Dinebra retroflexa Herbal Phytotherapy: A Simulation Study Based on Bleomycin-Induced Pulmonary Fibrosis Retraction Potential in Swiss Albino Rats.

Background and Objectives: Fibrotic lung disease is one of the main complications of many medical conditions. Therefore, the use of anti-fibrotic agents may provide a chance to prevent, or at least modify, such complication. The aim of this study was to evaluate the protective pulmonary anti-fibrotic and anti-inflammatory effects of Dinebra retroflexa. Materials and methods: Dinebra retroflexa methanolic extract and its synthesized silver nanoparticles were tested on bleomycin-induced pulmonary fibrosis. Pulmonary fibrosis was induced by intratracheal instillation of bleomycin (5 mg/5 mL/kg-Saline) as a supposed model for induced lung fibrosis. The weed evaluation was performed by intratracheal instillation of Dinebra retroflexa methanolic extract and its silver nanoparticles (35 mg/100 mL/kg-DMSO, single dose). Results: The results showed that both Dinebra retroflexa methanolic extract and its silver nanoparticles had a significant pulmonary fibrosis retraction potential, with Ashcroft scores of three and one, respectively, and degrees of collagen deposition reduction of 33.8 and 46.1%, respectively. High-resolution UHPLC/Q-TOF-MS/MS metabolic profiling and colorimetrically polyphenolic quantification were performed for further confirmation and explanation of the represented effects. Such activity was believed to be due to the tentative identification of twenty-seven flavonoids and one phenolic acid along with a phenolic content of 57.8 mg/gm (gallic acid equivalent) and flavonoid content of 22.5 mg/gm (quercetin equivalent). Conclusion: Dinebra retroflexa may be considered as a promising anti-fibrotic agent for people at high risk of complicated lung fibrosis. The results proved that further clinical trials would be recommended to confirm the proposed findings.

Effect οf elicitοrs οn cell suspensiοn culture οf Urginea maritima L. tοwards prοductiοn οf prοscillaridin A.

BACKGROUND: Urginea maritima (L.f.) Baker (Hyacinthaceae) is a perennial bulbous medicinal plant that is currently at risk of extinction. Squill (white sea onion) is an analogous cardiotonic to digitalis. The purpose of the current work was to assess the optimal growth conditions for Urginea cells to synthesize the cardiac glycoside proscillaridin A by involving illumination, carbon source, methyl jasmonate (MJ), and culture system. RESULTS: When cells were cultured for 28 days at 21 ± 2 ∘C in the dark on Murashige and Skoog (MS) media containing 1 mg/L 2, 4-D and 0.5 mg/L Kin and 30 g/L sucrose, the cell proliferation, and proscillaridin A synthesis were effectively controlled. At low concentrations, MJ stimulated the synthesis of proscillaridin A (PsA). High-performance liquid chromatography (HPLC) analysis of suspension extracts demonstrated that the callus maintained in MS media enriched with 1 mg/L 2, 4-D and 0.5 mg/L Kin yielded a greater formation of Proscillaridin A (141.31 mg/g DW) than untreated plants. CONCLUSIONS: The results indicate that in vitro cultures of U. maritima may be an excellent source of proscillaridin A. Moreover, it is one of the most important cardiac glycoside, which has been found to exhibit anticancer activities. Suspension cultures of Urginea cells could be as highly productive as a callus culture.

Optimizing ectoine biosynthesis using response surface methodology and osmoprotectant applications.

PURPOSE: Numerous applications of compatible salts (osmolytes) as ectoine in food and pharmaceutical industries have been intensively increased nowadays. Decreasing the cost of industrial production of ectoine using low-cost cultivation media and improving the yield through modeling procedures are the main scopes of the present study. METHODS: Three statistical design experiments have been successfully applied for screening the parameters affecting the production process, studying the relations among parameters and optimizing the production using response surface methodology. RESULTS: A novel semi-synthetic medium based on hydrolyzed corn gluten meal has been developed to cultivate moderate halophilic bacterial strains; Vibrio sp. CS1 and Salinivibrio costicola SH3, and support ectoine synthesis under salinity stress. Two regression equations describe the production process in the new medium have been formulated for each bacterial strain. Response surface optimizer of the central composite model predicts the maximum ectoine production is achieved at incubation time; 63.7 h, pH; 7.47 and salinity; 7.27% for Vibrio sp. CS1 whereas these variables should be adjusted at 56.95 h, 7.089 and 10.34%; on the same order regarding Salinivibrio costicola SH3. In application studies, 50 µg ectoine decreases RBCs hemolysis due to streptolysin O toxin by 21.7% within ten minutes. In addition, 2% ectoine succeeds to increase the viability of lactic acid bacteria in Yogurt as a classic example of functional food during the storage period (7 days). CONCLUSION: The present study emphasizes on modeling the process of ectoine production by halophilic bacteria as well as its activity as a cryoprotectant agent.

