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1.
Biomol Concepts ; 15(1)2024 Jan 01.
Article in English | MEDLINE | ID: mdl-38353049

ABSTRACT

This study explores the synergistic antibacterial effects of essential oils (EOs) and phenolic extracts from three plants against foodborne pathogenic bacteria. The present work aimed to investigate the synergistic effects of the binary and the ternary combinations of extracts using different blend proportions of the following plant extracts: Artemisia campestris (AC), Artemisia herba alba (AHA), and Citrus aurantium (CA). The antimicrobial activities of EOs and phenolic extracts were determined and evaluated against five strains. For the EOs, the results of the DIZ showed the existence of synergism for different combinations of binary blends, such as AC/AHA or AHA/CA against Escherichia coli, and AC/CA against Enterobacter faecalis. In addition, ternary blends of AC:AHA:CA at a ratio of 1/6:2/3:1/6 exhibited a synergy effect, as measured by the CI, against E. coli. On the other hand, for the phenolic extracts, synergistic effects were noticed for binary blends of AC/CA at different ratios against E. coli, E. faecalis, and Pseudomonas aeruginosa strains. Similarly, ternary blends of phenolic extracts presented synergy against E. coli, E. faecalis, P. aeruginosa strains, and even C. albicans. In this case, the blending ratios were crucial determining factors for maximizing the synergy effect. The study established that the proportion of a single drug could play an essential role in determining the bioefficacy of a drug combination treatment. Therefore, the results showed the importance of studying the modulation of antibacterial activities based on the proportions of extracts in the mixture and finding the range of proportions (as determined by SLMD) that have a synergistic/additive/antagonistic effect with no or low side effects, which can be used in a food preservation system.


Subject(s)
Artemisia , Citrus , Oils, Volatile , Oils, Volatile/pharmacology , Escherichia coli , Anti-Bacterial Agents/pharmacology , Phenols/pharmacology
2.
Molecules ; 28(23)2023 Nov 27.
Article in English | MEDLINE | ID: mdl-38067527

ABSTRACT

Fenugreek (Trigonella foenum-graecum) has a great beneficial health effect; it has been used in traditional medicine by many cultures. Likewise, the α-amylase inhibitors are potential compounds in the development of drugs for the treatment of diabetes. The beneficial health effects of fenugreek lead us to explore the chemical composition of the seeds and their antioxidant and α-amylase inhibition activities. The flavonoid extraction from fenugreek seeds was achieved with methanol through a Soxhlet apparatus. Then, the flavonoid glycosides were characterized using HPLC-DAD-ESI-MS analysis. The antioxidant capacity of fenugreek seed was measured using DPPH, FRAP, ABTS, and CUPRAC assays. Finally, the α-amylase inhibition activity was carried out using in vitro and in silico methods. The methanolic extract was found to contain high amounts of total phenolics (154.68 ± 1.50 µg GAE/mg E), flavonoids (37.69 ± 0.73 µg QE/mg E). The highest radical-scavenging ability was recorded for the methanolic extract against DPPH (IC50 = 556.6 ± 9.87 µg/mL), ABTS (IC50 = 593.62 ± 9.35 µg/mL). The ME had the best reducing power according to the CUPRAC (A 0.5 = 451.90 ± 9.07 µg/mL). The results indicate that the methanolic extracts of fenugreek seed best α-amylase inhibition activities IC50 = 653.52 ± 3.24 µg/mL. Twenty-seven flavonoids were detected, and all studied flavonoids selected have good affinity and stabilize very well in the pocket of α-amylase. The interactions between the studied flavonoids with α-amylase were investigated. The flavonoids from fenugreek seed present a good inhibitory effect against α-amylase, which is beneficial for the prevention of diabetes and its complications.


Subject(s)
Diabetes Mellitus , Trigonella , Humans , Antioxidants/chemistry , Trigonella/chemistry , Flavonoids/pharmacology , Flavonoids/analysis , Molecular Docking Simulation , alpha-Amylases , Chromatography, High Pressure Liquid , Plant Extracts/chemistry , Methanol/chemistry , Seeds/chemistry
3.
Molecules ; 28(1)2023 Jan 01.
Article in English | MEDLINE | ID: mdl-36615545

ABSTRACT

Pistacia Atlantica in folk medicine is used by Algerian traditional healers for treating a wide variety of diseases and conditions including dyspepsia, digestive problems, peptic ulcers, and, in particular, inflammatory diseases. The present study aimed to assess the phytochemical composition, in vitro antioxidant activity (using 2,2-diphenyl-1-picrylhydrazyl (DPPH), ABTS+, and reducing power methods), enzyme inhibitory activity (towards α-amylase and urease), antibacterial activity, and in vivo anti-inflammatory activity of the unripe fruit extracts of Pistacia atlantica collected from different parts of the Djelfa region of Algeria. According to the findings, various aqueous extracts exhibited significant antioxidant and enzymatic activities in all tests, but showed that they have a weak inhibitory effect against all tested bacterial strains. Twenty-one minerals comprising both macro- and microelements (Ba, Br, Ca, Cl, Co, Cr, Cs, Eu, Fe, K, Mg, Mn, Mo, Na, Rb, Sb, Sc, Sr, Th, U, and Zn) were determined using the technique of neutron activation analysis (INAA). The result indicates that the concentration of the mineral element is close to the minimal FAO recommendation. In addition, the result revealed significant anti-inflammatory activities. The data generated can be a valuable source of information for the pharmaceutical industry and medical research. These results suggest that the unripe fruit extracts of Pistacia atlantica have an appropriate potential to be utilized across a wide range of contexts as an agent with multifunctional uses, as well as a natural remedy for other physiological diseases.


