Insights into free radicals scavenging, α-Amylase inhibition, cytotoxic and antifibrotic activities unveiled by Peganum harmala extracts.

BACKGROUND: Peganum harmala L. is used in traditional medicine to treat several health ailments. Hence, the present work aimed to investigate the DPPH free radical scavenging, α-amylase, cytotoxic, and antifibrotic effects of the hydrophilic extract and fixed oil obtained from P. harmala seeds. METHODS: The hydrophilic extract and fixed oil of P. harmala were assessed for their abilities to scavenge DPPH free radicals and inhibit α-amylase using reference bioassays. The cytotoxicity was assessed on several cancer and normal cell lines, including B16F1, Caco-2, COLO205, HeLa, Hep 3B and Hep G2, MCF-7, and HEK-293 T cells. The MTS assay was used to evaluate the antifibrotic capabilities utilizing the human hepatic stellate (LX-2) cell line. RESULTS: P. harmala plant fixed oil has potent DPPH free radical scavenging activity with an IC50 dose of 79.43 ± 0.08 µg/ml. Besides, the hydrophilic extract has a poor anti-α-amylase effect compared with the antidiabetic drug Acarbose, with IC50 doses of 398 ± 0.59 and 25.11 ± 1.22 µg/ml, respectively. In addition, the growth of MCF-7, Hep3B, HepG2, HeLa, COLO205, CaCo2, B16F1, and HeK293t was inhibited by P. harmala hydrophilic extract with IC50 doses of 121.34 ± 1.71, 268.3 ± 0.75, 297.20 ± 1.00, 155.60 ± 1.14, 150.01 ± 0.51, 308.35 ± 0.53, 597.93 ± 1.36, and 5.38 ± 0.99 µg/ml, respectively. In addition, at 1000 µg/ml, 5-Fluorouracil reduced fibrosis cells by 0.089%, while the hydrophilic extract decreased the number of LX-2 cells by 5.81%. CONCLUSION: P. harmala plant-fixed oil exhibits potential antioxidant properties. While the hydrophilic extract showed limited effectiveness as an anti-α-amylase agent and demonstrated notable cytotoxic effects against various tested cancer cell lines. Furthermore, this extract significantly reduces the number of LX-2 fibrotic cells. These findings emphasize the therapeutic potential of these products in managing various health disorders and warrant further investigation into their mechanisms of action and clinical applications.

Phytochemical screening, antioxidant, anti-diabetic, and anti-obesity activities, formulation, and characterization of a self-nanoemulsion system loaded with pomegranate (Punica granatum) seed oil.

Pomegranate (Punica granatum) is a tree of the Punicaceae family that is widespread all over the world and has several types and therapeutic uses. The current study aimed to investigate the phytochemical compounds by GC analysis and carried out physical characterization of the pomegranate seed oil and its self-nanoemulsifying system. Then antioxidant, anti-diabetic, and anti-lipase activities were investigated for both.The pomegranate seed oil was extracted, and its self-nanoemulsifying system was then prepared. Phytochemical compounds were analyzed by GC, and physical characterization was established of the pomegranate seed oil and its self-nanoemulsifying system. Then antioxidant, anti-diabetic, and anti-lipase activities were investigated for both.The GC-MS analysis revealed that punicic acid, ß-eleosteric acid, catalpic acid, α-eleosteric acid, and oleic acid were the most predominant compounds in pomegranate seed oil. Other active compounds like linoleic acid, palmitic acid, stearic acid, and α-linolenic acid were detected in trace percentages. The self-nanoemulsifying system was prepared using various concentrations of surfactant (Tween 80), co-surfactant (Span 80), and pomegranate seed oil. The selected formulation had a PDI of 0.229 ± 0.09 and a droplet size of 189.44 ± 2.1 nm. The free radical scavenging activity of pomegranate seed oil, the self-emulsifying system, and Trolox was conducted using DPPH. The oil-self-nanoemulsifying system showed potent antioxidant activity compared to Trolox. Also, pomegranate oil inhibited α-amylase with a weak IC50 value of 354.81 ± 2.3 µg/ml. The oil self-nanoemulsifying system showed potent activity compared to acarbose and had a weaker IC50 value (616.59 ± 2.1 µg/ml) and a potent IC50 value (43.65 ± 1.9 µg/ml) compared to orlistat.Pomegranate seed oil self-nanoemulsifying system could be applied in the future for the preparation of possible oral medications for the prevention and treatment of oxidative stress, diabetes, and obesity due to its high activity against free radical, amylase, and lipase enzymes compared to pomegranate seed oil itself and the references used. This study reveals that self-nanoemulsion systems can enhance oil drug formulations by improving pharmacokinetics and pharmacodynamics, acting as drug reservoirs, and facilitating efficient oil release.