Chemical Composition and Antimicrobial Activities of Essential Oils of Some Coniferous Plants Cultivated in Egypt.

Family Cupressaceae is the largest coniferous plant family. Essential oils of many species belonging to family Cupressaceae are known to have several biological activities specially antimicrobial activity. The essential oils from aerial parts of Calocedrus decurrens Torr., Cupressus sempervirens stricta L. and Tetraclinis articulata (Vahl) Mast. were prepared by hydrodistillation. The chemical composition of the essential oils has been elucidated by gas chromatography-mass spectroscopy analysis. The prepared essential oils were examined against selected species of Gram-positive, Gram-negative bacteria and Candida species. Broth dilution methods were used to detect minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC). Sixteen compounds were identified in the essential oils of both Calocedrus decurrens and Cupressus sempervirens L. and fifteen compounds were identified in the essential oil of Tetraclinis articulata. δ-3-Carene (43.10%), (+)-Cedrol (74.03%) and Camphor (21.23%) were the major constituents in the essential oils of Calocedrus decurrens, Cupressus sempervirens L. and Tetraclinis articulata, respectively. The essential oils showed strong antimicrobial activities against the selected microorganisms in concentration range 0.02 3- 3.03 µL/mL. This study could contribute to the chemotaxonomic characterization of family Cupressaceae. In addition, it proved that the essential oils under investigation possess potential antimicrobial properties.

New triterpenoidal saponins from Koelreuteria paniculata.

Bioassay guided fractionation and chemical investigation of the ethanolic extract of the aerial parts of Koelreuteria paniculata Laxm. (Sapindaceae), resulted in the isolation and identification of three new triterpenoid saponins 1-3 named Paniculatosoid A-C, along with eleven known compounds. The structures of the isolated compounds were elucidated using 1D and 2D NMR experiments, HRESIMS, and comparison with literature data. The occurrence of tridesmosidic saponin is reported for the first time from family Sapindaceae, as well as it is rarely found in natural saponins. Compounds 4-13 were evaluated for their antibacterial, antifungal, antimalarial and antileishmanial activities. Compound 12 showed weak antibacterial activity against Escherichia coli with an IC50 value of 101 µM. Compounds 12 and 13 showed antimalarial activity against chloroquine-sensitive (D6) Plasmodium falciparum protozoan with IC50 values of 6.46 and 6.95 µM, and against chloroquine-resistant (W2) Plasmodium falciparum protozoan with IC50 values of 9.34 and 4.18 µM.

Asphodosides A-E, anti-MRSA metabolites from Asphodelus microcarpus.

Bioassay guided fractionation of the ethanolic extract of Asphodelus microcarpus Salzm. et Viv. (Xanthorrhoeaceae or Asphodelaceae) resulted in isolation of five compounds identified as asphodosides A-E (1-5). Compounds 2-4 showed activity against methicillin resistant Staphylococcus aureus (MRSA) with IC50 values of 1.62, 7.0 and 9.0µg/mL, respectively. They also exhibited activity against Staphylococcus aureus (non-MRSA) with IC50 values of 1.0, 3.4 and 2.2µg/mL, respectively. The structure elucidation of isolated metabolites was carried out using spectroscopic data (1D and 2D NMR), optical rotation and both experimental and calculated electronic circular dichroism (ECD).

Phenolic content of some selected Lamiaceous Egyptian medicinal plants: antioxidant potential and ecological friend mosquito-larvicldal.

