently deliver drugs toward this route. Notably, the stability of vesicular constructs is different based on the different ingredients added. A low GIT stability of liposomes and niosomes and a low loading capacity of exosomes in drug delivery have been described in the literature. Bilosomes are nonionic, amphiphilic, flexible surfactant vehicles that contain bile salts for the improvement of drug and vaccine delivery. The bilosomes' stability and plasticity in the GIT facilitate the efficient carriage of drugs (such as antimicrobial, antiparasitic, and antifungal drugs), vaccines, and bioactive compounds to treat infectious agents. Considering the intricate and harsh nature of the GIT, bilosomal formulations of oral substances have a remarkably enhanced delivery efficiency, overcoming these conditions. This review aimed to evaluate the potential of bilosomes as drug delivery platforms for antimicrobial, antiviral, antifungal, and antiparasitic GIT-associated drugs and vaccines.

9.
RSC Adv ; 13(35): 24656-24673, 2023 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-37601597

RESUMO

In this paper, we have assessed the design, synthesis, characterization, anticancer properties, toxicity, and in silico study of 8-piperazinyl caffeinyl-triazolylmethyl derivatives as new caffeine hybrid conjugates. These compounds consist of four moieties comprising 8-caffeinyl, piperazinyl, 1,2,3-triazolyl, and alkyl substituents. The synthesis of these compounds was started by bromination of caffeine to attain 8-BC, SNAr reaction with piperazine to acquire 8-PC, N-propargylation of 8-PC and finally click Huisgen cycloaddition with diverse alkyl azides. These compounds were in vitro tested against two significant cancer cell lines comprising breast cancer MCF-7 (ATCC HTB-22) and melanoma cancer A-375 (ATCC CRL-1619) cell lines and activities compared with methotrexate (MTX) as a reference drug. Anticancer assessments indicated 12j (IC50 = 323 ± 2.6) and 12k (IC50 = 175 ± 3.2) were the most potent compounds against A-375 and MCF-7 cell growth, respectively and their activities were even stronger than MTX (IC50 = 418 ± 2 for A375 and IC50 = 343 ± 3.6 for MCF-7). Toxicities were determined by screening compounds against normal cell line HEK-293 (ATCC CRL-11268) and indicated that except 12i (IC50 = 371 ± 2.3), 12j (IC50 = 418 ± 2.4), and MTX (IC50 = 199 ± 2.4), all compounds are non-toxic. Docking was conducted for 12j and 12k and determined the strong binding affinities to B-RAF kinase and hDHFR enzymes, respectively. In silico pharmacokinetic and physiochemical profiles of tested compounds were investigated which indicated that most compounds obeyed Lipinski's rule of five (RO5). The DFT study on M06-2X/6-311G (d,p) was used to indicate HOMO, LUMO, MEP, and other parameters for a better understanding of 12j and 12k reactivity. Owing to anticancer properties, toxicity, and in silico data, 12j and 12k can be proposed for further research in the future.

10.
Sci Rep ; 13(1): 11002, 2023 07 07.
Artigo em Inglês | MEDLINE | ID: mdl-37420038

RESUMO

Aedes aegypti and Anopheles stephensi have challenged human health by transmitting several infectious disease agents, such as malaria, dengue fever, and yellow fever. Larvicides, especially in endemic regions, is an effective approach to the control of mosquito-borne diseases. In this study, the composition of three essential oil from the Artemisia L. family was analyzed by Gas Chromatography-Mass Spectrometry. Afterward, nanoliposomes containing essential oils of A. annua, A. dracunculus, and A. sieberi with particle sizes of 137 ± 5, 151 ± 6, and 92 ± 5 nm were prepared. Besides, their zeta potential values were obtained at 32 ± 0.5, 32 ± 0.6, and 43 ± 1.7 mV. ATR-FTIR analysis (Attenuated Total Reflection-Fourier Transform InfraRed) confirmed the successful loading of the essential oils. Moreover, The LC50 values of nanoliposomes against Ae. aegypti larvae were 34, 151, and 197 µg/mL. These values for An.stephensi were obtained as 23 and 90, and 140 µg/mL, respectively. The results revealed that nanoliposomes containing A. dracunculus exerted the highest potential larvicidal effect against Ae. aegypti and An. stephensi, which can be considered against other mosquitoes.


