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Objective(s): The current study's objectives were to obtain different extracts and essential oils of Symphytum kurdicum and Symphytum asperrimum and to determine the chemical composition, as well as to evaluate free radical scavenging activity (IC50) and minimum bactericidal concentration (MBC), and the effect of liposomal formulation on antimicrobial properties. Materials and Methods: Air-dried powdered aerial parts of S. kurdicum and S. asperrimum were used. The antioxidant and antibacterial properties, essential oil compositions, total phenol, and flavonoid contents of different fractions were determined by DPPH test, disk diffusion assay, gas chromatography-mass spectrometry, Folin-ciocalteu reagent, and colorimetric assay method, respectively. The film hydration method was used to fabricate nanoparticles. Results: GC-MS analysis indicated that hexafarnesyl acetone was a major essential oil component. n-butanol and ethyl acetate extracts of S. kurdicum had the highest anti-oxidant activity. Extracts of both plants showed antimicrobial activity. The extracts' maximum inhibition zones against Staphylococcus epidermidis were established. A particle size analyzer detected the formulation size of 140 nm. The optimum formulation of liposomes contains the ratio of 75 mg lecithin, 25 mg cholesterol, and 50 mg herbal extract. Despite the nanoparticles' appropriate particle size, the liposomal extract's antimicrobial effect was lower than that of the free form. Conclusion: Our findings demonstrated that extracts have significant antibacterial and anti-oxidant activities, attributed to their bioactive constituents. [ABSTRACT FROM AUTHOR]

The genus Verbascum, belonging to the family Scrophulariaceae, has a significant center of diversity in Iran. Two of its species, V. erianthum and V. stachydiforme, originate in the Iranian-Turanian region, but no studies have been conducted on the induction of their hairy roots. This genus is a valuable source of biologically active compounds such as iridoid glycosides and flavonoids. Hairy root culture is a suitable technique for the production and accumulation of secondary metabolites. Three different studies were conducted to optimize the induction and establishment of hairy roots. In the first experiment, the influence of explant type (leaf and hypocotyl), six infection methods, and co-culture time (48 and 72 h) on the efficiency of hairy root induction was investigated. The results showed that the highest hairy root induction (68.18%) was observed in the leaf explants inoculated by direct infection with three wounds within 72 h co-culture time. In the second experiment, the effect of four Agrobacterium rhizogenes strains (ATCC 15834, A4, A7, and A13) and leaf age (14, 21, and 28 days) on transformation efficiency and some morphological traits examined in both species were studied. The high transformation efficiency of hairy root (80.55%) was detected in the 21-day-old leaf explant of V. erianthum species that was inoculated with the A13 strain. The transformed hairy root colons were confirmed by PCR using rolB gene-specific primers. To optimize hairy root growth and avoid tissue browning, hairy roots were cultured in various media containing different antioxidants and improver agents (including ascorbic acid, citric acid, and NAA). The results showed that the highest fresh growth index (20.42) and the lowest tissue browning (9%) as well as total phenol (8.51 mg GA/g DW), and total flavonoid content (4.42 mg QUE/g DW) were obtained in medium B5 with 1.5 mg/l NAA. [ABSTRACT FROM AUTHOR]

Phytochemical analysis of the methanolic and dichloromethane extracts of the aerial parts of Scutellaria pinnatifida led to the isolation of a phenylpropanoid, 1-o-feruloyl-ß-D-glucose (1), two known flavonoids including luteolin-7-o-glucoside (2) and apigenin-7-o-glucoside (3), three known phenylethanoid glycosides composed of phlomisethanoside (4), syringalide A (5), and verbascoside (6), and oleic acid (7). Isolation and structural elucidation of compounds were accomplished by HPLC and spectroscopic methods (UV, 1HNMR, 13C-NMR). The extracts were also evaluated for their radical scavenging activity and insecticidal property by 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay and contact toxicity method, respectively. Among the extracts, the methanol extract showed the most potent free radical scavenging activity with a RC50 value of 0.044 ± 0.350 mg/mL which could be attributed to the presence of the isolated phenolic compounds. In the case of insecticidal activity, the n-hexane extract displayed the most potent activity and caused 10%, 15%, and 40% mortality to Oryzaephilus mercator at the concentration of 5, 10, and 15 mg/mL after 4 h of exposure. [ABSTRACT FROM AUTHOR]

Purpose: Psyllium seeds are used in traditional herbal medicine to treat various disorders. Moreover, as a soluble fiber, psyllium has potential to stimulate bacterial growth in digestive system. We aimed to substitute alkali-extractable polysaccharides of psyllium for alginate in beads with second coat of poly-l-lysine to coat Lactobacillus acidophilus. Methods: Beads were prepared using extrusion technique. Poly-l-lysine as second coat was incorporated on optimum alginate/psyllium beads using immersion technique. Beads were characterized in terms of size, encapsulation efficiency, integrity and bacterial survival in harsh conditions. Results: Beads with narrow size distribution ranging from 1.85 ± 0.05 to 2.40 ± 0.18 mm with encapsulation efficiency higher than 96% were achieved. Psyllium concentrations in beads did not produce constant trend in bead sizes. Surface topography by SEM showed that substitution of psyllium enhanced integrity of obtained beads. Psyllium successfully protected the bacteria against acidic condition and lyophilization equal to alginate in the beads. Better survivability with beads of alginate/psyllium-poly-l-lysine was achieved with around 2 log rise in bacterial count in acid condition compared to the corresponding single coat beads. Conclusion: Alginate/psyllium (1:2) beads with narrow size distribution and high encapsulation efficiency of the bacteria have been achieved. Presence of psyllium produced a much smoother and integrated surface texture for the beads with sufficient protection of the bacteria against acidic condition as much as alginate. Considering the health benefits of psyllium and its prebiotic activity, psyllium can be beneficially replaced in part for alginate in probiotic coating. [ABSTRACT FROM AUTHOR]

Abstract: Shikonin and some of its derivative have approved apoptotic potential in different human cancer cell lines, and moreover have a dominant fluorescent emission at ?600nm. Here, to enhance shikonin-Act anti-proliferation properties, it was successfully incorporated in Solid Lipid Nanoparticles (SLNs) by the hot homogenization and entrapment efficiency (EE) of drug in SLNs was determined by ultrafiltration method. Scanning electron microscopy (SEM), laser diffractometry and zeta-sizer indicated that shikonin-Act-SLN were spherical and regular particles in the range of 70–120nm with polydispersity index (PI) of less than 0.10. The physical stability of shikonin-Act-loaded SLN in aqueous dispersion was evaluated in terms of size, PI, EE and drug leakage and the results showed that SLNs were stable upon storing three month. Long term in vitro release of the shikonin-Act was also approved. Cellular uptake of the shikonin-Act-SLN was examined by the in vitro fluorescent microscopy and facs flow cytometry analyses. In vivo rat imaging approved the penetrating capability of shikonin-Act-SLN emission through living tissues. In vitro anti-proliferation and genotoxicity evaluation by MTT and comet assay confirmed that shikonin-Act-SLN showed higher cytotoxic/antitumor potential than intact shikonin in terms of IC50 and DNA damage. This work provide sufficient information about improving of the therapeutic efficacy of the shikonin-Act, and also using of the shikonin-Act-SLN in bio-distribution studies during drug delivery investigation by incorporating in lipidic and colloidal drug delivery particles such as SLNs. [Copyright &y& Elsevier]