Phenol compounds are naturally occurring biologically active compounds existing in all plants had received major medical concern so development in research focused on their extraction, identification and quantification have occurred over the last 25 years; they constitute an important source of antioxidants and were used to help human body to reduce oxidative damage. Mosquitos-borne diseases constitute one of the major health problems worldwide. Control strategies involving pinpointing natural ecological friend, cheap and safe mosquitocides, mainly larvicides to stop their life cycle. Quantitative estimation of total phenol, flavonoids, phenylethanoid and iridoid contents of sixteen selected Lamiaceous Egyptian plants for screening of their antioxidant and mosquito larvicidal effects was carried out. The results showed that the most suitable medicinal plants used as antioxidants were Lavendula dentata L., Thymus capitatus L. and Thymus bovei Benth., which contain adequate mixture of total phenol, flavonoid and phenylethanoid contents, with distinct larvicidal effect in a descending order was T. capitatus L., T. bovei Benth. and L. dentata L. by their adequate mixture of total phenol, flavonoid, iridoid and phenylethanoid glycoside content.

Antileukemic α-pyrone derivatives from the endophytic fungus Alternaria phragmospora.

Four new (1-4) and two known (5 and 6) α-pyrone derivatives have been isolated from Alternaria phragmospora, an endophytic fungus from Vinca rosea, leaves. The isolated compounds were chemically identified to be 5-butyl-4-methoxy-6-methyl-2H-pyran-2-one (1), 5-butyl-6-(hydroxymethyl)-4-methoxy-2H-pyran-2-one (2), 5-(1-hydroxybutyl)-4-methoxy-6-methyl-2H-pyran-2-one (3), 4-methoxy-6-methyl-5-(3-oxobutyl)-2H-pyran-2-one (4), 5-(2-hydroxyethyl)-4-methoxy-6-methyl-2H-pyran-2-one (5), and 5-[(2E)-but-2-en-1-yl]-4-methoxy-6-methyl-2H-pyran-2-one (6). Compounds 2 and 4 showed moderate antileukemic activities against HL60 cells with IC50 values of 2.2 and 0.9 µM and against K562 cells with IC50 values of 4.5 and 1.5 µM, respectively.

Nigrosphaerin A a new isochromene derivative from the endophytic fungus Nigrospora sphaerica.

Nigrosphaerin A, a new isochromene derivative (1), was isolated from the endophytic fungus Nigrospora sphaerica and chemically identified as 3-(3,4-dihydroxyphenyl)-4,6,8-trihydroxy-1H-isochromen-1-one-6-O-ß-d-glucopyranoside. In addition nineteen known compounds (2-20) were isolated from the same fungus and chemically identified. Compounds (1-3, 5, and 7-16) were isolated for the first time from this fungus. In vitro antileukemic, antileishmanial, antifungal, antibacterial and antimalarial activities of (1-20) were examined. Compounds 5, 7, 9 and 10 showed good antileukemic activity against HL60 cells with IC50 values of 0.03, 0.39, 0.2 and 0.4 µg/mL, respectively and against K562 cells with IC50 values of 0.35, 0.35, 0.49 and 0.01 µg/mL, respectively. Compounds 3, 4 and 6 showed moderate antileishmanial activity with IC50 values of 30.2, 26.4 and 36.4 µg/ml, respectively. Compound 7 showed moderate antifungal activity against Cryptococcus neoformans with IC50 value of 14.8 µg/mL.

Isolation and characterization of new secondary metabolites from Asphodelus microcarpus.

Phytochemical study of the ethanolic extract of Asphodelus microcarpus Salzm. et Viv. (Asphodelaceae) resulted in the isolation of two new compounds, methyl-1,4,5-trihydroxy-7-methyl-9,10-dioxo-9,10-dihydroanthracene-2-carboxylate (1), and (1R) 3,10-dimethoxy-5-methyl-1H-1,4-epoxybenzo[h]isochromene (2) as well as three known compounds; 3,4-dihydroxy-methyl benzoate (3), 3,4-dihydroxybenzoic acid (4), and 6-methoxychrysophanol (5). Compound 1 showed a potent activity against methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus aureus with IC50 values of 1.5 and 1.2 µg/mL, respectively. Compound 3 showed antileishmanial activity with an IC50 value of 33.2 µg/mL. Compound 2 is the first isochromene possessing a highly strained 1,4-epoxy moiety. The structure elucidation of isolated metabolites was carried out using spectroscopic data, the absolute configuration of 2 based on optical rotation and electronic circular dichroism experiments and calculations.

