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1.
Front Pharmacol ; 15: 1351743, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38515857

RESUMO

Artemisia dracunculus: L. (A. dracunculus) is a popular vegetable and spice cultivated across many Middle Eastern countries. The herb's aqueous extract has significant folkloric medicinal importance for treating various disorders. Hence, the present investigation aimed to investigate A. dracunculus hydrophilic extract phytochemical constituents and pleiotropic biological potentials, as no previous studies have investigated the antilipase and anti-α-amylase effects of the A. dracunculus plant. Total phenol content and phytochemical screening assays were performed utilizing standard analytical methods. While the α-amylase inhibition, free radical-scavenging, antilipase, and cytotoxic activities were determined using dinitrosalicylic acid (DNSA), DPPH, p-nitrophenyl butyrate (PNPB), and MTS assays, respectively. The standard phytochemical analysis of A. dracunculus aqueous extract shows that this extract contains only a phenolic group. The total phenol content was 0.146 ± 0.012 mg GAE/g of the plant dry extract. The A. dracunculus aqueous extract exhibited potent DPPH free radical inhibitory (IC50 dose of 10.71 ± 0.01 µg/mL) and anti-lipase activities (IC50 dose of 60.25 ± 0.33 µg/mL) compared with Trolox (IC50 = 5.7 ± 0.92 µg/mL) and Orlistat (IC50 = 12.3 ± 0.35 µg/mL), respectively. However, it showed a weak anti-α-amylase effect (IC50 value > 1,000 µg/mL) compared with Acarbose (IC50 = 28.18 ± 1.27 µg/mL). A. dracunculus has a cytotoxic effect against the HeLa cancer cell line compared with the chemotherapeutic agent Doxorubicin. The extract has the same percent of inhibition as Doxorubicin (99.9%) at 10 mg/mL. Overall, these results pointed out for the first time the importance of considering A. dracunculus effects as a favorite candidate for preventing and treating metabolic disorders. Also, our results confirm the findings of previous reports on the role of A. dracunculus in the management of cancer and disorders resulting from the accumulation of harmful free radicals. On the contrary, the current study concluded that the antidiabetic role of A. dracunculus could be minimal. Further in-depth investigations are urgently warranted to explore the importance of A. dracunculus in pharmaceutical production.

2.
Curr Pharm Des ; 30(2): 151-160, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38532324

RESUMO

BACKGROUND: The use of naturally occurring bioactive materials is getting great attention owing to their safety and environmental properties. Oily compounds, known as oleoresins, are expected to provide an important source for the natural products industry aiming to develop novel treatments for skin conditions. In this work, Capsicum annuum oleoresin nanoemulgel formulations have been prepared and investigated for their antibacterial and anticancer properties. METHODOLOGY: Several C. annuum oleoresin nanoemulgel formulations were prepared by incorporating a Carbopol 940 gel in a self-nanoemulsifying nanoemulsion consisting of C. annuum, tween 80, and span 80. The systems were characterized for particle size, polydispersity index (PDI), zeta potential, and rheology. The in vitro antimicrobial and cytotoxic activities of the optimum formulation were evaluated. RESULTS: The selected formulation is composed of 40% tween, 10% span 80, and 40% C. annuum oleoresin. This formulation produced a stable nanoemulsion with a narrow PDI value of 0.179 ± 0.08 and a droplet size of 104.0 ± 2.6 nm. Results of the in vitro antimicrobial studies indicated high potency of the systems against methicillin-resistant Staphylococcus aureus (MRSA) (zone of inhibition of 29 ± 1.9 mm), E. coli (33 ± 0.9 mm), K. pneumonia (30 ± 1.4 mm), and C. albicans (21 ± 1.5 mm), as compared to the reference antibiotic, ampicillin (18 ± 1.4 mm against K. pneumonia), and antifungal agent, fluconazole (12 ± 0.1 mm against C. albicans). Furthermore, cytotoxicity results, expressed as IC50 values, revealed that the oleoresin and its nanoemulgel had the best effects against the HepG2 cell line (IC50 value of 79.43 µg/mL for the nanoemulgel) and MCF7 (IC50 value of 57.54 µg/mL), and the most potent effect was found against 3T3 (IC50 value of 45.7 µg/m- L). On the other side, the system did not substantially exhibit activity against By-61 and Hela. CONCLUSION: C. annuum oleoresin and its nanoemulgel can be considered valuable sources for the discovery of new antibacterial, antifungal, and anticancer compounds in the pharmaceutical industry, especially due to their potent activity against various cancer cell lines as well as bacterial and fungal strains.