Biological, phytochemical and molecular docking characteristics of Laurus nobilis L. fresh leaves essential oil from Palestine.

BACKGROUND: The historical use of Laurus nobilis L., the plant is native to the Mediterranean region and has been cultivated for its aromatic leaves, which are used as a flavoring agent in cooking and for their potential therapeutic properties. METHODS: The purpose of the current investigation was to characterize the essential oil composition of the fresh L. nobilis leaves from Palestine by 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. While MTS assay were used to evaluate their antiproliferative activities on panels of cell lines. Moreover, the docking studies were aided by the Prime MM GBSA method for estimating binding affinities. RESULTS: The GC-MS investigation demonstrated that the fresh L. nobilis leaves essential oil has a variety of chemicals, about 31 different biochemicals were identified, and the major compounds were 1,8-cineole (48.54 ± 0.91%), terpinyl acetate (13.46 ± 0.34%), and α-terpinyl (3.84 ± 0.35%). Furthermore, the investigated oil demonstrated broad-spectrum antimicrobial activity against all tested bacterial and candidal strains and significantly inhibited the growth of MCF-7 cancerous cells more than the chemotherapeutic drug Doxorubicin. Furthermore, it contains robust DPPH free radicals, as well as porcine pancreatic α-amylase and lipase enzymes. Using the 1,8-cineole compound as the predominant biomolecule found in the L. nobilis essential oil, molecular docking studies were performed to confirm these observed fabulous results. The molecular docking simulations proposed that these recorded biological activities almost emanated from its high ability to form strong and effective hydrophobic interactions, this led to the getting of optimal fitting and interaction patterns within the binding sites of the applied crystallographic protein targets. CONCLUSION: The results of these experiments showed that the fresh L. nobilis leaves essential oil has outstanding pharmacological capabilities, making this oil a potential source of natural medications.

Total phenolic contents, cytotoxic, free radicals, porcine pancreatic α-amylase, and lipase suppressant activities of Artemisia dracunculus plant from Palestine.

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.

Capsicum annuum Oleoresin Nanoemulgel - Design Characterization and In vitro Investigation of Anticancer and Antimicrobial Activities.

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.

Multi-biological activity assessment and phytochemical characterization of an aqueous extract of the Cymbopogon citratus grown in Palestine.

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.

Eucalyptus camaldulensis Dehnh Leaf Essential Oil from Palestine Exhibits Antimicrobial and Antioxidant Activity but No Effect on Porcine Pancreatic Lipase and α-Amylase.

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.

Biological Evaluation of Xanthene and Thioxanthene Derivatives as Antioxidant, Anticancer, and COX Inhibitors.

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.

Assessment of anticancer, antimicrobial, antidiabetic, anti-obesity and antioxidant activity of Ocimum Basilicum seeds essential oil from Palestine.

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.

The effect of Lavandula Coronopifolia essential oil on the biophysical properties of desensitization and deactivation gating currents in ionotropic receptors.

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.

Design, synthesis, molecular docking studies and biological evaluation of thiazole carboxamide derivatives as COX inhibitors.

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.

Comparing and contrasting different herbal products intended for the management of obesity approved in the Palestinian markets.

BACKGROUND: The use of conventional medical therapies has proven to have many setbacks and safety concerns that need further improvement. However, herbal medicine has been used for over 2000 years, and many studies have proven the use of herbs to be effective and safe. This article discussed the efficacy of different herbal products used in the management of obesity. To evaluate the efficacy of seven herbal-based weight loss products currently available on the Palestinian market, using in vitro assays to screen for antioxidants, anti-amylase, and anti-lipase effects for each product. METHOD: Pancreatic lipase and salivary amylase inhibitory activities, as well as antioxidant analysis, were tested in vitro on a variety of herbal products. Then the IC50 was measured for each test. RESULTS: The anti-lipase assay results, IC50 values in (µg/mL) of each of the seven products (Product A, product B, product C, product D, product E, product F, and product G) were 114.78, 532.1, 60.18, 53.33, 244.9, 38.9, and 48.97, respectively. The IC50 value for orlistat (Reference) was 12.3 µg/ml. On the other hand, the IC50 value for alpha amylase inhibition of the seven products (Product A, product B, product C, product D, product E, product F, and product F) were 345.93, 13,803.84 (Inactive), 73.79, 130.91, 165.95, 28.18, and 33.11 µg/ml respectively, while acarbose (Reference) was 23.38 µg/ml. The antioxidant activity (IC50 values) for the seven products (Product A, product B, product C, product D, product E, product F, and product F) were 1258.92, 707.94, 79.43, 186.20, 164.81, 17.53, and 10.47 µg/ml respectively. While the IC50 value for Trolox was 2.70 µg/ml. CONCLUSION: It can be concluded that the seven products showed varied anti-lipase, anti-amylase, and antioxidant effects. However, products F and G showed superiority in all categories.