Subject(s)
Antioxidants , Pistacia , Antioxidants/pharmacology , Antioxidants/analysis , Pistacia/chemistry , Urease , Plant Extracts/chemistry , Fruit/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/analysis , Minerals/analysis , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/analysis , Amylases
4.
J Biomol Struct Dyn ; 41(15): 7055-7068, 2023.
Article in English | MEDLINE | ID: mdl-36001586

ABSTRACT

Excessive intake of purine-rich foods such as seafood and red meat leads to excess xanthine oxidase activity and provokes gout attacks. The aim of this paper is to evaluate in vitro and in silico, the inhibition effect of Cupressus sempervirens plant extracts (flavonoids (Cae) and alkaloids (CaK)) and its six derivative compounds on bovine xanthine oxidase (BXO). The in silico study consists of molecular docking with GOLD v4.0 based on the best PLPchem score (PLP) and prediction of biological activity with the PASS server tool. The inhibitors used were lignan (cp1), Amentoflavone (cp2), Cupressuflavone (cp3), Isocryptomerin (cp4), Hinokiflavone (cp5), and Neolignan (cp6). The in vitro results showed that CaK gives an IC50 of 3.52 ± 0.04 µg/ml. Similarly, Cae saved an IC50 of 8.46 ± 1.98 µg/ml compared with the control (2.82 ± 0.10 µg/ml). The in silico results show that cp1 was the best inhibitor model (PLP of 88.09) with approved pharmacokinetics. These findings suggest that cp1 and cp2 may offer good alternatives for the treatment of hyperuricemia; cp3 was moderate, while the others (cp4 to cp6) were considered weak inhibitors according to their PLP.Communicated by Ramaswamy H. Sarma.

5.
Curr Comput Aided Drug Des ; 18(4): 307-317, 2022.
Article in English | MEDLINE | ID: mdl-35713136

ABSTRACT

BACKGROUND: Through this study, the Chemical composition realized by UHPLC-DADESI- MSn allowed the detection of different phenolic compound groups from Pistacia atlantica Desf. leaves extracts. We studied the inhibition of main protease (CL3 Mpro) and RNA-dependent RNA polymerase (RdRp) of the SARS-CoV-2 by the identified molecules through molecular docking. OBJECTIVE: The objective of this study is to identify compounds from Pistacia atlantica Desf. leaves extracts, which might have anti-viral effects. METHODS: Chemical composition was realized by UHPLC-DAD-ESI-MSn, and the inhibition of the main protease (CL3 Mpro) and RNA-dependent RNA polymerase (RdRp) of the SARS-CoV-2 was studied using molecular docking with Autodock Vina software. ADMET analysis was carried out. RESULTS: The identified compounds are quinic acid, digallic acid, galloylquinic acid, gallic acid, trigallic acid, digalloylquinic acids, trigalloylquinic acids and methyl gallate; digallic and quinic acids are the best inhibitors. Digallic acid had binding affinity energy (BAE) of -8.2 kcal/mol, and Ki of 1µM for the CL3 Mpro, Ki of 0.62 mM for the RdRp. Quinic acid showed Ki of 4.6 mM, recorded for both enzymes. Through ADMET analysis, we have found that the two molecules are good drug candidates. CONCLUSION: This is the first time that a group of identified compounds from Pistacia atlantica Desf. leaves are studied for their potential activity against the novel virus by inhibiting two key enzymes in its life cycle, and no further studies have been published in this context.


Subject(s)
COVID-19 Drug Treatment , Pistacia , Gallic Acid/pharmacology , Molecular Docking Simulation , Peptide Hydrolases , Pistacia/chemistry , Protease Inhibitors/pharmacology , Quinic Acid/pharmacology , RNA-Dependent RNA Polymerase , SARS-CoV-2 , Plant Leaves/chemistry , Plant Extracts/pharmacology
6.
Molecules ; 26(11)2021 Jun 01.
Article in English | MEDLINE | ID: mdl-34206087

ABSTRACT

Polyphenolic and Terpenoids are potent natural antiparasitic compounds. This study aimed to identify new drug against Leishmania parasites, leishmaniasis's causal agent. A new in silico analysis was accomplished using molecular docking, with the Autodock vina program, to find the binding affinity of two important phytochemical compounds, Masticadienonic acid and the 3-Methoxycarpachromene, towards the trypanothione reductase as target drugs, responsible for the defense mechanism against oxidative stress and virulence of these parasites. There were exciting and new positive results: the molecular docking results show as elective binding profile for ligands inside the active site of this crucial enzyme. The ADMET study suggests that the 3-Methoxycarpachromene has the highest probability of human intestinal absorption. Through this work, 3-Methoxycarpachromene and Masticadienonic acid are shown to be potentially significant in drug discovery, especially in treating leishmaniasis. Hence, drug development should be completed with promising results.