Assuntos
Anti-Infecciosos , Capsicum , Staphylococcus aureus Resistente à Meticilina , Extratos Vegetais , Pneumonia , Humanos , Escherichia coli , Antibacterianos/farmacologia , Anti-Infecciosos/farmacologia , Candida albicans
3.
BMC Complement Med Ther ; 24(1): 27, 2024 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-38195607

RESUMO

BACKGROUND: Plants have historically been a rich source of medicinal compounds, with many modern pharmaceuticals derived from botanical origins. In contemporary healthcare, there is a resurgence in utilizing botanical substances as recognized medicinal agents. This study delved into understanding the phytochemical makeup and the multifaceted biological activities of an aqueous extract from Cymbopogon citratus (C. citratus). The investigated activities were its effect on AMPA receptors, antioxidant capacity, anti-lipase, anti-α-amylase actions, cytotoxicity, and antimicrobial properties. METHODS: The extract of C. citratus received a comprehensive investigation, which included the study of its phytochemical composition, assessment of its antioxidant and anti-lipase properties, evaluation of its capacity to inhibit α-amylase, analysis of its impact on cell viability, and assessment of its antimicrobial activity. The approaches are used to clarify the complex physiological and biochemical characteristics. RESULTS: The results were compelling; receptor kinetics had a marked impact, notably on the GluA2 subunit. Regarding its medicinal potential, the extract demonstrated potent antioxidant and anti-diabetic activities with IC50 values of 15.13 and 101.14 µg/mL, respectively. Additionally, it displayed significant inhibitory effects on the lipase enzyme and showed cytotoxicity against the Hep3B cancer cell line, with IC50 values of 144.35 and 148.37 µg/mL. In contrast, its effects on the normal LX-2 cell line were minimal, indicating selectivity. CONCLUSION: The aqueous extract of C. citratus shows promising therapeutic properties. The findings advocate for further research into its compounds for potential isolation, purification, and in-depth pharmacological studies, especially in areas like nervous system disorders, diabetes, obesity, and combating oxidative stress.


Assuntos
Anti-Infecciosos , Cymbopogon , Humanos , Antioxidantes/farmacologia , Árabes , Lipase , Compostos Fitoquímicos/farmacologia , Anti-Infecciosos/farmacologia
4.
Plants (Basel) ; 12(22)2023 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-38005702

RESUMO

Eucalyptus camaldulensis Dehnh is a tree species that is commonly used for various purposes, including forestry, agroforestry, and conservation. The present investigation was designed to determine the composition of E. camaldulensis leaves essential oil and estimate its free radicals, porcine pancreatic lipase, α-amylase inhibitory, and antimicrobial properties in vitro. The chemical constituents were analyzed using the gas chromatography-mass spectrometry (GC-MS) technique. DPPH (2,2-diphenyl-1-picrylhydrazyl), p-nitrophenyl butyrate, and 3,5-dinitro salicylic acid (DNSA) methods were employed to estimate the antioxidant, antiobesity, and antidiabetic effects of the essential oil. The microdilution assay was employed to assess the antimicrobial efficacy of the substance against a total of seven distinct microbial species. The GC-MS results revealed that E. camaldulensis essential oil contains 52 components that makeup 100% of the entire oil. The main chemical constituents in E. camaldulensis essential oil are p-cymene (38.64%), followed by aromadendrene (29.65%), and 1,8-cineol (6.45%), with monocyclic monoterpene being the most abundant phytochemical group, followed by the sesquiterpene hydrocarbon group, representing 44.27 and 31.46%, respectively. The essential oil showed a weak antioxidant effect and had no antilipase or antiamylase effects. At the same time, the oil showed a strong antimicrobial effect against methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus aureus, and Proteus vulgaris, which was even more potent than the positive controls, ciprofloxacin and ampicillin, which had MIC doses of 0.2 ± 0.01, 0.2 ± 0.01, and 6.25 ± 0.1 µg/mL, respectively. It also has a strong anti-Candida albicans effect with a MIC of 0.2 ± 0.01 µg/mL. In light of these findings, in vivo studies should be conducted to determine the efficiency of the E. camaldulensis essential oil in treating microbial infections.