Phytochemical screening, antiobesity, antidiabetic and antimicrobial assessments of Orobanche aegyptiaca from Palestine.

BACKGROUND: Microbial resistance, diabetes mellitus, and obesity are global health care problems that have posed a serious threat to both human and environmental ecosystems. The goals of the present investigations are to investigate the phytoconstituents, antilipase, anti-α-amylase, and antimicrobial activity of Orobanche aegyptiaca Pers. (OA) from Palestine. METHODS: Identification of the phytoconstituents of OA plant petroleum ether, methylene chloride, chloroform, acetone, and methanol extracts were conducted using pharmacopeia's methods, while porcine pancreatic lipase and α-amylase inhibitory activities were examined using p-nitrophenyl butyrate and 3,5-dinitro salicylic acid methods, respectively. Moreover, the antimicrobial activity was evaluated utilizing broth microdilution assay against eight bacterial and fungal strains. RESULTS: The phytochemical screening results showed that the methanol extract of the OA plant is rich in phytochemical components, also this extract has powerful antilipase potential with an IC50 value of 19.49 ± 0.16 µg/ml comparing with the positive control (Orlistat) which has antilipase activity with IC50 value of 12.3 ± 0.35 µg/ml. Moreover, the methanol and chloroform extracts have powerful α-amylase inhibitory activity with IC50 values of 28.18 ± 0.22 and 28.18 ± 1.22 µg/ml, respectively comparing with Acarbose which has α-amylase inhibitory activity with IC50 dose of 26.3.18 ± 0.28 µg/ml. The antibacterial results showed that the methylene chloride extract exhibited the highest antibacterial activity among the other OA plant extracts with a MIC value of 0.78 mg/ml against S. aureus, while, the methylene chloride, petroleum ether, and chloroform extracts of the OA plant showed potential antifungal activity against C. albicans strains with MIC value of 0.78 mg/ml. CONCLUSION: The OA methanol and chloroform extracts could be excellent candidates as antilipase and anti-α-amylase bioactive materials. In addition, methylene chloride, petroleum ether, and chloroform extracts could be potential natural antimicrobial products.

Development of Coriandrum sativum Oil Nanoemulgel and Evaluation of Its Antimicrobial and Anticancer Activity.

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.

Anticancer, Free Radicals, and Digestive Enzyme Inhibitory Activities of Rubus sanctus Schreb Root Four Solvent Fractions.

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.

Molecular docking, chemo-informatic properties, alpha-amylase, and lipase inhibition studies of benzodioxol derivatives.

Currently, available therapies for diabetes could not achieve normal sugar values in a high percentage of treated patients. In this research project, a series of 17 benzodioxole derivatives were evaluated as antidiabetic agents; that belong to three different groups were evaluated against lipase and alpha-amylase (α-amylase) enzymes. The results showed that 14 compounds have potent inhibitory activities against α-amylase with IC50 values below 10 µg/ml. Among these compounds, 4f was the most potent compound with an IC50 value of 1.11 µg/ml compared to the anti-glycemic agent acarbose (IC50 6.47 µg/ml). On the contrary, these compounds showed weak or negligible activities against lipase enzyme. However, compound 6a showed the best inhibitory anti-lipase activity with IC50 44.1 µg/ml. Moreover, all the synthesized compounds were undergone Molinspiration calculation, and the result showed that all compounds obeyed Lipinski's rule of five. Molecular docking studies were performed to illustrate the binding interactions between the benzodioxole derivatives and α-amylase enzyme pocket. Related to the obtained results it was clear that the carboxylic acid, benzodioxole ring, halogen or methoxy substituted aryl are important for the anti-amylase activities. The potent inhibitory results of some of the synthesized compounds suggest that these molecules should go further in vivo evaluation. It also suggests the benzodioxole derivatives as lead compounds for developing new drug candidates.

Spectral characterization, antioxidant, antimicrobial, cytotoxic, and cyclooxygenase inhibitory activities of Aloysia citriodora essential oils collected from two Palestinian regions.

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.

Antiamylase, Antilipase, Antimicrobial, and Cytotoxic Activity of Nonea obtusifolia (Willd.) DC. from Palestine.

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.

Development and Antimicrobial Evaluation of Eruca Sativa Oil Nanoemulgel with Determination of the Oil Antioxidant, Sun Protection Factor and Elastase Inhibition.

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.

Antibacterial, Anticandidal, Phytochemical, and Biological Evaluations of Pellitory Plant.

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.