Subject(s)
Leishmania infantum/enzymology , NADH, NADPH Oxidoreductases/antagonists & inhibitors , Phytochemicals/pharmacology , Triterpenes/pharmacology , Catalytic Domain/drug effects , Computer Simulation , Drug Evaluation, Preclinical , Humans , Intestinal Absorption , Leishmania infantum/drug effects , Molecular Docking Simulation , Molecular Dynamics Simulation , Phytochemicals/chemistry , Phytochemicals/pharmacokinetics , Protozoan Proteins/antagonists & inhibitors , Structure-Activity Relationship , Triterpenes/chemistry , Triterpenes/pharmacokinetics
7.
J Diabetes Metab Disord ; 20(1): 427-438, 2021 Jun.
Article in English | MEDLINE | ID: mdl-34178849

ABSTRACT

BACKGROUND: Several medicinal plants are used in the steep area of Algeria (Laghouat) for treatment of inflammation and diabetes. Furthermore, Hammada elegans Botsch. (Chenopodiaceae) a xerophytic plant popularly known as (Ajram) is widely spread perennial shrub in Laghouat region and it is traditionally used to treat inflammation and diabete. Then, the objective of this work is to study for the first time the in vivo anti-inflammatory, antidiabetic and acute toxicity effects of acetonic, methanolic and aqueous Hammada elegans Botsch extracts. METHODS: The acute toxicity test was performed according to the OECD method using single increasing doses (50-1500 mg/kg bw). The anti-inflammatory effect is investigated in Wistar rats by using the rat paw edema assay. The antidiabetic activity was evaluated in vivo using three tests: short-term test (in non-diabetic rats), starch-induced hyperglycemia test (in non-diabetic rats) and long-term alloxan test (experimental diabetes). RESULTS: The acute toxicity results show no deaths in rats and no clinical signs of toxicity. The anti-inflammatory effects showed that all extracts significantly inhibit rat paw edema (EC50 less than 345.51 ± 0.29 mg/kg bw). Therefore, the acetonic extract (EC50 = 157.45 ± 0.33 mg/kg bw) had the more active anti-inflammatory activity than that of the standard inhibitor "Ibuprofen". In addition, the evaluation of the antidiabetic activities by three tests shows that: in, in the short-term test, there was no important decrease in normal rats glucose rate, while in the starch-induced hyperglycemia test, the aqueous extract decreased significantly hyperglycemia (57.21 ± 1.24 mg AEAC / kg bw) compared to all tested extracts. While in the long-term test, the acetone extract significantly decreased hyperglycemia (9.18 ± 0.72 mg GEAC / kg bw) compared to all the tested extracts. CONCLUSIONS: Hammada elegans Botsch extracts seem to have therapeutic opportunities for the treatment of the inflammation and diabetes.

8.
Mol Cell Probes ; 58: 101733, 2021 08.
Article in English | MEDLINE | ID: mdl-33957269

ABSTRACT

The two important targets to treat gout disease are (1) control the hyperuricemia by the inhibition of Xanthine Oxidase (XO) and (2) treatment of acute attacks of gout by the use of anti-inflammatory drugs. It is important to distinguish between therapy to manage hyperuricemia and to reduce acute inflammation. While reducing hyperuricemia is resolved very slowly with available drugs, gout symptoms like pain and inflammation may become persistent. The objective of this study is to find a relevant treatment with a beneficial double effect. (1) As an anti-inflammatory, analgesic, and antipyretic effect and (2) as XO inhibitory effect, which is the main objective of this study. We investigated the effect of five non-steroidal anti-inflammatory drugs (NSAIDs) against human and bovine milk xanthine oxidases (HXO and BXO) using the double enzyme detection method (DED) and molecular docking with the Autodock vina program. in vitro results show that the NSAIDs give an important inhibition to HXO and BXO with an IC50 of 2.04 ± 0.13 µg/ml, 2.75 ± 0.23 µg/ml, 1.45 ± 0.19 µg/ml, 0.31 ± 0.13 µg/ml and 1.27 ± 0.11 µg/ml, for HXO, and 2.96 ± 0.27 µg/ml, 9.46 ± 0.13 µg/ml, 6.21 ± 1.17 µg/ml, 0.83 ± 0.11 µg/ml, and 3.48 ± 0.13 µg/ml, for BXO, for respectively, Naproxen, Ibuprofen, Diclofenac, Indomethacin, and Celecoxib. Testing the inhibitory activity of these drugs on both XOs shows an important inhibition, especially from Indomethacin, which could be a promising lead compound for reducing acute inflammation and at the same time controlling hyperuricemia.