Assuntos
Aedes , Anopheles , Artemisia , Culex , Inseticidas , Óleos Voláteis , Animais , Humanos , Óleos Voláteis/farmacologia , Óleos Voláteis/análise , Larva , Inseticidas/química , Folhas de Planta/química , Extratos Vegetais/química
11.
Food Sci Nutr ; 11(6): 2823-2837, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37324854

RESUMO

Retardation of quality loss of seafood has been a new concept in recent years. This study's main objective was to evaluate the microbial, chemical, and sensory attributes of shrimp coated with alginate sodium nanoparticles containing Zataria multiflora and Cuminum cyminum essential oils (EOs) during refrigerated storage. At the end of storage time (15 days storage at 4°C), the pH, thiobarbituric acid reactive substances (TBARS), and total volatile basic nitrogen (TVBN) amounts in shrimps coated with the alginate nanoparticles were 7.62, 1.14 mg MDA/kg, and 117 mg/100 g which were significantly (p < .05) lower than the control groups. The count of all bacteria groups was also lower in this treatment, which was 2-2.74 Log CFU/mL on day 15 of cold storage. This combined treatment also obtained the highest sensory scores (around 7) and the lowest melanosis score (2.67) due to the effective delaying microbial and oxidation activities. Therefore, this edible coating could substantially retard microbial and chemical changes and improve the organoleptic properties of shrimp under refrigerated storage.

12.
Biomedicines ; 11(5)2023 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-37238916

RESUMO

Owing to drawbacks in the current common cancer therapies including surgery, chemotherapy and radiotherapy, the development of more reliable, low toxic, cost-effective and specific approaches such as immunotherapy is crucial. Breast cancer is among the leading causes of morbidity and mortality with a developed anticancer resistance. Accordingly, we attempted to uncover the efficacy of metallic nanoparticles (MNPs)-based breast cancer immunotherapy emphasizing trained immunity provocation or innate immunity adaptation. Due to the immunosuppressive nature of the tumor microenvironment (TME) and the poor infiltration of immune cells, the potentiation of an immune response or direct combat is a goal employing NPs as a burgeoning field. During the recent decades, the adaptation of the innate immunity responses against infectious diseases and cancer has been recognized. Although the data is in a scarcity with regard to a trained immunity function in breast cancer cells' elimination, this study introduced the potential of this arm of immunity adaptation using MNPs.

13.
Arch Microbiol ; 205(6): 252, 2023 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-37249707

RESUMO

Inflammatory bowel disease (IBD) is a chronic recurrent inflammation of the gastrointestinal tract (GIT). IBD patients are susceptible to various infections such as viral infections due to the long-term consumption of immunosuppressive drugs and biologics. The antiviral and IBD protective traits of flavonoids have not been entirely investigated. This study objective included an overview of the protective role of flavonoids quercetin and silymarin in viral-associated IBD. Several viral agents such as cytomegalovirus (CMV), Epstein-Barr virus (EBV), varicella zoster virus (VZV) and enteric viruses can be reactivated and thus develop or exacerbate the IBD conditions or eventually facilitate the disease remission. Flavonoids such as quercetin and silymarin are non-toxic and safe bioactive compounds with remarkable anti-oxidant, anti-inflammatory and anti-viral effects. Mechanisms of anti-inflammatory and antiviral effects of silymarin and quercetin mainly include immune modulation and inhibition of caspase enzymes, viral binding and replication, RNA synthesis, viral proteases and viral assembly. In the nutraceutical sector, natural flavonoids low bioavailability and solubility necessitate the application of delivery systems to enhance their efficacy. This review study provided an updated understanding of the protective role of quercetin and silymarin against viral-associated IBD.