5.
ACS Omega ; 8(41): 38597-38606, 2023 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-37867642

RESUMO

Xanthene and thioxanthene analogues have been investigated for their potential as anticancer and anti-inflammatory agents. Additionally, cysteine analogues have been found to possess antioxidant, anti-inflammatory, and anticancer activities due to their role in cellular redox balance, scavenging of free radicals, and involvement in nucleophilic reactions and enzyme binding sites. In this study, we synthesized a library of tertiary alcohols derived from xanthene and thioxanthene, and further, some of these compounds were coupled with cysteine. The objective of this research was to explore the potential anticancer, antioxidant, and anti-inflammatory activities of the synthesized compounds. The synthesized compounds were subjected to test for anticancer, antioxidant, and anti-inflammatory activities. Results indicated that compound 3 exhibited excellent inhibition activity (IC50 = 9.6 ± 1.1 nM) against colon cancer cells (Caco-2), while compound 2 showed good inhibition activity (IC50 = 161.3 ± 41 nM) against hepatocellular carcinoma (Hep G2) cells. Compound 4 demonstrated potent antioxidant inhibition activity (IC50 = 15.44 ± 6 nM), and compound 7 exhibited potent anti-inflammatory activity with cyclooxygenase-2 (COX-2) inhibition IC50 (4.37 ± 0.78 nM) and high selectivity for COX-2 (3.83). In conclusion, certain synthesized compounds displayed promising anticancer activity and anti-inflammatory effects. Nevertheless, additional research is necessary to create more analogues, develop a more distinct comprehension of the structure-activity relationship (SAR), and perform in vivo experiments to evaluate the pharmacokinetic and pharmacodynamic characteristics of the compounds under examination. Such research may pave the way for the development of novel therapeutic agents with potential applications in cancer and inflammatory diseases.

6.
BMC Complement Med Ther ; 23(1): 221, 2023 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-37403162

RESUMO

BACKGROUND: Many modern pharmaceutical researchers continue to focus on the discovery and evaluation of natural compounds for possible therapies for obesity, diabetes, infections, cancer, and oxidative stress. Extraction of Ocimum basilicum seed essential oil and evaluation of its antioxidant, anti-obesity, antidiabetic, antibacterial, and cytotoxic activities were the goals of the current study. METHOD: O. basilicum seed essential oil was extracted and evaluated for its anticancer, antimicrobial, antioxidant, anti-obesity, and anti-diabetic properties utilizing standard biomedical assays. RESULTS: O. basilicum seed essential oil showed good anticancer activity against Hep3B (IC50 56.23 ± 1.32 µg/ml) and MCF-7 (80.35 ± 1.17 µg/ml) when compared with the positive control, Doxorubicin. In addition, the essential oil showed potent antibacterial (against Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Proteus mirabilis, and Pseudomonas aeruginosa) and antifungal (against Candida albicans) activities. Moreover, as for the anti-amylase test, IC50 was 74.13 ± 1.1 µg/ml, a potent effect compared with the IC50 of acarbose, which was 28.10 ± 0.7 µg/ml. On the other hand, for the anti-lipase test, the IC50 was 112.20 ± 0.7 µg/ml a moderate effect compared with the IC50 of orlistat, which was 12.30 ± 0.8 µg/ml. Finally, the oil had a potent antioxidant effect with an IC50 of 23.44 ± 0.9 µg/ml compared with trolox (IC50 was 2.7 ± 0.5 µg/ml). CONCLUSION: This study has provided initial data that supports the importance of O. basilcum essential oil in traditional medicine. The extracted oil not only exhibited significant anticancer, antimicrobial, and antioxidant properties but also antidiabetic and anti-obesity effects, which provided a foundation for future research.


Assuntos
Anti-Infecciosos , Ocimum basilicum , Óleos Voláteis , Antioxidantes/farmacologia , Hipoglicemiantes/farmacologia , Anti-Infecciosos/farmacologia , Óleos Voláteis/farmacologia , Antibacterianos/farmacologia
7.
Sci Rep ; 13(1): 8417, 2023 05 24.
Artigo em Inglês | MEDLINE | ID: mdl-37225859

RESUMO

The rising incidence of cancer and the lack of effective therapeutic interventions for many neurological illnesses like Alzheimer's and epilepsy has prompted us to investigate the composition and effects of the Lavandula coronopifolia oil from Palestine on cancer cells and AMPA receptor subunits in the brain due to the vast range of beneficial properties of Lavandula coronopifolia essential oil (EO). GC/MS was used to analyze L. coronopifolia's EO chemistry. EO's cytotoxicity and biophysical effects on AMPA receptors were investigated using MTS and electrophysiological techniques. The GC-MS results revealed that L. coronopifolia EO has a high content of eucalyptol (77.23%), ß-pinene (6.93%), and α-pinene (4.95%). The EO showed more significant antiproliferative selectivity activities against HepG2 cancer cell lines than HEK293T cell lines with IC50 values of 58.51 and 133.22 µg/mL, respectively. The EO of L. coronopifolia affected AMPA receptor kinetics (desensitization and deactivation) and preferred homomeric GluA1 and heteromeric GluA1/A2 receptors. These findings indicate the potential therapeutic use of L. coronopifolia EO in the selective treatment of HepG2 cancer cell lines and neurodegenerative diseases.