Purpose: Echinacea purpurea (L.) Moench is a member of the Asteraceae family and is traditionally used mainly due to its immunostimulatory properties. Various compounds including alkylamides and chicoric acid were reported as active ingredients of E. purpurea. Here, we aimed to prepare electrosprayed nanoparticles (NPs) containing hydroalcoholic extract of E. purpurea using Eudragit RS100 (EP-Eudragit RS100 NPs) to improve the immunomodulatory effects of the extract. Methods: The EP-Eudragit RS100 NPs with the different extract:polymer ratios and solution concentrations were prepared using the electrospray technique. The size and morphology of the NPs were evaluated using dynamic light scattering (DLS) and field emission-scanning electron microscopy (FE-SEM). To evaluate the immune responses, male Wistar rats were administrated with the prepared EP-Eudragit RS100 NPs and plain extract in the final dose of 30 or 100 mg/kg. The blood samples of the animals were collected and the inflammatory factors and complete blood count (CBC) were investigated. Results: In vivo studies indicated that the plain extract and EP-Eudragit RS100 NPs (100 mg/kg) significantly increased the serum level of tumor necrosis factor-α (TNF-α) and interleukin 1-β (IL1-β) whereas the EP-Eudragit RS100 NPs (30 mg/kg) significantly increased the number of white blood cells (WBCs) compared to the control group. Lymphocytes' count in all groups was increased significantly compared to the control group (P < 0.05) whereas other CBC parameters remained unchanged. Conclusion: The prepared EP-Eudragit RS100 NPs by electrospray technique caused significant reinforcement in the immunostimulatory effects of the extract of E. purpurea. [ABSTRACT FROM AUTHOR]

Introduction: In vitro antioxidant and antibacterial activity and volatile compositions of two Heracleum species (Apiaceae) including Heracleum transcaucasicum and Heracleum anisactis roots Essential Oil (EO) were investigated. Methods: The volatile compositions of EOs were analyzed by GC/Mass spectroscopy. To detect the antioxidant activity of essential oils TLC-bioautography and DPPH radical scavenging assay by spectrophotometry was performed. Additionally, the antibacterial activity of two essential oils were studied and compared against four pathogenic bacteria by agar disc diffusion method and MIC values of the EOs were determined using the broth dilution method. Results: Myristicin was the dominant component in both EOs. It was identified as 96.87% and 95.15% of the essential oil composition of H. transcaucasicum and H. anisactis roots, respectively. The TLC-bioautography showed antioxidant spots in both EOs and IC50 of H. anisactis and H. transcaucasicum EO was found to be 54 μg × ml (-1) and 77 μg × ml (-1), respectively. Regarding the antimicrobial assay, H. anisactis EO exhibited weak to moderate antibacterial activity against gram-positive bacteria and also Escherichia coli, whereas the essential oil from H. transcaucasicum was inactive. Conclusion: Based on the results from this study, both tested EOs mainly consist of myristicin. Despite the presence of myristicin with known antibacterial property, the EO from H. transcacausicum showed no antibacterial activity. Thus it is supposed that the biological activity of plants is remarkably linked to the extracts' chemical profile and intercomponents' synergistic or antagonistic effect could play a crucial role in bioactivity of EOs and other plant extracts. [ABSTRACT FROM AUTHOR]

Purpose: Two plant essential oils (EOs), including those from Heracleum transcaucasicum and Heracleum anisactiss (Umbeliferae) were studied to detect the chemical constituents and evaluated for their antibacterial activities against Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli and Pseudomonas aeruginosa. Methods: The EOs of H. transcaucasicum and H.anisactis (Apiacae) were obtained by hydrodistillation from aerial parts of the plants. The chemical analyses of the EOs were performed by GC/Mass spectrometry (GC/MS). Myristicin was found to be the principal constituent in both EOs. The susceptibility tests of EOs were performed by agar disc diffusion technique against Gram-positive and Gram-negative bacterial strains. Results: Eight components comprising 99.97% of the total essential oil of H. transcaucasicum and a total of three compounds accounting for 98.5% of the total oil composition of aerial parts of H. anisactis were identified, of which myristicin was the main compound in both EOs. The EOs of H. transcaucasicum and H. anisactis showed weak antibacterial property against Gram-positive strains of Staphylococcus aureus and Staphylococcus epidermidis with no measurable effect on Escherichia coli and Pseudomonas aeruginosa. Conclusion: Our GC-MS study revealed myristicin to be the major constituent of H. transcaucasicum and H.anisactis aerial parts. In spite of all the information available on the antibacterial properties of plants essential oils, we were not able to find significant antibacterial activity for both EOs. [ABSTRACT FROM AUTHOR]

Effects of four different salts, sodium chloride, sodium carbonate, calcium chloride and calcium carbonate used as additives in the water distillation process, on the essential oil quality and recovery of Mentha pulegium L. were evaluated. GC/MS analysis of oils revealed that salts application had considerable effects on the chemical constituents of distilled oil. Chemical constituents proportional variation was salt-dependant. Pulegone (39.1-45.3%) was the main common component of the oils with its high content detected in the control oil (hydrodistillation without any salt addition). Menthone (13.8-20.9%) was another major component with the highest amount related to calcium chloride. Compositional variation of other major components such as piperitenone oxide, isopulegol, 1,8-cineole, cis-piperitone epoxide and (E)-caryophyllene was greatly salt-dependant. [ABSTRACT FROM AUTHOR]

The composition of the essential oils obtained from the flowering aerial parts of two populations of Thymus pubescens, collected from Mishov-Dagh, was determined by the GC-MS analyses. A total of 18 compounds, representing about 95% of the total oils, were identified in both samples of the essential oils. The essential oils of these two populations showed the presence of high amounts of citronellol (42.0% and 42.6%), geranyl acetate (14.0 and 14.0%), geraniol (13.0 and 13.1%), citronellyl acetate (3.9 and 3.8%), L-linalool (7.8% and 7.9%), cis-nerodiol (5.9% and 5.5%) and citronellyl acetate (3.9% and 3.8%). However, in the published literature, carvacrol, thymol and p-cymene were reported to be the major compounds in T. pubescens. This significant difference in the composition of the essential oils was a clear evidence of chemical polymorphism with in the T. pubescens taxon, suggesting that these two populations of T. pubescens were in deed a new chemotype of this species, and the name Thymus pubescens Boiss. & Kotschy ex Celak chemotype Citronellol for this new chemotype has been proposed. The antibacterial and free-radical-scavenging properties of the essential oils of T. pubescens have also been evaluated. [ABSTRACT FROM AUTHOR]

The volatile oils of stem, umbels, fruits and roots of Astrodaucus orientalis (L.) Drude (Apiaceae) growing wild in Iran were obtained by hydro-distillation and analyzed by GC-MS. The main components of the oils from the stem were sabinene (23.1%), α-pinene (16.4%) and fenchyl-acetate (7.5%). Sabinene (25.6%), β-pinene (22.3%) and a-copaene (16.1%) were the main constituents of the volatile oils of the fruits. While α- copanene (26.1%), β-pinene (15.3%) and sabinene (13.7%) were the major components of the volatile oils of the umbels (flowers), that of the roots were mainly composed of anisole (37.9%), bornyl acetate (36.9%) and geranyl tiglate (11.4%). [ABSTRACT FROM AUTHOR]

Background: Stachys schtschegleevii (SSC) is a herbal medicine used to treat infections. To date, this is the first study aimed to investigate the effects of SSC tea on disease activity score (DAS), serum inflammatory biomarkers and matrix metalloproteinases (MMP-1 and MMP-3) among women with rheumatoid arthritis (RA). Methods: This pilot, triple-blind, randomized controlled clinical trial was conducted among forty-four women (age: 30–65 years) diagnosed with moderately active RA. Subjects were randomly assigned (1:1 ratio) into either SSC group (2.4 g/day SSC + 2.4 g/day black tea, n=22) or placebo (2.4 g/day black tea, n=22) for 8 weeks. Serum high-sensitivity C-reactive protein (hs-CRP), interleukin-1 beta (IL-1β), and MMPs were measured using ELISA. According to the American College of Rheumatology guideline considering hs-CRP, DAS28 was assessed. Results: Both study groups had respondent rates above 94.9%. The SSC intervention caused significant reductions in the number and the percent changes of the tender joints (SSC: −74.39% vs. placebo: −57.15%, mean differences= −0.77; P<0.05) and DAS28 [SSC: −32.44% vs. placebo: −22.32%, mean differences= −0.41, P<0.05). Unlike the intervention within SSC group that showed significant reductions in the mean serum levels of hs-CRP, IL-1β, and MMP-3, SSC caused significant MMP-3 reductions (SSC: −20.59% vs. placebo: 1.29%, P<0.05). Conclusion: The SSC intervention showed an appropriate clinical efficacy for female RA patients, accompanying remarkable reductions in the number of tender and swollen joints, DAS28, and serum levels of MMP-3. This can provide additional insights to the interventional studies controlling RA-related pathological and inflammatory outcomes. Trial registration Prospectively registered at the Iranian Registry of Clinical Trials (IRCT), linked to the WHO Registry Network (https://en.irct.ir/trial/11602, IRCT registration number: IRCT2015032011335N5, Registration date:2015-05-12). Key Points • Stachys schtschegleevii improved clinical outcomes and attenuated disease severity in RA patients. • Stachys schtschegleevii ameliorated serum level of MMP-3 in RA patients. [ABSTRACT FROM AUTHOR]