Assuntos
Infecções por Vírus Epstein-Barr , Doenças Inflamatórias Intestinais , Silimarina , Humanos , Herpesvirus Humano 4/genética , Quercetina/farmacologia , Silimarina/farmacologia , Flavonoides , Doenças Inflamatórias Intestinais/tratamento farmacológico , Antivirais/farmacologia , Antivirais/uso terapêutico
14.
Virus Genes ; 59(4): 635-642, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37259013

RESUMO

Diabetic foot ulcer (DFU) is associated with long-term hospitalization and amputation. Antibiotic resistance has made the infection eradication more difficult. Hence, seeking alternative therapies such as phage therapy seems necessary. Bacteriophages are viruses targeting specific bacterial species. Klebsiella pneumoniae (K. pneumoniae) is among causative agents of the DFU. In this study, the therapeutic effects of single phage and phage cocktail were investigated against multidrug-resistant (MDR) K. pneumonia isolated from DFU. Bacteriophages were isolated from animal feces and sewage samples, and were enriched and propagated using K. pneumoniae as the host. Thirty K. pneumoniae clinical isolates were collected from hospitalized patients with DFU. The antibiotic susceptibility pattern was determined using agar disk diffusion test. The phages' morphological traits were determined using transmission electron microscopy (TEM). The killing effect of isolated phages was assessed using plaque assay. Four phage types were isolated and recognized including KP1, KP2, KP3, and KP4. The bacterial rapid regrowth was observed following each single phage-host interaction, but not phage cocktail due to the evolution of mutant strains. Phage cocktail demonstrated significantly higher antibacterial activity than each single phage (p < 0.05) without any bacterial regrowth. The employment of phage cocktail was promising for the eradication of MDR-K. pneumoniae isolates. The development of phage therapy in particular, phage cocktail is promising as an efficient approach to eradicate MDR-K. pneumoniae isolated from DFU. The application of a specific phage cocktail can be investigated to try and achieve the eradication of various infections.


Assuntos
Bacteriófagos , Diabetes Mellitus , Pé Diabético , Terapia por Fagos , Animais , Bacteriófagos/genética , Klebsiella pneumoniae , Pé Diabético/terapia , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico
15.
RSC Adv ; 13(5): 3056-3070, 2023 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-36756447

RESUMO

In this research the synthesis, characterization, anticancer and the cytotoxicity assessments of novel 8-caffeinyl-triazolylmethoxy hybrid conjugates have been described. These compounds are the first caffeine-1,2,3-triazolyl hybrid molecules that structurally are composed of three compartments comprising caffeinyl, 1,2,3-triazolyl and N-alkyl/aryl residues. The in vitro evaluations of synthesized compounds on cancer cell lines, including two breast cancer cell lines MDA-MB-468 (ATCC HTB-22), MCF-7 (ATCC HTB-22), melanoma cell line A-375 (ATCC CRL-1619) and normal cell line HEK-293 (ATCC CRL-11268) have determined that 22c (IC50 < 12.5 µM) demonstrated potent activity against A375 and its toxicity is even stronger than methotrexate (MTX) as a standard drug. Additionally, 22c involves more selectivity than MTX regarding its non-toxicity for the HEK-293 cell line. Among the tested compounds against two breast cancer cell lines, 22f (IC50 = 136 ± 0.2 and 126 ± 0.6 µM for MCF-7 and MDA-MB-468, respectively) and 22i (IC50 = 165 ± 1.8 and 175 ± 1.4 µM for MCF-7 and MDA-MB-468, respectively) were the most potent compounds but their activities were less than MTX, moreover 22f showed more selectivity regarding its lower toxicity against HEK-293. Overall, 22f displayed general toxicity and selectivity on all tested cancer cell lines. The in silico physicochemical properties, pharmacokinetic profile, and drug likeness predictions were also carried out for all the studied compounds. Most new compounds exhibited zero violation of Lipinski's rule (RO5). A molecular docking study was also conducted to predict the binding mode and the interaction of 22c as the most active anti-melanoma entry with B-RAF V600E kinase enzyme. The docking results determined that 22c exhibited a strong binding affinity to the active site of the enzyme. These findings demonstrated 22c and 22f as potential future anticancer drug candidates.