Assuntos
Lavandula , Óleos Voláteis , Humanos , Células HEK293 , Receptores de AMPA , Óleos Voláteis/farmacologia , Biofísica
8.
BMC Chem ; 17(1): 11, 2023 Mar 06.
Artigo em Inglês | MEDLINE | ID: mdl-36879343

RESUMO

BACKGROUND: Nonsteroidal anti-inflammatory drugs (NSAIDs) have been the most commonly used class of medications worldwide for the last three decades. OBJECTIVES: This study aimed to design and synthesize a novel series of methoxyphenyl thiazole carboxamide derivatives and evaluate their cyclooxygenase (COX) suppressant and cytotoxic properties. METHODS: The synthesized compounds were characterized using 1H, 13C-NMR, IR, and HRMS spectrum analysis and were evaluated for their selectivity towards COX-1 and COX-2 using an in vitro COX inhibition assay kit. Besides, their cytotoxicity was evaluated using the Sulforhodamine B (SRB) assay. Moreover, molecular docking studies were conducted to identify the possible binding patterns of these compounds within both COX-1 and COX-2 isozymes, utilizing human X-ray crystal structures. The density functional theory (DFT) analysis was used to evaluate compound chemical reactivity, which was determined by calculating the frontier orbital energy of both HOMO and LUMO orbitals, as well as the HOMO-LUMO energy gap. Finally, the QiKProp module was used for ADME-T analysis. RESULTS: The results revealed that all synthesized molecules have potent inhibitory activities against COX enzymes. The percentage of inhibitory activities at 5 µM concentration against the COX2 enzyme was in the range of 53.9-81.5%, while the percentage against the COX-1 enzyme was 14.7-74.8%. That means almost all of our compounds have selective inhibition activities against the COX-2 enzyme, and the most selective compound was 2f, with selectivity ratio (SR) value of 3.67 at 5 µM concentration, which has a bulky group of trimethoxy on the phenyl ring that could not bind well with the COX-1 enzyme. Compound 2h was the most potent, with an inhibitory activity percentage at 5 µM concentration of 81.5 and 58.2% against COX-2 and COX-1, respectively. The cytotoxicity of these compounds was evaluated against three cancer cell lines: Huh7, MCF-7, and HCT116, and negligible or very weak activities were observed for all of these compounds except compound 2f, which showed moderate activities with IC50 values of 17.47 and 14.57 µM against Huh7 and HCT116 cancer cell lines, respectively. Analysis of the molecular docking suggests 2d, 2e, 2f, and 2i molecules were bound to COX-2 isozyme favorably over COX-1 enzyme, and their interaction behaviors within COX-1 and COX-2 isozymes were comparable to celecoxib, as an ideal selective COX-2 drug, which explained their high potency and COX-2 selectivity. The molecular docking scores and expected affinity using the MM-GBSA approach were consistent with the recorded biological activity. The calculated global reactivity descriptors, such as HOMO and LUMO energies and the HOMO-LUMO gaps, confirmed the key structural features required to achieve favorable binding interactions and thus improve affinity. The in silico ADME-T studies asserted the druggability of molecules and have the potential to become lead molecules in the drug discovery process. CONCLUSION: In general, the series of the synthesized compounds had a strong effect on both enzymes (COX-1 and COX-2) and the trimethoxy compound 2f was more selective than the other compounds.