Gleditsia caspica Desf. (Caesalpinaceae) is traditionally used to treat diverse diseases. This research paper aims to investigate anti-proliferative properties and phytochemical compounds of methanolic extract from the pods of G. caspica. MTT test was used to measure in vitro anti-proliferative effect of the soxhlet-extracted methanolic extract of G.caspica pods with the concentration ranging from 25-1000 μg/ml against A549 cell line. The extract was applied to SPE, HPLC preparative system, and spectral analysis (1HNMR, 13CNMR, and UV) for fractionation, purification, and identification of phytoconstituents, respectively. The results indicated that the extract prevented proliferation of A549 cell line dependent on time and concentration. After 48 h and 72 h, there was a significant decrease in cell viability initiated from 100 and 500 (μg/ml) concentrations in comparison to untreated control. Phytochemical assessment of the extract resulted in two alkaloids, locustoside A and saikachinoside A, and four flavonoids quercetin-3,7-diglucoside, luteolin-4',7–diglucoside, quercetin-3-glucoside, and quercetin. This experiment was an activity-guided phytochemical study. In prior studies, quercetin and quercetin-3-β-D-glucoside showed in vitro inhibitory effect on proliferation of A549 cell line. However, the cytotoxic properties of the other identified compounds have not been reported. Cytotoxic properties of G.caspica was previously attributed to saponins, while isolated flavonoids and alkaloids could be responsible for the extract’s cytotoxic effects. This paper first explored cytotoxic activity of methanolic extract from the pods of G.caspica on A549 cell line and identified flavonoids and alkaloids of this plant. [ABSTRACT FROM AUTHOR]

• An eco-friendly stimuli-sensitive AgNPs synthesis was demonstrated. • Comparative synthesizing by two green and wet chemical methods were done. • Ag ions were reduced to AgNPs by aqueous-soluble polyols. • Colloidal AgNPs were synthesized with average particle sizes of 16–50 nm. • Different morphologies (polygonal, oval, spherical) were characterised. Through the current comparative study, colloidal silver nanoparticles (AgNPs) were synthesized with various morphologies and sizes using Prunus domestica (P-dom) extract and sodium citrate as green and chemical reducing agents, respectively. AgNPs were synthesized employing different concentrations of the reducing agents in an aqueous solution at various pH values (3–10) and temperatures (25–85 °C). The UV–visible absorption spectrum indicated characteristic SPR peaks of AgNPs at 380–450 nm. Fourier transform infrared spectroscopy revealed aqueous-soluble polyols (such as glycosides, phenols, and flavanols) participation in Ag ions reduction to the corresponding AgNPs at various pH values. The crystallinity of AgNPs was detected by an X-ray diffractometer. Different morphologies (polygonal, oval, and spherical) of the AgNPs with varying pH values were confirmed conducting transmission electron microscopy (TEM). Average particle sizes of 16–50 nm were determined using scanning electron microscopy, TEM, and dynamic light scattering assessments for AgNPs synthesized at various reaction conditions. This study is a demonstration for a facile, cheap, and eco-friendly stimuli-sensitive preparation of the AgNPs. [ABSTRACT FROM AUTHOR]

Astragalus is a well-known genus in Leguminosae family that represented more than 800 species growing in Iran. Nevertheless, there are a few reports on Astragalus plants endemic to Iran. The roots of Astragalus plants are rich in saponins, flavonoids and polysaccharides that possess various pharmacological activities. In the present study, chemical components, antioxidant and antibacterial activity of Astragalus chrysostachys Boiss. roots were evaluated. For determination of phytochemicals in Astragalus chrysostachys Boiss. roots, total hydroalcoholic extract was fractionated with ethyl acetate and n-butanol. Ethyl acetate extract as a flavonoid rich extract was analyzed using vacuum liquid chromatography and preparative TLC and consequently a major flavonoid was isolated. The structure of the obtained compound was elucidated with 1D and 2D NMR experiments. Additionally, the essential oil of the roots was analyzed by GC-MS. Antioxidant activity of all extracts was evaluated by different assays. Moreover, antibacterial activities of the extracts were also investigated against 2 Gram-positive and 2 Gram-negative bacteria using Micro-dilution Broth method. Apigenin-6, 8-di-C-glucoside was detected in ethyl acetate extract for the first time in genus Astragalus. In addition, m-tolualdehyde, acetophenone, croweac in were found to be characteristics of the volatile oil of roots. Ethyl acetate extracts revealed notable antioxidant activity in DPPH scavenging assay with IC50 value of 14.6 µg/mL. Evaluation of antibacterial activity on the tested extracts showed mild activity against Gram-positive bacteria. Since there have been no reports on Astragalus chrysostachys Boiss. to date, the present data might be promising for application of this plant derivatives in phytotherapeutic practice. [ABSTRACT FROM AUTHOR]

This research paper presents findings of an investigation about antibacterial effect of methanol/water fractions as well as cytotoxic activity of the extracts obtained from Pedicularis wilhelmsiana (Scrophulariaceae) which grows in Azarbaijan/Iran by agar well diffusion method and brine shrimp lethality test successively. Phytochemical study of this plant was determined as well. A combination of solid-phase extraction (SPE), preparative reversed-phase HPLC analysis and spectroscopic means were applied for fractionation, purification, and identification of ingredients respectively. Antimicrobial test demonstrated that 40% and 60% methanol/water fractions were more active than methanolic extract and other SPE fractions. No cytotoxic effect was detected from the extracts of this plant by brine shrimp lethality assay. Phytochemical study of aerial parts of Pedicularis wilhelmsiana (P. wilhelmsiana) afforded two phenylethanoids (verbascoside and martynoside), three iridoids (Aucubin, ipolamiid, 5-hydroxy-8-epi-loganin) and two flavonoids (luteolin, luteolin-7-glucoside) along with mannitol on the basis of spectral evidences (UV, ¹H and 13CNMR) as well as comparison with literature data. The findings of this research supported further studies related to antibiotic potential of methanolic extract of P. wilhelmsiana. [ABSTRACT FROM AUTHOR]

Alcea glabrata from the family Malvaceae, was selected for evaluating its xanthine oxidase inhibitory, anti-malarial, and antioxidant activities. In addition, some phytochemical analysis upon different extracts of A. glabrata were performed. Aerial parts of the collected A. glabrata plant material were dried and solvent extracted via soxhlet apparatus using different solvents. Various chromatographic techniques were used for extra fractionation of the achieved extracts. Xanthine oxidase (XO) inhibitory, antimalarial and antioxidant activity assays upon different A. glabrata extracts and fractions were carried out and reported in terms of IC 50s. Total phenolic and flavonoid contents of the A. glabrata methanol extract (MeOH) were determined using the 2,2-Di Phenyl-1-Picryl Hydrazyl (DPPH) assay, aluminum chloride colorimetric, and Folin-Ciocalteu reagents, respectively. In addition, A. glabrata essential oil was obtained through hydrodistillation by a Clevenger apparatus. Analysis and identification of essential oil compounds were carried out through gas chromatography mass spectrometry (GC-MS) analysis. MeOH extract showed the highest XO inhibitory activity with the IC 50 of 0.37 ± 0.12 mg/mL antioxidant activity with the RC 50 of 0.24 ± 0.06 mg/mL. While, chloroform extract revealed the strongest antimalarial activity with the IC 50 of 0.4 ± 0.05 mg/mL. The total flavonoid and phenolic contents of the A. glabrata methanol extract were 39.8 mg quercetin equivalent and 6.1 g gallic acid equivalent per 100 g of dry plant material, respectively. GC-MS analysis showed that the monoterpenes were prevailing in A. glabrata essential oil where the major constituents: octacosane (30.7%), eugenol (12.3%), and anethole (12.0%). Concerning the results of this study, A. glabrata extracts and its ingredients could be considered as a novel promising herbal medicine in the design and also treatment of new drugs for the relief of gout and malaria diseases. [Display omitted] • Eleven components were determined from endemic A. glabrata essential oil. • Eugenol and anethole were the major monoterpenes of the A. glabrata essential oil. • A. glabrata methanol extract showed the highest xanthine oxidase inhibitory activity. • The strongest antimalarial activity with the IC 50 of 0.4 mg/mL were obtained from A. glabrata chloroform extract. [ABSTRACT FROM AUTHOR]