Subject(s)
Enzyme Inhibitors , Xanthine Oxidase , Anti-Inflammatory Agents/pharmacology , Enzyme Inhibitors/pharmacology , Humans , Molecular Docking Simulation , Plant Extracts
9.
Curr Comput Aided Drug Des ; 17(3): 360-377, 2021.
Article in English | MEDLINE | ID: mdl-32116197

ABSTRACT

OBJECTIVE: The present study is carried out to screen the anticholinesterase effect of the total alkaloids of L. sativum seeds and other plants, and studied the ability of Lepidine B & E to inhibit AChE, BuChE, BACE, and MAGL. Hence, determining the main interactions in the inhibitorenzyme complex. METHODS: Inhibitory effect of Lepidium sativum, Juniperus phoenicea and Juniperus oxycedrus extracts on acetylcholinesterase using the Ellman method was investigated with Donepezil as the positive control. A molecular docking study is achieved using Autodock Vina. The structures of target molecules Lepidine B & E and the four enzymes were obtained from the PubChem database and Protein databank. RESULTS: Alkaloidal extract of Lepidium sativum and ethyl acetate extracts of Juniperus phoenicea and Juniperus oxycedrus exhibit a strong acetylcholinesterase inhibitory activity with IC50 values of 0.59 ± 0.04, 0.57 ± 0.00 and 0.49 ± 0.00 mg/mL, respectively using Donepezil <0.25 mg/mL as a positive control. The major components of alkaloids of L. sativum, Lepidine B & E bind tightly to AChE and BuChE as much as galantamine and donepezil. We suggest that Lepidine B is a noncompetitive inhibitory by interacting with PAS of AChE and BuChE, therefore it is capable to prevent the HuAChE-induced Aß aggregation. All the complexes of Lepidine B &E with the four enzymes show significant, several and different interactions. CONCLUSION: Our current study indicates that Lepidine B & E are promising anti-AD drugs and might become drug candidates to prevent Alzheimer's disease due to their multiple roles as potent inhibitors for AChE, BuChE, BACE, and MAGL. Indeed, they could inhibit Aß fibrillogenesis. No previous results about the inhibitory effect of Lepidine B & E on the AChE, BuChE, ß secretase, and monoacylglycerol lipase were reported.


Subject(s)
Alkaloids/pharmacology , Alzheimer Disease/drug therapy , Cholinesterase Inhibitors/pharmacology , Imidazoles/therapeutic use , Plant Extracts/pharmacology , Acetylcholinesterase/drug effects , Alkaloids/chemistry , Alkaloids/isolation & purification , Alkaloids/therapeutic use , Alzheimer Disease/enzymology , Amyloid Precursor Protein Secretases/antagonists & inhibitors , Aspartic Acid Endopeptidases/antagonists & inhibitors , Butyrylcholinesterase/drug effects , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/isolation & purification , Donepezil/pharmacology , Humans , Imidazoles/chemistry , Imidazoles/isolation & purification , Inhibitory Concentration 50 , Juniperus/chemistry , Lepidium sativum/chemistry , Molecular Docking Simulation , Monoacylglycerol Lipases/antagonists & inhibitors , Plant Extracts/administration & dosage , Plant Extracts/chemistry , Seeds
10.
J Ethnopharmacol ; 265: 113329, 2021 Jan 30.
Article in English | MEDLINE | ID: mdl-32889035

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Pistacia atlantica (wild pistachio) belongs to the Anacardiaceae family, and growing from the Mediterranean basin to central Asia, especially in Iran, Turkey, Iraq and Saudi Arabia where it is extensively used in traditional medicine for a wide range of ailments related to relieving upper abdominal discomfort and pain, dyspepsia and peptic ulcer. OBJECTIVE: Despite the diverse biological activities of P. atlantica, there is no current review summarizing medicinal properties of its subspecies, including cabulica, kurdica and mutica. Thus, this paper aims to explore the current understanding of the chemical, pharmacological, and biochemical properties of the extracts and the main active constituents found in each subspecies of this plant. METHODS: Peer-reviewed articles, using "Pistacia atlantica" as search term (″all fields″), were retrieved from Scifinder, Pubmed, Science direct, Wiley, Springer, ACS, Scielo, Web of Science and other web search instruments (Google Scholar, Yahoo search). Papers published until July 2020 are considered. In addition, various books were consulted that contained botanical and ethnopharmacological information. The information provided in this review is based on peer-reviewed papers in English and French. RESULTS: Phytochemical studies have shown the presence of numerous valuable compounds, including volatile compounds, flavonoids, phenolic compounds, fatty acids, tocopherols and phytosterols. P. atlantica contains also minerals and trace elements, like iron, lead, copper, potassium, sodium and calcium; fatty acids, like oleic, linoleic, and palmitic acid; fat-soluble vitamins, such as α, ß, γ and δ tocopherols; phytosterols, like betasitosterol, stigmasterol, campesterol and Δ5-avenasterol. Crude extracts and isolated compounds from P. atlantica show a wide range of pharmacological properties, such as antimicrobial, antifungal, anti-inflammatory, analgesic, antinociceptive, wound healing, anticancer, cytotoxic, anticholinesterase, antidiabetic, hepatoprotective, urease inhibition, antihypertension, nipple fissure healing, antileishmanial and antiplasmodial activities. However, there are no reports summarizing the P. atlantica bioactivity, its therapeutic value, and the roles played by each of the numerous phytoconstituents. CONCLUSION: Many traditional uses of P. atlantica and its subspecies have now been confirmed by pharmacologic research. Systematic phytochemical investigation of the P. atlantica subspecies and the pharmacological properties, especially the mechanisms of action and toxicology, to illustrate their ethnomedicinal use, to explore the therapeutic potential and support further health-care product development, will undoubtedly be the focus of further research. Therefore, detailed and extensive studies and clinical evaluation of P. atlantica subspecies should be carried out in future for the safety approval of therapeutic applications.