9.
Biomed Res Int ; 2021: 5247816, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34671674

RESUMO

This study is aimed at developing coriander oil into a nanoemulgel and evaluating its antimicrobial and anticancer effects. Coriander (Coriandrum sativum) oil was developed into a nanoemulgel by using a self-nanoemulsifying technique with Tween 80 and Span 80. Hydrogel material (Carbopol 940) was then incorporated into the nanoemulsion and mixed well. After this, we evaluated the particle size, polydispersity index (PDI), rheology, antimicrobial effect, and cytotoxic activity. The nanoemulsion had a PDI of 0.188 and a particle size of 165.72 nm. Interesting results were obtained with the nanoemulgel against different types of bacteria, such as Pseudomonas aeruginosa, Klebsiella pneumoniae, and methicillin-resistant Staphylococcus aureus (MRSA), with a minimum inhibitory concentration (MIC) of 2.3 µg/ml, 3.75 µg/ml, and 6.5 µg/ml, respectively. In addition, the half-maximal inhibitory concentration (IC50) of the nanoemulgel when applying it to human breast cancer cells (MCF-7), hepatocellular carcinoma cells (Hep3B), and human cervical epithelioid carcinoma cells (HeLa) was 28.84 µg/ml, 28.18 µg/ml, and 24.54 µg/ml, respectively, which proves that the nanoemulgel has anticancer effects. The development of C. sativum oil into a nanoemulgel by using a self-nanoemulsifying technique showed a bioactive property better than that in crude oil. Therefore, simple nanotechnology techniques are a promising step in the preparation of pharmaceutical dosage forms.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Coriandrum/química , Nanoestruturas/administração & dosagem , Neoplasias/tratamento farmacológico , Óleos Voláteis/farmacologia , Óleos de Plantas/farmacologia , Antibacterianos/química , Antineoplásicos/química , Linhagem Celular Tumoral , Emulsões , Humanos , Nanoestruturas/química , Neoplasias/metabolismo , Neoplasias/patologia , Óleos Voláteis/química , Tamanho da Partícula , Óleos de Plantas/química
10.
Artigo em Inglês | MEDLINE | ID: mdl-34221089

RESUMO

BACKGROUND: Humankind used herbal products as a source of medicines since they understood their therapeutic benefits from ancient times. Therefore, the current research aimed to determine the anticancer, antioxidant, and metabolic enzyme inhibitory activities of Rubus sanctus (RS) root four solvent fractions for the first time. METHODS: The antioxidant, antilipase, and anti-α-amylase potentials of (RS) four solvent fractions were evaluated using standard biomedical assays. Moreover, the DNA cell cycle of liver cancer was assessed using a propidium iodide (PI) assay. At the same time, the apoptosis activity was estimated utilizing flow the cytometry method. RESULTS: The methanol and acetone (RS) fractions showed the highest antioxidant activity with IC50 values of 0.078 ± 0.22 and 0.67 ± 0.25 µg/ml, respectively, compared with Trolox, which has an antioxidant IC50 value of 2.039 ± 0.52 µg/ml. Moreover, the methanol (RS) fraction has the highest anti-α-amylase activity with an IC50 value of 20.12 ± 0.34 µg/ml compared with acarbose, which has an IC50 value of 6.565 ± 0.3 µg/ml. Also, the acetone (RS) fraction revealed the highest antilipase activity with an IC50 value of 6.03 ± 1.23 µg/ml compared with the positive control orlistat which has an IC50 value of 0.39 ± 0.45 µg/ml. The aqueous, methanol, acetone, and hexane fractions of the (RS) roots decreased the secretion of the α-fetoprotein in the liver cancer cells. The acetone fraction was the most potent α-fetoprotein inhibitor with an average of 237 ± 12.5% compared with the average of the untreated cells, which was 4066.6 ± 202%. The hexane fraction was the most effective in diminishing apoptosis with an average of 14.5 ± 1.6%, compared with 49% ± 2 untreated cells' average. In inhibiting cell cycle progression, it was recognized that methanol fraction seems to be the most powerful amplifier of the (RS) effect, as it increased the proportion of the cells with an average of 24.5 ± 2.2%, compared with 7.4 ± 1.8% in the doxorubicin (DOX). Data indicated a decrease in cell proliferation rate by prolonging the G2-M phase and thus slowing cancer progression. Our results suggest that (RS) roots four solvent fractions have potential anticancer activity. CONCLUSION: The (RS) roots four solvent fractions have potential anticancer, antioxidant, antilipase, and α-amylase inhibitory activities. It could be a promising source for applications in the functional food, nutraceutical, and pharmaceutical industries.