Purpose: Cucurbita maxima Duchense (C. maxima) has been widely used in China and Mexico as a hypoglycemic plant for controlling blood glucose in diabetic patients. Furthermore, in northwest of Iran, this plant is used traditionally for controlling of diabetes. We examined the effect of C. maxima pulp besides insulin on control of hyperglycemia in diabetic patients admitted to Intensive care unit (ICU). Methods: Twenty critically ill patients who were admitted to the ICU were enrolled in this study. 5g lyophilized powder of C. maxima was administrated every 12 hours for 3 days. Moreover, blood glucose level and insulin dose were measured every 1-4 hours during 3 days before administration and 3days at the time of C. maxima administration. Results: The average of glucose level in 3 days before C. maxima administration was 214.9 ± 55.7 mg/dl, while in 3 days during C. maxima administration it was decreased to 178.4 ± 36.1 mg/dl (P<0.001). Additionally, the average insulin dose during 3 days before intervention was 48.05 ± 36.5 IU and during the 3 days of C. maxima administration was decreased to 39.5 ± 27.8 IU (P=0.06). Conclusion: It seems that C. maxima may decrease high blood glucose level fast and effective in diabetic critically ill patients. [ABSTRACT FROM AUTHOR]

A combination of solid-phase-extraction (SPE) and reversed-phase preparative high-performance liquid chromatography (prep-HPLC) of the methanolic extract of the aerial parts of Artemisia splendens (common name: “Asia Minor Wormwood”), an endemic Iranian species, afforded Z- and E-melilotosides (1 and 2), Z- and E-4-methoxy-melilotosides (3 and 4), and a new dimer, bis-ortho-Z-melilotoside (5, named: splendenoside). Whilst the structures of these compounds (1-5) were elucidated unequivocally by spectroscopic means, the in vitro free-radical-scavenging property of 1-5 was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. This is the first report on the occurrence of any melilotoside derivatives in the genus Artemisia. [ABSTRACT FROM AUTHOR]

This study compares the green synthesis method using the Lycium ruthenicum (L. Ru) with wet chemical extraction using citrate reduction to synthesize stable gold nanoparticles (AuNPs). The effect of pH on the synthesized AuNPs has also been evaluated in the present investigation. AuNPs were synthesized successfully by both methods, as well; by the way, there were reported differences between the microstructure of resulting powders. For AuNPs synthesized using the green method, a pH value of 3 was reported to be the optimum pH due to the characteristics of synthesized AuNPs. In the mentioned pH, the AuNPs were spherical, mono-dispersed, and highly crystalline, characteristic of a well-done synthesis. Both chemo- and biosynthesized AuNPs revealed a relatively smaller particle size (33.92 and 55.65 nm, respectively) with well-dispersed spherical morphology under alkaline conditions. This study revealed that employing L. Ru extract could be considered a simple, facile, and green technique in stimuli-sensitive AuNPs synthesis. [ABSTRACT FROM AUTHOR]

The composition of the volatile oils from the aerial parts ofArtemisia spicigeraandA. splendens, growing in Iran, was analyzed by GC-MS and GC-FID. A total of 47 constituents from each of the oils (87.6 % and 58.3 % of the total oil ofA. spicigeraandA. splendens, respectively) were separated and identified. The major components of theA. spicigeraoil werecis-chrysanthenyl acetate (24.0 %), camphor (21.0 %), 1,8-cineol (13.9 %) andcis-chrysanthenol (8.5 %), while 1,8-cineol (4.7 %), caryophyllene oxide (3.8 %), valencene (3.5 %) and α-terpenyl acetate (3.4 %) were detected as the major constituents of the oils ofA. splendens. The free-radical-scavenging activity of the oils was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. Both oils showed weak antiradical effect with RC50values of 55.6 and 106.4 µg/mL, respectively, forA. spicigeraandA. splendens. The oils displayed broad and potent insecticidal activity againstOryzaephilus mercator, but no noticeable toxicity towards brine shrimp. [ABSTRACT FROM AUTHOR]

This study aimed to determine phenolic compounds of Artemisia spicigera (family Asteraceae) growing in East-Azarbaijan province of Iran. 20%, 40% and 60% SPE fractions of methanolic extract of A. spicigera, were subjected to reversed phase preparative HPLC, with the mobile phase consisted of methanol and water. Structural identification of phytochemicals by spectroscopic methods including UV and NMR spectroscopy, yielded 4, 6-di methoxy acetophenone-2-O-β-D-glucopyranoside from 20%, 5-methoxyluteolin 7-O-β-D-glucopyranoside, luteolin and chrysoeriol 7-O-β-D-glucopyranoside from 40% and 5-methoxy luteolin from 60% SPE fractions. Although within identified pure compounds, luteolin was the only phenolic reported from some other species of Artemisia, but occurrence of remained identified phenolics in this study, was firstly reported from Artemisia genus. Further phytochemical investigations were proposed in order to isolate some other active fractions and pure compounds. [ABSTRACT FROM AUTHOR]

This study aimed to determine biological activity and phytochemical study of Scutellaria platystegia (family Labiatae). Methanolic (MeOH) extract of aerial parts of S. platystegia and SPE fractions of methanolic extract (specially 20% and 40% methanolic fractions), growing in East-Azarbaijan province of Iran were found to have radical scavenging activity by DPPH (2, 2-diphenyl -1- pycryl hydrazyl) assay. Dichloromethane (DCM) extract of this plant exhibited animalarial activity by cell free method providing IC50 at 1.1876 mg/mL. Crude extracts did not exhibit any toxicity assessed by brine shrimp lethality assay. Phytochemical study of methanolic extract by using reverse phase HPLC method and NMR instrument for isolation and identification of pure compounds respectively, yielded 2-(4- hydroxy phenyl) ethyl-O-β-D- glucopyranoside from 10% and apigenin 7-O-glucoside, verbascoside and martynoside from 40% SPE fraction. Occurance of verbascoside and martynoside as biochemical markers appeared to be widespread in this genus. Antioxidant and antimalarial activity of MeOH and DCM extracts, respectively, as well as no general toxicity of them could provide a basis for further in-vitro and in-vivo studies and clinical trials to develop new therapeutical alternatives. [ABSTRACT FROM AUTHOR]

Purpose: Naturally occurring substances as novel drugs in cancer therapy, at all times, represent a challenge to science since medicinal plants are proving to be brilliant sources of new chemopreventive agents. Methods: In the present study, methanol extract from aerial parts of Marrubium crassidens was assessed for its antiproliferative activity in the breast cancer cell line MCF-7 through MTT bioassay using cell viability and cytotoxicity indices. The antioxidant property of M. crassidens extract together with its phenolic and flavonoids content were evaluated, as well. Results: According to data obtained in the study, M. crassidens exhibited antiproliferative activity with a gradual rise in cytotoxicty effect setting out on 240μg/mL concentration of the extract. Moreover, the RC50 value for antioxidant activity of the extract was determined as 40μg/mL and values for the total phenolic and flavonoids were calculated as 512.64mg gallic acid equivalent and 212.73mg quercetin equivalent per 100g of dry plant material. Conclusion: Generally, the observed antiproliferative and antioxidant properties of M. crassidens could be certified to the high amounts of phenolic and flavonoid content detected in the extract. [ABSTRACT FROM AUTHOR]