Biologically active secondary metabolites from Asphodelus microcarpus.

Bioassay guided fractionation of the ethanolic extract of Asphodelus microcarpus Salzm.et Vivi (Asphodelaceae) resulted in the isolation of one new metabolite, 1,6-dimethoxy-3-methyl-2-naphthoic acid (1) as well as nine known compounds: asphodelin (2), chrysophanol (3), 8-methoxychrysophanol (4), emodin (5), 2-acetyl-1,8-dimethoxy-3-methylnaphthalene (6), 10-(chrysophanol-7'-yl)-10-hydroxychrysophanol-9-anthrone (7), aloesaponol-III-8-methyl ether (8), ramosin (9) and aestivin (10). The compounds were identified by 1D and 2D NMR and HRESIMS. Compounds 3, 6 and 10 were isolated for the first time from this species. Compounds 3 and 4 showed moderate to weak antileishmanial activity with IC50 values of 14.3 and 35.1 microg/mL, respectively. Compound 4 exhibited moderate antifungal activity against Cryptococcus neoformans with an IC50 value of 15.0 microg/mL, while compounds 5, 7 and 10 showed good to potent activity against methicillin resistant Staphylococcus aureus (MRSA) with IC50 values of 6.6, 9.4 microg/mL and 1.4 microg/mL respectively. Compounds 5, 8 and 9 displayed good activity against S. aureus with IC50 values of 3.2, 7.3 and 8.5 microg/mL, respectively. Compounds 7 and 9 exhibited a potent cytotoxic activity against leukemia LH60 and K562 cell lines. Compound 10 showed potent antimalarial activities against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum with IC50 values in the range of 0.8-0.7 microg/mL without showing any cytotoxicity to mammalian cells.

Phenolic content, antioxidant potential and Aedes aegyptii ecological friend larvicidal activity of some selected Egyptian plants.

Polyphenols constitute a distinct group of natural compounds of medicinal importance exhibiting wide range of physiological activities as antioxidant, immunestimulant, antitumor and antiparasitic. Yellow fever and dengue fever are mosquito-borne infectious diseases transmitted by Aedes aegyptii, the presence of yellow fever in Sudan and dengue fever in Saudi Arabia are threats to Egypt with the reemerging of Ae. aegyptii in Southern Egypt, larvae control is feasible than flying adults. This work was conducted targeting estimation of the relative levels of total phenolic content, antioxidant potential and larvicidal activity of 110 selected Egyptian plants. The highest total phenolic contents were estimated in aqueous extracts of Coronilla scorpioides L., Forsskaolea tenacissima L., Crataegus sinaica Boiss., Pistacia khinjuk Boiss. and Loranthus acacia Benth.; they were 916.70 +/- 4.80, 813.70 +/- 4.16, 744.90 +/- 4.93, 549.00 +/- 3.93& 460.80 +/- 4.02 mg% while those of methanol extracts were estimated in Coronilla scorpioides, Forsskaolea tenacissima, Crataegus sinaica, Loranthus acacia and Pistacia khinjuk, they were 915.60-4.86, 664.60 +/- 4.16, 659.30 +/- 4.80, 590.80 +/- 4.49 & 588.00 +/- 3.85 mg% respectively. Investigation of the antioxidant potentials revealed that the most potent plants were Co-ronilla scorpioides, Forsskaolea tenacissima, Crataegus sinaica, Pistacia khinjuk and Loranthus acacia with calculated values of 454.80 +/- 4.83, 418.4 +/- 4.16, 399.10 +/- 4.90, 342.5 +/- 2.72 & 239.7 +/- 2.91% for aqueous extracts and 452.9 +/- 4.94, 389.6 +/- 4.6, 378.48 +/- 3.84, 352.3 +/- 3.06 & 346.5 +/- 2.98% for methanol extracts respectively while screening of larvicidal activity proved that Coronilla scorpioides, Forsskaolea tenacissima, Crataegus sinaica, Pistacia khinjuk and Loranthus acacia exhibited highest potency calculated as 22.53 +/- 2.01, 23.85 +/- 2.07, 28.17 +/- 2.06, 31.60 +/- 2.93 & 39.73 +/- 4.58 mg% aqueous extracts and 18.53 +/- 1.95, 18.8 +/- 1.67, 20.17 +/- 1.85, 23.28 +/- 2.7 & 28.48 +/- 3.9 mg% methanol ones respectively.