Subject(s)
Medicine, Traditional , Pistacia/chemistry , Plant Extracts/pharmacology , Animals , Ethnobotany , Ethnopharmacology , Humans , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Phytotherapy , Plant Extracts/chemistry
11.
Chem Biodivers ; 17(9): e2000117, 2020 Sep.
Article in English | MEDLINE | ID: mdl-32558253

ABSTRACT

The current study investigated the effect of developmental stages on the chemical composition and the antioxidant activity of fifteen crude oil samples obtained from Pistacia atlantica Desf. leaves, galls, and fruits. Twelve fatty acids were detected by GC/FID, linolenic acid (C18 : 3) was the major fatty acid detected in leaves crude oils that registered [41.73 % (P<0.05)] on the last stage. The best content of tocopherols and carotenoids was recorded at the last stage for leaves and galls oils, respectively, with values of [1.530±0.01, 0.52±0.01 (P<0.05) mg α-tocopherol equivalent/g DW] and [86.60±0.95, 69.15±0.13 (P<0.05) µg ß-carotene equivalent/g DW]. For fruits oils, the content varied depending on the levels of fruits maturation. The results from DPPH, FRAP, and ABTS assays revealed that the antioxidant activity increased with the increasing content of tocopherols and carotenoids in leaves and galls oils during development stages, and varied for fruits oils depending on the ripening stages. Moreover, according to PCA analysis, the best phytoconstituent content and antioxidant activity were attributed to P. atlantica Desf. fruit's crude oils. Also, a strong relationship was found between the antioxidant activity and bioactive phytochemical components, such as tocopherols, carotenoids, and omega-three fatty acid, which confirmed that P. atlantica Desf. crude oils present a valuable source of natural antioxidant that could be used for pharmaceutical and food industries purposes.


Subject(s)
Antioxidants/pharmacology , Carotenoids/pharmacology , Fatty Acids/pharmacology , Petroleum/analysis , Pistacia/chemistry , Tocopherols/pharmacology , Antioxidants/chemistry , Benzothiazoles/antagonists & inhibitors , Biphenyl Compounds/antagonists & inhibitors , Carotenoids/chemistry , Fatty Acids/chemistry , Fluorescence Recovery After Photobleaching , Fruit/chemistry , Picrates/antagonists & inhibitors , Plant Leaves/chemistry , Sulfonic Acids/antagonists & inhibitors , Tocopherols/chemistry
12.
Article in English | MEDLINE | ID: mdl-30987578

ABSTRACT

BACKGROUND AND OBJECTIVE: The present paper aims to study the inhibition of Candida albicans growth as candidiasis treatment, using seeds of Lepidium sativum as source. METHODS: In vitro assays were carried out on the antifungal activity of three kinds of extracts from L. sativum seeds against four strains of C. albicans, then testing the same phytochemicals on the inhibition of Lipase (LCR). A new in silico study was achieved using molecular docking, with Autodock vina program, to find binding affinity of two important and major lepidine alkaloids (lepidine E and B) towards the four enzymes secreted by C. albicans as target drugs, responsible of vitality and virulence of this yeast cells: Lipase, Serine/threonine phosphatase, Phosphomannose isomerase and Sterol 14-alpha demethylase (CYP51). RESULTS: The results of the microdillution assay show that the hexanic and alkaloidal extracts have an antifungal activity with MICs: 2.25 mg/ml and 4.5mg/ml, respectively. However, Candida rugosa lipase assay gives a remarkable IC50 values for the hexanic extract (1.42± 0.04 mg/ml) followed by 1.7± 0.1 and 2.29 ± 0.09 mg/ml of ethyl acetate and alkaloidal extracts respectively. The molecular docking confirms a significant correlation between C. albicans growth and inhibition of crucial enzymes involved in the invasion mechanism and cellular metabolisms, for the first time there were an interesting and new positive results on binding modes of lepidine E and B on the four studied enzymes. CONCLUSION: Through this work, we propose Lepidine B & E as potent antifungal drugs.