Objective(s): In regard to the high incidence of asthma and the side-effects of the drugs used, finding novel treatments for this disease is necessary. Our previous studies demonstrated the preventive effect of Nigella sativa extract on ovalbumin-induced asthma. In addition, water-soluble substances of N. sativa extract and methanol fraction of this plant were responsible for the relaxant effect of this plant on tracheal chains of guinea pigs. Therefore, for the first time, in the present study, in order to identify main constituents of the methanolic extract, the relaxant effects of five different methanolic fractions (20%, 40%, 60%, 80%, and 100%) of N. sativa on tracheal chains of guinea pigs were examined. Materials and Methods: The relaxant effects of four cumulative concentrations of each fraction (0.8, 1.2, 1.6, and 2.0 g%) in comparison with saline as negative control and four cumulative concentrations of theophylline (0.2, 0.4, 0.6, and 0.8 mM) were examined by their relaxant effects on precontracted tracheal chains of guinea pig by 60 mM KCl (group 1) and 10 μM methacholine (group 2). Results: In group 1, all concentrations of only theophylline showed significant relaxant effects but all concentrations of these methanolic fractions showed significant contractile effects compared with that of saline (P<0.001 to P<0.05). However, in group 2, all concentrations of theophylline and these methanolic fractions showed significant relaxant effects compared with that of saline (P<0.001 to P<0.05). Conclusion: These results showed a potent relaxant effect of 20% methanolic fractions from N. sativa on tracheal chains of guinea pigs that were higher than that of theophylline at the used concentrations. [ABSTRACT FROM AUTHOR]

We aimed to investigate the apoptotic effects of the methanolic extract of Dorema glabrum seed on WEHI-164, cancerous cells in comparison with L929, normal cells and compared them with the cytotoxic effects of Taxol. So, MTT test and DNA fragmentation assay were performed on cultured and treated cells. Also electrophoresis which was followed by immunoblotting was done to survey the production of Caspase-3 and Bcl2 proteins, and to inquire into their relative genes expression, RT-PCR was used. According to our findings, the methanolic extract of Dorema glabrum seed can alter cells morphology as they shrink and take a spherical shape and lose their attachment too. So, the plant extract inhibits cell growth albeit in a time- and dose-dependent manner and results in degradation of chromosomal DNA. Induction of apoptosis by the plant extract was proved by the reduction of pro-Caspase-3 and Bcl2 proteins and increase in Caspase-3 gene expression and decrease in that of bcl2 too. Our data well established the antiproliferative effect of methanolic extract of Dorema glabrum seed and clearly showed that the plant extract can induce apoptosis and not necrosis in vitro. These results demonstrated that Dorema glabrum seed might be a novel and attractive therapeutic candidate for tumor treatment. [ABSTRACT FROM AUTHOR]

Chemical composition of the essential oil obtained from the aerial parts of Scrophularia amplexicaulis Benth. was analyzed, for the first time, by the gas chromatography/mass spectrometry (GC-MS) and gas chromatography/flame ionization detection (GC-FID). A total yield of 3 mg of essential oil per100 g of plant dry mass was obtained, and 27 compounds were identified, representing 97.7% of total oil. The essential oil were characterized by a high content of oxygenated monoterpenes and phenolic derivatives. The main constituents were eugenol (53.8%), eugenol acetate (24.5%), β-caryophyllene (5.7%), caryophyllene oxide (6.4%) and aromadendrene oxide II (2.1%). The antimicrobial activity of the essential oil was tested against Staphylococcus aureus using the well diffusion method, and the free-radical-scavenging activity was assessed by the 2,2-diphenyl-picryl-hydrazyl (DPPH) assay. [ABSTRACT FROM AUTHOR]

This study was conducted to extract the essential oils (EOs) of Caccinia macranthera identify their phytochemicals, evaluate their phytotoxicity, antimicrobial activity and enzyme inhibition effects using in silico molecular docking technique. EOs of aerial parts, seeds, and roots of C. macranthera were extracted and analyzed via Gas chromatography-Mass Spectrometry. The antibacterial activity of EOs were determined on nine microorganisms via disk diffusion and microbroth dilution assays. In addition, the allelopathic properties of EOs were investigated by calculating the IC 50 s for inhibition of germination, seedling length and seedling weight growth of Cuscuta campestris seeds. In order to assess the possible inhibitory effect of major components of C. macranthera EOs on enzymes inhibiting germination and plant growth, molecular docking was employed against the glutamine synthetase (GS), acetohydroxyacid synthetase (AHAS), and 4-hydroxyphenyl pyruvate dioxygenase (HPPD) enzymes. The main compounds of EOs from aerial parts, seeds, and roots EOs were dihydrocarveol (29.5%), Trimethyl-2-Pentadecanone (13.6%), and Palmitic acid (16.8%), respectively. The maximum antibacterial effect was related to the aerial parts EO against Staphylococcus epidermidis. Phytotoxicity analysis exhibited a concentration-dependent increase (p ≤ 0.05) activity. The aerial parts EO demonstrated a substantial allelopathy effect, with IC 50 values of 0.22 ± 0.026, 0.39 ± 0.021, and 0.20 ± 0.025 mg/mL, respectively, on inhibitory germination, seedling length and seedling weight growth of Cuscuta campestris seeds. Molecular docking analyzes showed that Oleic acid was suitable for dynamic stabilization of HPPD (−6.552 kJ/mol) and GS (−7.265 kJ/mol) and Eupatoriochromene had the inhibitory potential against AHAS, with docking score of −4.189 kJ/mol. The current research demonstrated that C. macranthera EOs from its aerial parts have an acceptable phytotoxic activity against Cuscuta campestris weed. The major components of EOs, Oleic acid and Eupatoriochromene, presented the strongest binding with HPPD, GS, and AHAS active sites causing disturbance in germination, photosynthesis and weed growth suggesting it as a natural herbicide for controlling the weeds. [Display omitted] • Dihydrocarveol, trimethyl-2-pentadecanone and palmitic acid were the major compounds of essential oils. • Aerial parts essential oil demonstrated significant antibacterial activity against Staphylococcus epidermidis. • Caccinia macranthera essential oils exhibited satisfactory allelopathic and phytotoxicity effects. • Oleic acid and eupatoriochromene found in essential oils inhibited allelopathic related enzymes in silico. [ABSTRACT FROM AUTHOR]

Hypoxia-inducible factor-1 is a target for the management of cancer. Here, the anti-proliferation properties of corosolic acid (CA) against A549 human lung epithelial cancer cells in CoCl 2 -induced hypoxia is reported. CA was isolated from the roots of Salvia syriaca based on a bioassay-guided isolation platform and identified by 1D and 2D NMR experiments. Several cytotoxicies and genotoxicity analyses were performed using MTT, DAPI, cell cycle, DNA ladder, and annexin V/PI detection. Cobalt chloride (CoCl 2) was used to stimulate hypoxia. The adaptation of A549 cells to a stimulated hypoxic condition in the presence of CA was evaluated. CA decreased the growth of A549 cells with an IC 50 of 12 μg/mL at 48 h. Also, chromatin condensation and DNA fragmentation were detected as signs of apoptosis occurrence. CA induced ~85% apoptosis and even 1% necrosis. The expression of hypoxia-inducible factor-1 α (HIF-1α), HIF-1β and downstream genes was strongly suppressed in the presence of CA in CoCl 2 -stimulated hypoxia condition. Results indicated that CA has remarkable cytotoxicity against the cancerous cell in hypoxia condition and may be regarded for preparation of new formulations for possible uses as supplement and medicine in cancer therapy. Unlabelled Image • The roots of Salvia syriaca were subjected to bioassay-guided isolation • Triterpenoid corosolic acid (CA) was found to be anti-proliferative compound • CA attenuates HIF-1 stabilization upon CoCl 2 -induced hypoxia in A549 cancer cells • CA has remarkable anti-cancer activity in hypoxia through targeting HIF-1 [ABSTRACT FROM AUTHOR]