Interrelation of antioxidant, anticancer and antilieshmania effects of some selected Egyptian plants and their phenolic constituents.

Medicinal plants are the most potential resource of new therapeutic agents. They are diverse, largely productive, biologically active and chemically unique; among their constituents "polyphenol compounds group" one of the main determinant factors in evaluating the pharmacological potentials i.e. polyphenols display an array of pharmacological properties such as antioxidant, immunostimulant, antitumor and antiparasitic effects. Cancer is a dreadful human disease, increasing with changing life style, nutrition and global warming while current available anticancer drugs cause serious side effects in most instances. Several reports suggested the relationship between antioxidant, anticancer and antiparasitic effects; they suggested that they act indirectly through promoting host resistance, restabilizing body equilibrim and conditioning body tissues in addition to their direct effect on certain parasites involved in cancer etiology. This work was conducted for estimation of total phenolic, flavonoids, phenylethanoid glycoside and iridoid content of twenty-three selected Egyptian plants as well as screening of their anticancer, antioxidant and antileishmanial effects, the overall gained results for suggest that the most suitable medicinal plant used as anticancer and antioxidant is Petrea volubilis L. which contain adequate mixture of total phenolic compounds 88.7 mg% and flavonoids 50.80 mg% and also suggest that flavonoid compounds are the category of phenolic compounds possess significant antioxidant and anticancer effects while the antilieshamnia screening revealed that Thymus decussatus Benth. extract exhibited the highest effect due to the presence of flavonoids and iridoids in adequate combination where iridoid compounds 201 mg% and flavonoid content was 128 mg%.

Comparative study of the flavonoids of some Verbena species cultivated in Egypt by using high-performance liquid chromatography coupled with ultraviolet spectroscopy and atmospheric pressure chemical ionization mass spectrometry.

Verbena rigida L., Verbena tenera Spreng. and Verbena venosa L. were investigated for their flavonoid content. Analysis was carried out by high-performance liquid chromatography coupled to diode array UV detection (LC-UV), using different techniques, also using post-column addition of shift reagents, afforded precise structural information about the position of the free hydroxyl groups in the flavonoid nucleus. LC-MS using atmospheric pressure chemical ionization (APCI) in the positive mode provided the molecular weight, the number of hydroxyl groups, the number of sugars and an idea about the substitution pattern of the flavonoid. On-line UV and MS data demonstrated the presence of orientin, vitexin, isovitexin, luteolin, luteolin 7-O-glucoside, apigenin 7-O-glucoside in addition to luteolin, chryseriol and apigenin aglycones in the three Verbena species with different concentrations. Quantitative determination of flavonoid content revealed the presence of 69.84 mg/g dry sample, 88.26 mg/g dry sample and 85.82 mg/g dry sample total flavonoid compounds in V. rigida L., V. tenera Spreng. and V. venosa L., respectively. The method developed for identification is useful for further chromatographic fingerprinting of plant flavonoids.

Antioxidant potential and phenolic acid content of certain cucurbitaceous plants cultivated in Egypt.

Many species belonging to Cucurbitaceae family have long been regarded as food, medicinal plants, or both. Preliminary phytochemical screening of Citrullus colocynthis L., Cucumis sativus L. and Momordica charantia L. herbs showed the presence of phenolic compounds. Quantitative analysis of total phenolic compounds using Folin-Ciocalteu reagent revealed the presence of 50.87 mg GAE g(-1), 56.58 mg GAE g(-1) and 42.36 mg GAE g(-1) in C. colocynthis L., C. sativus L. and M. charantia L. herbs, respectively. HPLC analysis of phenolic content showed the presence of chlorogenic acid (16.3 mg per 100g dry sample and 27.7 mg per 100 g(-1) dry samples in C. colocynthis L. and C. sativus L., respectively) and gallic acid (26.7 mg per 100 g dry sample) as a major phenolic acids in M. charantia L. herb. The antioxidant activity of the herb of plants under investigation was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and total antioxidant capacity was determined in terms of GAE. This study showed that C. sativus L. is the most active antioxidant, followed by C. colocynthis L., while M. charantia L. has the least antioxidant activity.