Subject(s)
Antifungal Agents/pharmacology , Candida albicans/drug effects , Enzyme Inhibitors/pharmacology , Fungal Proteins/antagonists & inhibitors , Lepidium sativum , Molecular Docking Simulation , Plant Extracts/pharmacology , Seeds , Antifungal Agents/chemistry , Antifungal Agents/isolation & purification , Candida albicans/enzymology , Candida albicans/growth & development , Cytochrome P-450 Enzyme System/metabolism , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Fungal Proteins/chemistry , Fungal Proteins/metabolism , Lepidium sativum/chemistry , Lipase/antagonists & inhibitors , Lipase/metabolism , Mannose-6-Phosphate Isomerase/antagonists & inhibitors , Mannose-6-Phosphate Isomerase/metabolism , Molecular Targeted Therapy , Phosphoprotein Phosphatases/antagonists & inhibitors , Phosphoprotein Phosphatases/metabolism , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Protein Conformation , Seeds/chemistry , Structure-Activity Relationship , Virulence
13.
Chem Biodivers ; 16(11): e1900420, 2019 Nov.
Article in English | MEDLINE | ID: mdl-31529756

ABSTRACT

The widespread use of Deverra scoparia Coss. & Durieu in Algerian folk-medicine as a remedy can be relatively attributed to its total phenolic compounds. The current study aimed to provide a scientific basis for optimal collection and usage of Deverra scoparia Coss. & Durieu plant. Hence, 37 samples were gathered from nine sites in Algeria during two seasons 2016 and 2017, then exposed to a green extraction. Total phenolic (TPC), flavonoid (FC) and condensed tannins (CTC) content were estimated spectrophotometrically. The antioxidant activity was measured using five different methods, DPPH. , ABTS.+ , FRAP, CUPRAC and Fe2+ -chelating. The results have revealed considerable amounts of TPC varied from 804 to 1544 mg GAE/100 g dry matter, FC started from 187 up to 410 mg QE/100 g dry matter and CTC varied from 111 to 394 mg CE/100 g dry matter. The best IC50 values (µg/mL) of DPPH. , ABTS•+ , FRAP, CUPRAC and Fe2+ -chelating tests were 56.62, 5.41, 21.26, 52.93 and 78.10, respectively. Moreover, high correlations were found between CTC and most of the antioxidant tests. Hence, CTC are suggested to be the principal group of antioxidant activity in Deverra scoparia Coss. & Durieu extracts.


Subject(s)
Antioxidants/analysis , Flowers/chemistry , Methanol/chemistry , Phenols/analysis , Plant Extracts/analysis , Seeds/chemistry , Algeria , Antioxidants/pharmacology , Benzothiazoles/antagonists & inhibitors , Biphenyl Compounds/antagonists & inhibitors , Copper/chemistry , Iron Chelating Agents/chemistry , Phenols/pharmacology , Picrates/antagonists & inhibitors , Plant Extracts/pharmacology , Principal Component Analysis , Seasons , Sulfonic Acids/antagonists & inhibitors
14.
Article in English | MEDLINE | ID: mdl-30706829

ABSTRACT

BACKGROUND AND OBJECTIVE: Lipase inhibitors have gained great interest because they could help in the therapy of many diseases, however, unfortunately, only a few drugs are currently available on the market. Therefore, the aim of this work was to evaluate for the first time the lipase inhibition effect of Thapsia garganica extracts from seeds, leaves and roots. METHODS: Polyphenols and flavonoids contents were determined using spectrophotometric method. Inhibitory activity of ethyl acetate extracts from seeds, leaves and roots of T. garganica against Candida rugosa lipase was determined. To uncover the active constituents responsible for this anti-lipase activity, further investigations were performed by employing theoretical docking simulations, using AutoDock Vina program to discuss the nature of interactions and the inhibition mechanism by major bioactive compounds synthesized by this plant. RESULTS: Seeds, leaves and roots extracts of T. garganica showed appreciable contents of polyphenols and flavonoids which is most in seeds extract with 2.90±0.02mg GAE/gdw and 1.53±0.05mg QE/gdw, respectively. Hence, their inhibitory activities against Candida rugosa lipase were determined as IC50 of 1.19mg/ml, 1.96mg/ml and 1.87mg/ml, respectively. Docking simulations have shown that nortribolid and tribolid are best inhibitors for both lipases (Candida rugosa and human pancreatic lipases). CONCLUSION: Testing the anti-lipase activity of the ethyl acetate extracts of T. garganica revealed a potent lipase inhibition activity, which suggests the use of these molecules as anti-obesity drugs.