Abstract The adaptation of solid tumors to the low oxygen/nutrient environment is mediated by the pivotal transcription role of hypoxia-inducible factor-1 (HIF-1). Thus, the HIF-1 and its subunits have been considered to be hopeful anti-cancer targets. Various natural compounds were reported to persuade cell cytotoxicity through targeting and downregulation of the HIF-1. The genus Salvia is a rich source of bioactive terpenoids which show promising anti-cancer activities. Here, the identification of natural anti-proliferative compound targeting the HIF-1α expression was reported. A bioassay-guided isolation was employed for the discovery of natural anti-proliferative compounds from Salvia extracts using MTT assay against A549 cells. In this direction, clerodermic acid (CDA) as a potent cytotoxic compound was purified from Salvia nemorosa and identified using 1D and 2D NMR analysis. Results indicated that CDA has anti-proliferation activity (IC 50 value of 35 μg/mL) which was confirmed by genotoxicity and apoptosis detection analyses. The quantitative qPCR analysis showed that the expression level of HIF-1 alpha was strongly inhibited in the hypoxic cells treated with CDA compared to the untreated cells tolerated hypoxia. Findings exhibited that S. nemorosa and clerodermic acid have significant potential for reducing HIF-1α expression and could be considered for further studies for cancer therapy. [ABSTRACT FROM AUTHOR]

Introduction. Menstrual bleeding cessation is one of the most frequent gynecologic disorders among women in reproductive age. The treatment is based on hormone therapy. Due to the increasing request for alternative medicine remedies in the field of women’s diseases, in present study, it was tried to overview medicinal plants used to treat oligomenorrhea and amenorrhea according to the pharmaceutical textbooks of traditional Persian medicine (TPM) and review the evidence in the conventional medicine. Methods. This systematic review was designed and performed in 2017 in order to gather information regarding herbal medications of oligomenorrhea and amenorrhea in TPM and conventional medicine. This study had several steps as searching Iranian traditional medicine literature and extracting the emmenagogue plants, classifying the plants, searching the electronic databases, and finding evidences. To search traditional Persian medicine references, Noor digital library was used, which includes several ancient traditional medical references. The classification of plants was done based on the repetition and potency of the plants in the ancient literatures. The required data was gathered using databases such as PubMed, Scopus, Google Scholar, Cochrane Library, Science Direct, and web of knowledge. Results. In present study of all 198 emmenagogue medicinal plants found in TPM, 87 cases were specified to be more effective in treating oligomenorrhea and amenorrhea. In second part of present study, where a search of conventional medicine was performed, 12 studies were found, which had 8 plants investigated: Vitex agnus-castus, Trigonella foenum-graecum, Foeniculum vulgare, Cinnamomum verum, Paeonia lactiflora, Sesamum indicum, Mentha longifolia, and Urtica dioica. Conclusion. Traditional Persian medicine has proposed many different medicinal plants for treatment of oligomenorrhea and amenorrhea. Although just few plants have been proven to be effective for treatment of menstrual irregularities, the results and the classification in present study can be used as an outline for future studies and treatment. [ABSTRACT FROM AUTHOR]

Introduction. Menstrual bleeding cessation is one of the most frequent gynecologic disorders among women in reproductive age. The treatment is based on hormone therapy. Due to the increasing request for alternative medicine remedies in the field of women’s diseases, in present study, it was tried to overview medicinal plants used to treat oligomenorrhea and amenorrhea according to the pharmaceutical textbooks of traditional Persian medicine (TPM) and review the evidence in the conventional medicine. Methods. This systematic review was designed and performed in 2017 in order to gather information regarding herbal medications of oligomenorrhea and amenorrhea in TPM and conventional medicine. This study had several steps as searching Iranian traditional medicine literature and extracting the emmenagogue plants, classifying the plants, searching the electronic databases, and finding evidences. To search traditional Persian medicine references, Noor digital library was used, which includes several ancient traditional medical references. The classification of plants was done based on the repetition and potency of the plants in the ancient literatures. The required data was gathered using databases such as PubMed, Scopus, Google Scholar, Cochrane Library, Science Direct, and web of knowledge. Results. In present study of all 198 emmenagogue medicinal plants found in TPM, 87 cases were specified to be more effective in treating oligomenorrhea and amenorrhea. In second part of present study, where a search of conventional medicine was performed, 12 studies were found, which had 8 plants investigated: Vitex agnus-castus, Trigonella foenum-graecum, Foeniculum vulgare, Cinnamomum verum, Paeonia lactiflora, Sesamum indicum, Mentha longifolia, and Urtica dioica. Conclusion. Traditional Persian medicine has proposed many different medicinal plants for treatment of oligomenorrhea and amenorrhea. Although just few plants have been proven to be effective for treatment of menstrual irregularities, the results and the classification in present study can be used as an outline for future studies and treatment. [ABSTRACT FROM AUTHOR]

The GC-MS analyses of the essential oils of inflorescence of Phlomis pungens Willd. (Lamiaceae), collected from Galalti, Altiagach and Nakhchivan of Azerbaijan, led to the identification of 2 monoterpenes, 44 sesquiterpenes, 1 diterpene and 4 aliphatic acids constituents accounting for over 93.9, 94.1 and 95.2% of the total oils. In the same way the GC-MS analyses of the essential oils of leaves collected from three localities led to the identification of 2 monoterpenes, 37 sesquiterpenes, 1 diterpene and 4 aliphatic acid constituents, too which responsible for over 90.3, 92.4 and 94.8% of the total oils. Non surprisingly, the main constituents of inflorescence and leaves oil were sesquiterpenes (mainly non-oxygenated) and aliphatic acids which these findings are consistent with previous studies on Phlomis genus. Quantitative and qualitative differences were found among essential oils of inflorescence and leaves of the plants collected from different localities of Azerbaijan. [ABSTRACT FROM AUTHOR]

Any dysfunctionality in maintaining the oxygen homeostasis by mammalian cells may elicit hypoxia/anoxia, which results in inescapable oxidative stress and possible subsequent detrimental impacts on certain cells/tissues with high demands to oxygen molecules. The ischemic damage in turn can trigger initiation of a number of diseases including organs ischemia, metabolic disorders, inflammatory diseases, different types of malignancies, and alteration in wound healing process. Thus, full comprehension of molecular mechanism(s) and cellular physiology of the oxygen homeostasis is the cornerstone of the mammalian cells metabolism, energetic pathways and health and disease conditions. An imbalance in oxygen content within the cellular microenvironment activates a cascade of molecular events that are often compensated, otherwise pathologic condition occurs through a complexed network of biomolecules. Hypoxia inducible factor-1 (HIF-1) plays a key transcriptional role in the adaptation of cell physiology in relation with the oxygen content within a cell. In this current study, we provide a comprehensive review on the molecular mechanisms of oxygen sensing and homeostasis and the impacts of HIF-1 in hypoxic/anoxic conditions. Moreover, different molecular and biochemical responses of the cells to the surrounding environment are discussed in details. Finally, modern technological approaches for targeting the hypoxia related proteins are articulated. [ABSTRACT FROM AUTHOR]