11.
BMC Complement Med Ther ; 21(1): 143, 2021 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-34001110

RESUMO

BACKGROUND: Aloysia citriodora Palau (AC) is commonly known as Lemon Verbena and has been utilized as a medicinal tea in folkloric medicine for the treatment of abdominal spasm, anxiety, and fever. The present investigation aimed to identify the chemical ingredients of AC essential oil (EO) collected from two different locations in Palestine and to assess their antioxidant, antimicrobial, cytotoxic, and cyclooxygenase (COX) inhibitory effects. METHODS: Gas chromatography/mass spectroscopy (GC/MS) technique was used to identify the chemical components of the hydro-distilled EO from both regions, while DPPH, MTS, and COX assays were utilized to estimate the antioxidant, cytotoxic, and COX inhibitory activities of the EOs, respectively. Moreover, a broth microdilution assay was used to assess antimicrobial potentials against seven microbial strains. RESULTS: The GC/MS technique revealed the presence of 17 compounds from the AC collected from the Umm al-Fahm region and 13 compounds from the sample from the Baqa al-Gharbiyye region, while α-citral was the major component of both EOs, representing 47.62 and 43.46%, respectively. The Baqa al-Gharbiyye AC EO exerted more potent antioxidant activity than the Umm al-Fahm EO, with IC50 values of 11.74 ± 0.18 and 35.48 ± 0.14 µg/mL, respectively, while the positive control Trolox had antioxidant IC50 values of 2.45 ± 0.01 µg/mL. Interestingly, both EOs inhibited more potential activity against Methicillin-Resistant Staphylococcus aureus (MRSA) and Proteus vulgaris than Ciprofloxacin and Ampicillin antibiotics and also showed more potent antifungal activity against Candida albicans than Fluconazole. Moreover, the Baqa al-Gharbiyye AC EO had a more potent cytotoxic effect than the Umm al-Fahm EO, with IC50 values of 84.5 ± 0.24 and 33.31 ± 0.01 µg/mL, respectively, compared with Doxorubicin, which had an IC50 dose of 22.01 ± 1.4 µg/mL. The EOs from Baqa al-Gharbiyye showed potent activity against both COX-1 and COX-2 enzymes, with IC50 of 52.93 ± 0.13 and 89.31 ± 0.21 µg/mL, respectively, while the EOs from the Umm al-Fahm region showed weaker activity against these enzymes, with IC50 of 349.99 ± 0.33 and 1326.37 ± 1.13 µg/mL, respectively. CONCLUSION: Both characterized EOs have a huge variety of chemical components. The Baqa al-Gharbiyye AC EO has more potent antioxidant and cytotoxic activities than the Umm al-Fahm EO, but both have potential antimicrobial activity against MRSA, P. vulgaris, and C. albicans. These results suggest the use of AC EOs as promising sources of active ingredients in the food, cosmetic, and pharmaceutical industries.


Assuntos
Anti-Infecciosos , Antioxidantes , Inibidores de Ciclo-Oxigenase , Óleos Voláteis , Verbenaceae/química , Anti-Infecciosos/análise , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Inibidores de Ciclo-Oxigenase/análise , Inibidores de Ciclo-Oxigenase/química , Inibidores de Ciclo-Oxigenase/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Células HeLa , Humanos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Óleos Voláteis/análise , Óleos Voláteis/química , Óleos Voláteis/farmacologia
12.
Biomed Res Int ; 2020: 8821319, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33344648

RESUMO

BACKGROUND: Medicinal plants are widely used in many cultures, traditions, and civilizations worldwide. Plants with high contents of the valuable biological compounds can efficiently cure many diseases. This study is aimed at assessing, for the first time, the anti-α-amylase, antilipase, antimicrobial, and cytotoxic activities of Nonea obtusifolia (Willd.) DC. of five extracts from Palestine. METHODS: The antimicrobial activity was estimated using well diffusion method for N. obtusifolia plant of five extracts against eight ATCC (American Type Culture Collection) and clinical isolates. The cytotoxic effects for these extracts were evaluated against HeLa (cervical) carcinoma cells using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Moreover, the lipase and α-amylase inhibitory properties were determined using standard biomedical assays. RESULTS: The acetone extract of N. obtusifolia plant showed a more potent α-amylase inhibitory compared with acarbose with IC50 values of 25.7 ± 0.08 and 28.18 ± 1.22 µg/ml, respectively. Additionally, the acetone and methanol extracts revealed moderate antilipase activity compared to orlistat with IC50 values of 30.19 ± 0.11, 33.11 ± 0.13, and 12.3 ± 0.35 µg/ml, respectively. The methylene chloride extract was found to inhibit the growth of all the tested bacterial and fungal strains and also found to have potential cytotoxic effect against HeLa cancer cell line. CONCLUSION: This research work reports for the first time the biological activity of N. obtusifolia from Palestine, and the results were promising indicating that N. obtusifolia extracts contain valuable bioactive molecules that have a potential anti-α-amylase, antilipase, antibacterial, and antifungal cytotoxic potentials. Therefore, N. obtusifolia could have a medical significance in the future.