16.
Sci Rep ; 13(1): 2578, 2023 02 13.
Artigo em Inglês | MEDLINE | ID: mdl-36782003

RESUMO

In the present study, a series of aryl-substituted thioqunoline conjugated to thiosemicarbazide were rationally designed and synthesized. The formation of target compounds was confirmed by spectral characterization techniques such as IR, 1H-NMR, 13C-NMR, ESI-MS, and elemental analysis. Among the synthesized derivatives, compound 10g bearing para-chlorophenyl moiety was proved to be the most potent tyrosinase inhibitor with an IC50 value of 25.75 ± 0.19 µM. Compound 10g as the most potent derivative exhibited a noncompetitive inhibition pattern against tyrosinase in the kinetic study. Furthermore, the in silico cavity detection, as well as the molecular docking assessments, were performed to follow the behavior of 10g within the proposed binding site. Besides, the toxicity of 10g and its potency to reduce the melanin content on A375 cell lines were also measured. Consequently, aryl-substituted thioqunolines conjugated to thiosemicarbazide might be a promising candidate in the cosmetics, medicine, and food industry as tyrosinase inhibitors.


Assuntos
Agaricales , Inibidores Enzimáticos , Monofenol Mono-Oxigenase , Agaricales/metabolismo , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/química , Melaninas , Simulação de Acoplamento Molecular , Estrutura Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Relação Estrutura-Atividade
17.
J Trop Med ; 2023: 5075581, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36793773

RESUMO

Cuminum cyminum L. is a widespread medicinal plant with a broad spectrum of biological activity. In the present study, the chemical structure of its essential oil was examined utilizing GC-MS analysis (gas chromatography-mass spectrometry). Then, a nanoemulsion dosage form was prepared with a droplet size and droplet size distribution (SPAN) of 121 ± 3 nm and 0.96. After that, the dosage form of the nanogel was prepared; the nanoemulsion was gelified by the addition of 3.0% carboxymethyl cellulose. In addition, the successful loading of the essential oil into the nanoemulsion and nanogel was approved by ATR-FTIR (attenuated total reflection Fourier transform infrared) analysis. The IC50 values (half maximum inhibitory concentration) of the nanoemulsion and nanogel against A-375 human melanoma cells were 369.6 (497-335) and 127.2 (77-210) µg/mL. In addition, they indicated some degrees of an antioxidant activity. Interestingly, after treatment of Pseudomonas aeruginosa with 5000 µg/mL nanogel, bacterial growth was completely (∼100%) inhibited. In addition, the growth of Staphylococcus aureus after treatment with the 5000 µg/ml nanoemulsion was decreased by 80%. In addition, nanoemulsion and nanogel LC50 values for Anopheles stephensi larvae were attained as 43.91 (31-62) and 123.9 (111-137) µg/mL. Given the natural ingredients and promising efficacy, these nanodrugs can be regarded for further research against other pathogens or mosquito larvae.

18.
BMC Complement Med Ther ; 23(1): 6, 2023 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-36624422

RESUMO

BACKGROUND: Topical drug delivery using nanoemulsions and nanogels is a promising approach to treating skin disorders such as melanoma. METHODS: In this study, the chemical composition of Mentha pulegium essential oil with five major compounds, including pulegone (68.11%), l-menthone (8.83%), limonene (2.90%), iso-pulegone (2.69%), and iso-menthone (1.48%) was first identified using GC-MS (Gas chromatography-Mass Spectrometry) analysis. Afterward, a nano-scaled emulsion containing the essential oil with a droplet size of 7.70 ± 1 nm was prepared. Nanogel containing the essential oil was then prepared by adding (2% w/v) carboxymethyl cellulose to the nano-scaled emulsion. Moreover, the successful loading of M. pulegium essential oil in the nano-scaled emulsion and nanogel was confirmed using ATR-FTIR (Attenuated total reflectance-Fourier Transform InfraRed) analysis. Then, human A375 melanoma cells were treated with different concentrations of samples, the MTT assay evaluated cell viability, and cell apoptosis was confirmed by flow cytometry. In addition, the expression of apoptotic and anti-apoptotic genes, including Bax and Bcl-2, was evaluated using the qPCR (quantitative Polymerase Chain Reaction) technique. RESULTS: The results showed that cell viability was reduced by 90 and 45% after treatment with 300 µg/mL of the nanogel and nano-scaled emulsion. As confirmed by flow cytometry, this effect was mediated by apoptosis. Furthermore, gene expression analysis showed up-regulation of Bax and down-regulation of Bcl-2 genes. Therefore, the prepared nanogel, with high efficacy, could be considered a potent anticancer agent for supplementary medicine and in vivo research.