Purpose: Zygophyllum fabago L. (Z. fabago) is a widespread perennial herb which is used as a medicinal plant in traditional medicine of Iran, Turkey and China. The present study was a survey on phytochemical constituents and biological activities of this plant. Methods: Methanolic extract of the roots was fractionated over a C-18 pre-packed cartridge (Sep-pak) and chromatographic separation was performed on a reversed-phase preparative HPLC. Structural elucidation of the isolated compounds was carried out using UV, 1H-NMR and 13C-NMR spectral analyses. Furthermore, the chemical compositions of the essential oil of the aerial parts were identified by GC-MS analysis. Antiproliferative and antioxidant activities of all extracts from aerials were determined by MTT and DPPH assays, respectively. Results: Phytochemical investigation on the plant roots led to the isolation and identification of two the 60% methanol-water Sep-pak fraction, a prenylated flavone glycoside, 6-C-prenyl-7-O-[β-D-4‴-O-acetyl-glucopyranosyl-(1‴→2″)-β-D-glucopyranosyl] apigenin, which was named as a Zygocaperoside and also, other flavonoid, was named as the Isorhamnetin -3-O glucoside. None of the extracts showed antiproliferative effect against cancerous cells. However, among the extracts, methanolic extract indicated antioxidant activity. Moreover, essential oils of flowers and leaves of plant have high amounts of sesquiterpene hydrocarbons and diterpenoides. Conclusion: The results of present study introduce Z. fabago roots as a new source of flavonoid glycosides and suggest it as an appropriate candidate for further pharmacological studies. [ABSTRACT FROM AUTHOR]

Purpose: Lycopene belongs to the carotenoids that shows good pharmacological properties including antioxidant, anti-inflammatory and anticancer. However, as a result of very low aqueous solubility, it has a limited systemic absorption, following oral administration. Methods:Here, we prepared a stable lycopene-loaded solid lipid nanoparticles using Precirol® ATO5, Compritol 888 ATO and myristic acid by hot homogenization method with some modification. The size and morphological characteristics of nanoparticles were evaluated using Scanning Electron Microscopy (SEM). Moreover, zeta potential and dispersity index (DI) were measured using zeta sizer. In addition, encapsulation efficiency (EE%), drug loading (DL) and cumulative drug release were quantified. Results: The results showed that the size and DI of particles was generally smaller in the case of SLNs prepared with precirol when compared to SLNs prepared with compritol. Scanning electron microscopy (SEM) and particle size analyses showed spherical SLNs (125 ± 3.89 nm), monodispersed distribution, and zeta potential of -10.06 ± 0.08 mV. High EE (98.4 ± 0.5%) and DL (44.8 ± 0.46 mg/g) were achieved in the case of nanoparticles prepared by precirol. The stability study of the lycopene-SLNs in aqueous medium (4 °C) was showed that after 2 months there is no significant differences seen in size and DI compared with the fresh formulation. Conclusion: Conclusively, in this investigation we prepared a stable lycopene-SLNs with good physicochemical characteristic which candidate it for the future in vivo trials in nutraceutical industries. [ABSTRACT FROM AUTHOR]

Objective(s): Chemoresistance remains the main causes of treatment failure and mortality in cancer patients. There is an urgent need to investigate novel approaches to improve current therapeutic modalities and increase cancer patients' survival. Induction of drug efflux due to overexpression of P-glycoproteins is considered as an important leading cause of multidrug resistance. In this study, we investigated the role of combination treatments of docetaxel and vinblastine in overcoming P-glycoprotein mediated inhibition of apoptosis and induction of cell proliferation in human non-small cell lung carcinoma cells. Materials and Methods: Cell proliferation and apoptosis were assessed using MTT assay and DAPI staining, respectively. P-glycoprotein expression was evaluated in gene and protein levels by Real-time RT-PCR and Western blot analysis, respectively. Results: Combination treatment of the cells with docetaxel and vinblastine decreased the IC50 values for docetaxel from (30±3.1) to (15±2.6) nM and for vinblastine from (30±5.9) to (5±5.6) nM (P≤0.05). P-glycoprotein mRNA expression level showed a significant up-regulation in the cells incubated with each drug alone (P≤0.001). Incubation of the cells with combined concentrations of both agents neutralized P-glycoprotein overexpression (P≤0.05). Adding verapamil, a P-glycoprotein inhibitor caused a further increase in the percentage of apoptotic cells when the cells were treated with both agents. Conclusion: Our results suggest that combination therapy along with P-glycoprotein inhibition can be considered as a novel approach to improve the efficacy of chemotherapeutics in cancer patients with high P-glycoprotein expression. [ABSTRACT FROM AUTHOR]

Context: Galbanic acid (GBA) is a sesquiterpene coumarin with different medicinal properties and anticancer effects. Objective: To improve the anticancer activities of GBA, in the current study, we aimed to fabricate GBA-loaded solid lipid nanoparticles (GBA-SLNs) and study their biological activities in vitro. Materials and methods: Hot homogenization was used for preparation of GBA-SLNs. The encapsulation efficiency (EE) and drug loading (DL) and in vitro release were determined. MTT, DAPI, DNA fragmentation, comet, and Anexin V apoptosis assays were used to compare the anti-cell proliferation and genotoxicity properties of GBA and GBA-SLNs against A549 cells and HUVEC to detect apoptosis and DNA damage in the final concentration of 100 µM after 48 h treatment. Results: Scanning electron microscopy (SEM) and particle size analysis showed spherical SLNs (92 nm), monodispersed distribution, and zeta potential of −23.39 mV. High EE (>98%) and long-term in vitro release were achieved. The stability of GBA-SLNs in aqueous medium was approved after 3 months in terms of size and polydispersity index. GBA was able to inhibit A549 growth with an IC50 value of 62 µM at 48 h. Although GBA-SLNs could also inhibit the growth rate of A549 cells, the effect is perceived after 48 h, as approved by the quantitative expression of Bcl-xL and Casp 9 genes, and also genotoxicity assays. Conclusion: Long-term apoptotic effect of GBA-SLNs compared with GBA may be due to the accumulation of GBA-SLNs in the tumor site because of deviant tumor pathology. Our data confirmed that SLNs could be exploited for sustained lipophilic GBA delivery. [ABSTRACT FROM AUTHOR]

Hypoxia Inducible Factor-1 plays a key transcriptional role in the adaptation of hypoxic solid tumors to low oxygen environment. Here, we aimed to investigate galbanic acid (GBA) inhibitory effects on HIF-1 activation during hypoxia and normoxia. MTT survival and Annexin V assays were used to evaluate GBA cytotoxicity and apoptosis in treated cells. Quantitative real time PCR and western blotting were used to estimate mRNA expression and translated protein, respectively. Results showed that GBA dose- and time-dependently decreased the in vitro growth of OVCAR-3 human epithelial carcinoma cells with an IC 50 of approximately 37, 12.1 and 10 μM GBA at 24, 48 and 72 h, respectively. Following phosphatidylserine of outer leaflet of the plasma membrane revealed occurrence of early/late apoptosis in GBA treated cells. In addition, we found that GBA down-regulates HIF-1α and HIF-1β mRNA expression in both hypoxia and normoxia. To determine the mechanism of action, we showed that GBA did not inhibit Akt and EGFR mRNA expression, yet protein degradation investigation showed that GBA shortened the half-life of EGFR through decreasing its stability with a decrease of nearly 2 and 3 h in A549 and OVCAR-3 cell lines, respectively. We also found that downstream genes contributed in glycolysis, including Eno 1 and GluT-1 , are underexpressed in GBA treated cells in hypoxia. Conclusively, GBA may inhibit HIF-1 activation through down-regulation of its subunit expression in hypoxia, and increasing of EGFR degradation in normoxia. [ABSTRACT FROM AUTHOR]

Introduction: Dorema glabrum (Apiaceae) is a rare and monocarpic species distributed in Transcaucasia and North West of Iran. We aimed to explore anticancer potency of bioactive compounds from the seeds of Dorma glabrum. Methods: Methanol extract was subjected to phytochemical investigation using normal phase Sep-pak and reversed-phase HPLC, and cytotoxic effect of isolated compounds on CAOV-4 cell line was evaluated. Furthermore, Annexin V/PI staining and comet assay were used to study genotoxicity of compounds. Results: Diglucosyl caffeoyl ester (1), Glucopyranosylcaffeic acid (2) and skimmin (3), were identified. MTT cytotoxicity assay showed growth inhibition of CAOV-4 cells due to treatment with compunds (1), (2) and (3) with an IC50 of 99.7, 87.3 and 70.03 |ig/ml at 48 h, respectively. Annexin V-FITC/PI staining showed occurrence of early/late apoptosis in the (1)-treated cells, while (2)-and (3)-treated cells necrosis/late apoptosis was dominant event. Single/double strands DNA breakages were observed by comet assay in all treatments. Conclusion: This work provides sufficient information about anti-cancer properties of the diglucosyl caffeoyl ester from the seeds of D. glabrum. [ABSTRACT FROM AUTHOR]