Assuntos
Amilases/antagonistas & inibidores , Anti-Infecciosos/farmacologia , Boraginaceae/química , Lipase/antagonistas & inibidores , Extratos Vegetais/farmacologia , Acetona/química , Animais , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Difusão , Células HeLa , Humanos , Concentração Inibidora 50 , Lipase/química , Lipídeos/química , Cloreto de Metileno/química , Testes de Sensibilidade Microbiana , Orlistate/farmacologia , Pâncreas/enzimologia , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Plantas Medicinais/química , Suínos , alfa-Amilases/química
13.
Curr Pharm Biotechnol ; 21(3): 244-255, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31924154

RESUMO

OBJECTIVES: This project aims to develop a bio-natural nano-product with Cosmeceutical and pharmaceutical applications. METHODS: E. sativa oil was evaluated for its anti-oxidant, sun protection factor and elastase inhibition. Then, nanoemulgel formulations were prepared for E. sativa oil through the combination of nanoemulsion with hydrogel. E. sativa nanoemulsion formulations were prepared by the help of a selfemulsification technique. After this, the optimum formulation was mixed with Carbopol to produce the nanoemulgel. Anti-bacterial and anti-fungal activities were evaluated. RESULTS: Nanoemulsion occurred when the size of the droplets was 195.29 nm with the lowest polydispersibility index 0.207. The results of antioxidant, anti-elastase and SPF activities for E. sativa oil were 2.10 µg/ml, 25.1 µg/ml and an SPF value of 5.57, respectively. In addition, in the anti-bacterial test for Staphylococcus aureus, it was found that nanoemulgel has an inhibition zone of 2.1 cm in diameter. According to the MRSA, the inhibition zone was 1.5 cm. CONCLUSION: E. Sativa oil could be a promising candidate in cosmeceutical and pharmaceutical preparations.


Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Brassicaceae/química , Nanoestruturas/química , Elastase Pancreática/antagonistas & inibidores , Óleos de Plantas/isolamento & purificação , Fator de Proteção Solar , Animais , Anti-Infecciosos/isolamento & purificação , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Candida/efeitos dos fármacos , Composição de Medicamentos , Emulsões , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Hidrogéis/química , Picratos/química , Sementes/química , Pele/efeitos dos fármacos , Pele/enzimologia , Suínos
14.
Biomed Res Int ; 2020: 6965306, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33415153

RESUMO

Pellitory plant (Parietaria judaica (PJ)) is one of the most widely used Arabian traditional medicinal plants due to its ability to cure several infectious diseases and other illnesses. The current study is aimed at assessing the phytoconstituents, antilipase, antiamylase, antimicrobial, and cytotoxic characters of the Pellitory plant (Parietaria judaica (PJ)). Phytochemical screening and procyanidin detection were conducted according to the standard phytochemical procedures. Porcine pancreatic lipase and α-amylase inhibitory activities were carried out using p-nitrophenyl butyrate and dinitrosalicylic acid assays, respectively. In addition, antimicrobial activity was determined utilizing a microdilution assay against several bacterial and fungal strains. Besides, the cytotoxic effect against HeLa cell line was tested employing 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) assay. The quantitative test results revealed that the methanol fraction of PJ contains 18.55 ± 0.55 mg of procyanidin and has a potential α-amylase inhibitory activity compared with the antidiabetic drug Acarbose with IC50 values of 15.84 ± 2.25 and 28.18 ± 1.22 µg/ml, respectively. Also, it has a potential antilipase activity compared to the commercial antiobesity drug, Orlistat, with IC50 values of 38.9 ± 0.29 and 12.3 ± 0.35 µg/ml, respectively. The acetone, hexane, and methanol fractions have broad-spectrum antibacterial activity against the screened bacterial strains, while the acetone fraction has shown anticandidal activity with a MIC value of 0.195 mg/ml. The PJ hexane and acetone fractions decreased HeLa cell viability significantly (p value < 0.0001) by approximately 90% at the concentration of 0.625 mg/ml. The revealed outcomes showed that the methanol fraction has strong α-amylase and lipase inhibitory characters. Besides, acetone, hexane, and methanol fractions have broad-spectrum antibacterial activity, while the acetone fraction revealed potent antifungal activity against Candida albicans. Moreover, at low concentrations, hexane and acetone fractions have potent cytotoxic and antiproliferative activity against HeLa cancer cells. Nevertheless, PJ acetone, hexane, and methanol fractions can serve as an effective source of natural products to develop new antiobesity, antidiabetic, antimicrobial, and anticancer agents.