Subject(s)
Lipase/antagonists & inhibitors , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Thapsia/chemistry , Anti-Obesity Agents/chemistry , Anti-Obesity Agents/isolation & purification , Anti-Obesity Agents/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/pharmacology , Biological Assay , Flavonoids/chemistry , Flavonoids/isolation & purification , Flavonoids/pharmacology , Humans , In Vitro Techniques , Lipase/chemistry , Lipase/metabolism , Models, Molecular , Molecular Docking Simulation , Plant Extracts/chemistry , Plant Leaves/chemistry , Plant Roots/chemistry , Polyphenols/chemistry , Polyphenols/isolation & purification , Polyphenols/pharmacology , Seeds/chemistry
15.
Nat Prod Res ; 33(6): 875-878, 2019 Mar.
Article in English | MEDLINE | ID: mdl-29210306

ABSTRACT

In this study, total phenolic and flavonoid contents, acute toxicity and the antinociceptive activity of Artemisia campestris and Artemisia herba-alba, individually and in combination, were investigated using multiple forms of pain in animals. Our results have been shown that plants are relatively safe without clinical signs of toxicity in animals. Thus, extracts were presented high levels in phenolic and flavonoid contents. Artemisia decoctions with 100, 200, 400 mg/kg b-w studied dose, clearly attenuate chemical and thermal noxious stimuli in writhing, formalin and hot-plate tests, and significantly reduced paw oedema in formalin test. Additionally, binary combination forms exhibited a great improvement in intensity and amplitude of antinociceptive activity in comparison with both plants used individually by a relative interference with opioid system. Our findings suggested the central and peripheral analgesic properties and confirmed the folkloric medicinal use of these plants in pain symptom treatment.


Subject(s)
Acute Pain/drug therapy , Analgesics/pharmacology , Artemisia/chemistry , Plant Extracts/pharmacology , Animals , Artemisia/classification , Male , Mice , Pain Measurement , Plant Components, Aerial/chemistry , Rats
16.
J Pharm Biomed Anal ; 149: 547-556, 2018 Feb 05.
Article in English | MEDLINE | ID: mdl-29190580

ABSTRACT

The objective of this paper is to evaluate the variations in the ability of Pistacia atlantica leaves to inhibit enzymes linked to type 2 diabetes (α-amylase and α-glucosidase) and to hypertension (angiotensin converting enzyme-I (ACE-I)), depending on harvesting month, gender and growing region, as well as to identify the peaks in chromatographic fingerprints that potentially correspond to components with enzymatic inhibitory activities. In this study, LC fingerprints of P. atlantica leave extracts were developed. Peaks which were probably responsible for the anti-amylase, anti-glucosidase and anti-ACE-I activities were assigned. For the latter purpose, the relevant information was extracted, linking the chromatographic fingerprints with the activities using a linear multivariate calibration technique, i.e., Partial Least Squares (PLS) regression. Prior to the construction of the models, the fingerprints are aligned using a warping method, called Correlation Optimized Warping (COW). Besides COW, different other data pretreatment methods were applied and compared. Our findings revealed that the influence of the growing region and gender on the α-amylase, α-glucosidase and ACE-I inhibitory activities of P. atlantica leaves was less important than the harvest time. Thirteen common peaks were selected from the chromatograms and used as a dataset to model the biological activities. The peaks potentially responsible for the biological activity of the samples were indicated by studying the regression coefficients of the models. Seven peaks corresponding to possibly anti-amylase compounds were found, while 6 peaks were considered important for inhibiting the α-glucosidase activity. Furthermore, the regression coefficients of the hypertension model indicated eight peaks as being important for inhibiting the ACE-I activity. The contributions of individual phenolic compounds of P. atlantica leaves to the α-amylase, α-glucosidase and ACE-I inhibitory activities were also identified. This investigation showed that the extract of P. atlantica leaves provides a rational basis for the isolation and development of antidiabetic and antihypertensive agents.


Subject(s)
Angiotensin-Converting Enzyme Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors/pharmacology , Pistacia/chemistry , Plant Extracts/pharmacology , Chemistry, Pharmaceutical/instrumentation , Chemistry, Pharmaceutical/methods , Chromatography, High Pressure Liquid/methods , Diabetes Mellitus, Type 2/drug therapy , Geography , Glycoside Hydrolase Inhibitors/chemistry , Humans , Hypertension/drug therapy , Least-Squares Analysis , Models, Chemical , Phenols/chemistry , Phenols/pharmacology , Plant Extracts/chemistry , Plant Leaves/chemistry , Seasons , alpha-Amylases/antagonists & inhibitors
17.
Arch Microbiol ; 199(10): 1345-1356, 2017 Dec.
Article in English | MEDLINE | ID: mdl-28707037

ABSTRACT

The antifungal potency of the essential oils of Rhanterium adpressum was evaluated against four mycotoxigenic strains of the genus Fusarium. The essential oils were obtained, separately, by hydro-distillation of the aerial parts of R. adpressum (leaves and flowers). The parts were collected during the period of bloom (3 months) for 3 years. The GC-MS analysis revealed thirty-six compounds for the essential oils, divided into four classes of chemical compounds, with variable percentages according to the month of extraction. The monoterpene hydrocarbons form the main class in these oils. On the other hand, the highest percentages of the oxygenated compounds are observed in the samples collected during the month of May. The direct contact method was used to evaluate the antifungal activity of the essential oils. The activity can be attributed to their relatively high composition of oxygenated monoterpenes. Flowers extract showed strong inhibitory activity, with very interesting concentrations of IC50 and MIC for both tests on solid and liquid medium. The effect of these oils on the production of type B trichothecenes (TCTBs) was evaluated, showing a significant inhibitory effect on TCTBs production, for both extracts (leaves and flowers). The rates of inhibition were 66-97 and 76-100% of FX, 3-ADON and 15-ADON, respectively. The inhibition of fungal biomass and the production of TCTBs depended on the used concentration of the essential oils. These results suggest that the essential oils from R. adpressum are able to control the growth of the tested strains and their subsequent production of TCTB mycotoxins.