Introduction: Lignans and flavonoids are widely distributed phenolics in the plant kingdom. Aryltetralin type lignans (podophyllotoxin derivatives) as the major secondary metabolites of Linum species play an important role in the production of chemotherapy drugs. In the present study, lignans and flavonoid glycosides from aerial parts of Linum mucronatum subsp. orientale were isolated and identified. Methods: The phytochemical investigation has been carried out on Hexane, DCM and MeOH extracts of the plant. Separation of chemical constituents was done using different chromatography (CC, prep-TLC, GC/MS and HPLC) methods. The major compounds of dichloromethane (DCM) and methanol extracts were isolated and their structures were elucidated using cochromatography in the presence of known lignans, HPLC and NMR techniques. Results: Our results showed that podophyllotoxin and 6-MeO-α- peltatin, as new compound, are the major lignans of the DCM extract of L. mucronatum subsp. orientale. Two new flavonoid glycosides were also elucidated in the methanolic extract. Conclusion: The DCM and methanol extracts of L. mucronatum were found to contain aryltetralin-type lignans and flavonoids. The occurrence of 6-MeO-α- peltatin and flavonoids in L. mucronatum has been reported for the first time. [ABSTRACT FROM AUTHOR]

General toxicity, antiproliferative, antibacterial and antioxidant activities of Caulerpa peltata J.V.Lamouroux (Caulerpaceae) collected from Oman Sea were investigated. Dried, ground alga was Soxhlet-extracted with hexane, dichloromethane and methanol successively. The methanol extract was subjected to vacuum liquid chromatography (VLC) fractionation on silica gel using a step gradient of different mixture of solvents. A known alkaloid, caulerpin, was subsequently isolated from the fraction eluted by ethyl acatete100%. The antioxidant activity of all extracts was assessed by using the (DPPH) assay. Antiproliferative activity of the all extracts and caulerpin against the cancerous cell line was evaluated using MTT assay. General toxicity of extracts was determined using Brine Shrimp Lethality Assay (BSLA). Based on our results, a weak activity observed for all extracts in MTT assay, while they were toxic toward brine shrimp nauplii comparing to the podophylotoxin. This is the first report on phytochemistry and bioactivity of C. peltata which collected from Oman Sea. [ABSTRACT FROM AUTHOR]

Purpose: This research paper presents antioxidant and antimicrobial activities of Pedicularis sibthorpii and Pedicularis wilhelmsiana which grow in Azerbaijan/Iran with claimed a lot of therapeutic effects. Methods: DPPH assay and agar well diffusion method were carried out to determine antioxidant and antimicrobial activities respectively. Results: Methanolic extract showed better antioxidant activity compared to other crude extracts (n-hexane and dichloromethane). Methanolic extracts of both Pedicularis sibthorpii and Pedicularis wilhelmsiana were found to have antibacterial activity especially against gram positive strains of S. ureus, S.epidermidis. No antifungal activity was observed in the tested extracts. Conclusion: Existence of some phenolic compounds in methanolic extracts, such as phenylethanoids and flavonoids (found in other species of Pedicularis), which cause both antioxidant and antibacterial activities, is probable. Antimicrobial and antioxidant activity of the methanolic extracts supports further studies related to phytochemical investigation and bioassay of different fractions to isolate pure compounds of plants. [ABSTRACT FROM AUTHOR]

Introduction: The potential health risks and toxicity of synthetic antioxidants resulted in an upsurge of interest in phytochemicals as new sources of natural antioxidants. Phenolics of Astragalus L. (Fabaceae) possess antioxidant properties and have been shown to have a protective effect against several degenerative diseases. The objective of this study was to determine total phenolics and antioxidant activity of methanolic extracts from different parts of A. compactus Lam. at different phenological phases and to investigate the correlations between antioxidation and the contents of the total phenolics. Methods: Total phenolic content (TPC) was determined using the Folin-Ciocalteau reagent and the antioxidant capacity was evaluated with the 1,1-diphenyl-2-picrylhydrazyl (DPPH) test. Results: Generally, the TPC in leaves was higher than that of the roots and flowers. TPC in leaves, roots and flowers of the species varied from 5.01-8.25, 4.29-7.89 and 4.19 µg GAE/mg DW, respectively. In addition, roots and leaves at fructification stage possessed higher TPC than vegetative and flowering stages. Therefore, the leaf extracts at fructification phase showed the highest TPC that accompanied with best antioxidant activity. In the root extracts, fructification stage was also characterized by the highest antioxidant activity. Conclusion: A positive relationship between antioxidant activity and TPC showed that phenolics were the dominant antioxidant components in the species. The results obtained suggest that A. compactus methanolic extracts may serve as potential sources of natural phenolic antioxidants and that the fructification phase could be considered as the best stage for the harvesting of this plant. [ABSTRACT FROM AUTHOR]

Introduction: Pedicularis sibthorpii and P. wilhelmsiana are endemic species mainly found in North-West of Iran. Plants of genus Pedicularis produce some important polyphenols and flavonoids. In the present work, total phenol and flavonoid contents of the mentioned species as well as their antioxidant capacity have been evaluated. Methods: Methanol extract of samples was fractionated by SPE method using an ODS cartridge and their 1H-NMR spectra were recorded. Total phenols and flavonoids of methanol extracts were determined using Folin- Ciocalteu and aluminum chloride methods. For determining antioxidant activity of the extracts and fractions, bleaching of purple color methanol solution of 1, 1-diphenylpycryl hydrazyl (DPPH) was measured by spectrophotometric assay. Results: Total phenols of Pedicularis sibthorpii and P. wilhelmsiana were in the range of 8-30 mg g-1 and 9-20 mg g-1, respectively. The 40% and 60% fractions of P. sibthorpii and the 20%, 40% and 60% fractions of P. wilhelmsiana showed higher amounts of phenolic compounds. The total flavonoid contents of P. sibthorpii and P. wilhelmsiana were in the range of 0-215 mg g-1 and 0-177 mg g-1, respectively, whereas the 40% and 60% fractions showed higher flavonoid amounts. Antioxidant activity of P. sibthorpii and P. wilhelmsiana were in the range of 0.01-0.7 mg mL-1 and 0.01-1.02 mg mL-1. In the same manner, the 20% and 40% fractions of P. sibthorpii and the 40% and 60% fractions of P. wilhelmsiana had lower RC50 than that of other fractions. Conclusion: Fractions with lower RC50 had higher contents of phenolic and flavonoid compounds. The results of NMR spectra were parallel with these findings and show that it is worth to do phytochemical studies on P. sibthorpii and P. wilhelmsiana. [ABSTRACT FROM AUTHOR]

Amygdalus lycioides var. horrida (Spach) Browicz (Rosaceae), also known as Prunus lycioides (Spach.) Schneid., is an endemic Iranian species of the genus Amygdalus. In Iranian traditional medicine, the aerial parts and roots of A. lycioides are used in the treatment of diabetes. Six flavonoids, i.e. quercetin 3-O-rhamnoside (1), luteolin 7-O-rhamnoside (2), isorhamnetin 3-O-rutinoside (3), kaempferol 3-O-rhamnoside (4), apigenin (5), and naringenin (6), have been isolated from the aerial parts of this plant. The structures of these compounds were elucidated by UV, MS, and NMR spectroscopic data analyses. While the antioxidant activity of these compounds was assessed by the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay, the vasorelaxant effect was determined using the rat aortic vascular smooth muscle. Compounds 1-6 displayed significant antioxidant activity, with the RC50 values ranging from 0.0033 to 0.5186 mg/ml. Compound 2 showed a considerable vasorelaxant activity on rat aortic vascular smooth muscle in a dose-dependent manner. [ABSTRACT FROM AUTHOR]