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Parietaria/química , Compostos Fitoquímicos/farmacologia , Animais , Biflavonoides/análise , Calibragem , Catequina/análise , Morte Celular/efeitos dos fármacos , Inibidores Enzimáticos/farmacologia , Células HeLa , Humanos , Lipase/antagonistas & inibidores , Lipase/metabolismo , Testes de Sensibilidade Microbiana , Proantocianidinas/análise , Suínos , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo
15.
Biomed Res Int ; 2018: 4034689, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30151381

RESUMO

INTRODUCTION: In traditional medicine, many pharmacological activities have already been ascribed to the genus of Teucrium plant. These include antirheumatic antispasmodic, anthelmintic, diuretic, hypoglycemic, and anticancer effects. The recent investigation aimed to characterize and estimate the chemical composition, anti-inflammatory, antioxidant, and anticancer potentials of the essential oil isolated by the microwave-ultrasonic apparatus from Teucrium pruinosum leaves collected from Palestine. METHODS: The essential oil (EO) was analyzed by Gas Chromatography equipped with mass spectrometry (GC-MS), while its anticancer activity was evaluated against HeLa cervical adenocarcinoma cells. The ability of T. pruinosum EO to inhibit the conversion of Arachidonic Acid (AA) to PGH2 by ovine COX-1 and human recombinant COX-2 was determined using a COX inhibitor screening assay. In addition, the antioxidant activity of the EO was evaluated on the basis of the scavenging activity with a stable 2,2-diphenyl-1-picrylhydrazyl (DPPH) method, while Trolox was used as a positive control. RESULTS: Forty-four molecules were identified in T. pruinosum EO, representing 100% of the total EO. Agarospirol was found to be the most abundant component (45.53%) followed by caryophyllene (19.35%). However, the cyclooxygenase inhibitor assay revealed that T. pruinosum has potential COX-1 and Cox-2 inhibitory activity with IC50 values of 0.25 µg/ml and 0.5 µg/ml, respectively. Moreover, the T. pruinosum EO showed moderate antioxidant capacity with an IC50 value of 16.98±0.84 µg/ml in comparison with the positive control Trolox, which has an antioxidant potential with an IC50 value of 2.09±0.17 µg/ml. In addition, 250, 125, 62.5, 31.25, 15.625, 7.67, and 3.84 mg/ml of T. pruinosum EO treatments inhibited mitochondrial activity (cell viability) significantly and extremely by 90-95%. CONCLUSION: The current study provided data that revealed that the T. pruinosum EO could be a suitable candidate for use as a novel anticancer, anti-inflammatory, and antioxidant medication. Further clinical trials would be required to ensure these effects and to allow the design of suitable pharmaceutical dosage forms from this natural oil.


Assuntos
Antioxidantes/farmacologia , Inibidores de Ciclo-Oxigenase/farmacologia , Óleos Voláteis/química , Teucrium/química , Animais , Anti-Inflamatórios , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Óleos Voláteis/farmacologia , Ovinos
16.
J Cosmet Dermatol ; 17(6): 1122-1129, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29377413

RESUMO

BACKGROUND: Sunlight exposure affects all skin types causing skin tanning, burns or even skin cancer. Sunscreens were invented to prevent these outcomes by scattering or absorbing the UV light. AIMS: This study aimed to verify the effectiveness of Mansur method in SPF measurement and to find out how much reliable the labeled sun protection factor (SPF) value for the products that are imported to Palestine knowing that they are considered as cosmetics and they don't undergo tests by the Ministry Of Health (MOH). MATERIALS: In this research, sun protection factor (SPF) was determined for 16 commercially available sunscreen products using Mansur equation which was also validated; moreover sunscreen classification, product phase determination and pH measurement were also done. RESULTS: Sun protection factor values were mostly 50, 43.75% of the analyzed samples were close to the labeled SPF, 31.25% were under the labeled value, and 25% SPF value above the labeled value. All samples exhibited a pH close to skin pH. 62% of them were found to be O/W. Cosmetic companies and importers should focus on pediatric sunscreens, since only 12.5% are pediatric sunscreens. CONCLUSIONS: Ministry Of Health should ask prove about the quality of an SPF value of sunscreens for final registration of these products. More instructions should be available on the label regarding the proper use especially, if they are not water proof.


Assuntos
Fator de Proteção Solar , Protetores Solares , Cosméticos , Humanos , Oriente Médio , Reprodutibilidade dos Testes , Estados Unidos , United States Food and Drug Administration
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