Subject(s)
Antifungal Agents/pharmacology , Asteraceae/metabolism , Fusarium/drug effects , Oils, Volatile/pharmacology , Plant Extracts/pharmacology , Flowers/metabolism , Fusarium/classification , Gas Chromatography-Mass Spectrometry , Microbial Sensitivity Tests , Monoterpenes/pharmacology , Mycotoxins/biosynthesis , Plant Leaves/metabolism , Trichothecenes/biosynthesis
18.
Pharm Biol ; 55(1): 1185-1194, 2017 Dec.
Article in English | MEDLINE | ID: mdl-28245729

ABSTRACT

CONTEXT: The widespread use of Pistacia atlantica Desf. ssp. (Anacardiaceae) in traditional medicine can be partly attributed to the content of its secondary metabolites, in particular, the phenolic compounds. OBJECTIVE: The effects of harvest period, growing region and gender on the phenolic compounds, flavonoids and condensed tannins contents were studied, as well as on the antioxidant activities of P. atlantica leaves in order to provide a scientific basis for optimal collection. MATERIALS AND METHODS: Leaves were collected monthly from April to October 2010 in two Algerian sites. The powdered leaves were used for preparing the ethyl acetate extract. Contents of total phenolics (TPC), flavonoids (FC) and condensed tannins (CTC) were determined spectrophotometrically. Antioxidant activity was evaluated through radical scavenging activity (RSA) of 2,2-diphenyl-1-picrylhydrazyl (250 µM) and the reducing power capacity (RPC) determination by K3Fe(CN)6 (1%). RESULTS: The TPC was found to vary from 79 ± 13 to 259 ± 8 mg gallic acid equivalents/g of dry weight (DW) during the study period. The RSA and RPC varied between 262 ± 18 and 675 ± 21 mg Ascorbic Acid Equivalent (AAE)/g DW, and from 259 ± 16 to 983 ± 20 mg AAE/g DW, respectively. A seasonal pattern was observed consisting of a decrease in TPC content and RPC from spring to autumn. The FC, CTC and RSA did not show a seasonal pattern. DISCUSSION AND CONCLUSION: Our findings showed that secondary metabolite content and antioxidant activities of P. atlantica leaves were more influenced by harvest time and growing region than by gender.


Subject(s)
Antioxidants/analysis , Flavonoids/analysis , Phenols/analysis , Pistacia , Plant Extracts/analysis , Seasons , Tannins/analysis , Plant Leaves , Sex Factors
19.
Nat Prod Commun ; 10(10): 1723-8, 2015 Oct.
Article in English | MEDLINE | ID: mdl-26669112

ABSTRACT

Pistacia atlantica fruit oil has been used for a long time by local populations for culinary and medicinal purposes. In this study, the fatty acid composition and tocopherol content were determined in twelve samples of P. atlantica fruit oil at three stages of maturation (immature, intermediate maturity and mature) collected in three different sites from the region of Laghouat. The results indicated a significant difference between the oil of mature fruits (green and black) and the immature ones (light red), which were distinguished by richness in unsaturated fatty acids and tocopherols. The oil from fruits of intermediate maturity (dark red) seems to combine these properties with those of the mature group, including oil yields. Such data emphasize the value of this oil, which needs further investigation.


Subject(s)
Fatty Acids/chemistry , Fruit/chemistry , Pistacia/chemistry , Plant Oils/chemistry , Tocopherols/chemistry , Algeria
20.
Nat Prod Res ; 29(20): 1945-9, 2015.
Article in English | MEDLINE | ID: mdl-25707439

ABSTRACT

The essential oils (EOs) of unripe galls (from male and female plants) of a total number of 52 samples of Pistacia atlantica collected from different regions in Algeria were analysed by GC/MS and GC. The yields of the extraction of the EO by hydrodistillation vary from low to high values (0.08-1.89% v/w). The results of both methods of principal component analysis and hierarchical ascendant classification revealed the presence of two different chemotypes: α-pinene chemotype and α-pinene/sabinene/terpinen-4-ol chemotype.


Subject(s)
Oils, Volatile/chemistry , Pistacia/chemistry , Plant Oils/chemistry , Plant Tumors , Algeria , Bicyclic Monoterpenes , Ecotype , Gas Chromatography-Mass Spectrometry , Monoterpenes/chemistry
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