Assuntos
Melanoma , Mentha pulegium , Óleos Voláteis , Humanos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Mentha pulegium/química , Nanogéis , Emulsões , Proteína X Associada a bcl-2 , Genes Reguladores , Melanoma/tratamento farmacológico , Apoptose
19.
Biomed Res Int ; 2022: 2346941, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36420097

RESUMO

Skin cancer is one of leading cancers globally, divided into two major categories including melanoma and nonmelanoma. Skin cancer is a global concern with an increasing trend, hence novel therapies are essential. The local treatment strategies play a key role in skin cancer therapy. Nanoparticles (NPs) exert potential applications in medicine with huge advantages and have the ability to overcome common chemotherapy problems. Recently, NPs have been used in nanomedicine as promising drug delivery systems. They can enhance the solubility of poorly water-soluble drugs, improve pharmacokinetic properties, modify bioavailability, and reduce drug metabolism. The high-efficient, nontoxic, low-cost, and specific cancer therapy is a promising goal, which can be achieved by the development of nanotechnology. Metallic NPs (MNPs) can act as important platforms. MNPs development seeks to enhance the therapeutic efficiency of medicines through site specificity, prevention of multidrug resistance, and effective delivery of therapeutic factors. MNPs are used as potential arms in the case of cancer recognition, such as Magnetic Resonance Imaging (MRI) and colloidal mediators for magnetic hyperthermia of cancer. The applications of MNPs in the cancer treatment studies are mostly due to their potential to carry a large dose of drug, resulting in a high concentration of anticancer drugs at the target site. Therefore, off-target toxicity and suffering side effects caused by high concentration of the drug in other parts of the body are avoided. MNPs have been applied as drug carriers for the of improvement of skin cancer treatment and drug delivery. The development of MNPs improves the results of many cancer treatments. Different types of NPs, such as inorganic and organic NPs have been investigated in vitro and in vivo for the skin cancer therapy. MNPs advantages mostly include biodegradability, electrostatic charge, good biocompatibility, high drug payload, and low toxicity. However, the use of controlled-release systems stimulated by electromagnetic waves, temperature, pH, and light improves the accumulation in tumor tissues and improves therapeutic outcomes. This study (2019-2022) is aimed at reviewing applications of MNPs in the skin cancer therapy.


Assuntos
Nanopartículas de Magnetita , Neoplasias Cutâneas , Humanos , Nanopartículas de Magnetita/química , Administração Cutânea , Sistemas de Liberação de Medicamentos/métodos , Neoplasias Cutâneas/tratamento farmacológico , Portadores de Fármacos/química
20.
RSC Adv ; 12(49): 31680-31687, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36380962

RESUMO

Here, we prepare an Au NP decorated dithiocarbamate functionalized boehmite (γ-AlO(OH)@C-NHCS2H·AuNPs). This stepwise synthetic method gives an efficient, cost-effective, and green heterogenous Au-based nanocatalyst for the A3-coupling preparation of the biologically essential propargylamines. Different characterization methods, including FT-IR, XRD, SEM, TEM, EDX spectra, and elemental SEM-mapping, were employed to investigate the structure of the manufactured γ-AlO(OH)@C-NHCS2H·AuNPs. Then we used the prepared composite as a heterogeneous gold-based nanocatalyst for the one-pot A3-coupling preparation of propargyl amines by reacting a variety of aldehydes, amines, and phenylacetylene which exhibited promising results.

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