Olive oil extract of the flowering aerial parts of
Hypericum perforatum L. (Hypericaceae) is a popular folk remedy for the treatment of wounds in Turkey. In order to prove the claimed utilization of ...the plant, the effects of the extracts and the fractions were investigated by using bioassay-guided procedures. For the wound healing activity assessment,
in vivo excision and incision wound models were applied. For the anti-inflammatory activity, an
in vivo model, based on the inhibition of acetic acid-induced increase in capillary permeability was used as well. Moreover, a parallel study was run on
Hypericum scabrum L., which is a widespread species of the gender but not known as a folk remedy for wound healing, to provide a preliminary data to compare and emphasize the selection of correct plant species.
Olive oil extract of the flowering aerial parts of
Hypericum perforatum L. (Hypericaceae) is a popular folk remedy for the treatment of wounds in Turkey.
In order to prove the claimed utilization of the plant, the effects of the extracts and the fractions were investigated by using bioassay-guided procedures. For the wound healing activity assessment,
in vivo excision and incision wound models were applied. For the anti-inflammatory activity, an
in vivo model, based on the inhibition of acetic acid-induced increase in capillary permeability was used as well. Moreover, a parallel study was run on
Hypericum scabrum L., which is a widespread species of the gender but not known as a folk remedy for wound healing, to provide a preliminary data to compare and emphasize the selection of correct plant species.
Initial investigations proved that the olive oil extract of
Hypericum perforatum has a significant wound healing effect on excision (5.1–82.6% inhibition) and circular incision (20.2–100.0% inhibition) wound models. In order to determine the active wound healing ingredient(s), aerial parts of the plant was extracted with ethanol, noteworthy wound healing activity profile was observed with the wound models; between 18.3% and 95.6% in excision model and from 13.9% to 100.0% inhibitions in incision model were determined. The ethanolic extract was then submitted to successive solvent extractions with
n-hexane, chloroform and ethyl acetate (EtOAc). Each solvent extract was also applied on the same wound models, consequently, EtOAc subextract was found to be the most active one by inhibiting wounds between 17.9% and 100.0% in excision model, subsequently between 9.4% and 100.0% in incision model. However, all subfractions obtained from the EtOAc subextract using Sephadex LH-20 column chromatography showed wound healing activity not more than the whole EtOAc subextract, which revealed that a possible synergistic activity that might be questioned. Among the active Sephadex fractions, Fr. A further yielded hyperoside, isoquercitrin, rutin and (−)-epicatechin and Fr. B yielded hypericin as the major components. Moreover, a dose-dependent anti-inflammatory activity was found for the ethanol extract, EtOAc subextract and Sephadex fractions of
Hypericum perforatum. These results suggest that anti-inflammatory activity of the active fractions might have a contributory role in the wound healing effect of the plant.
Results of the present study have proved that aerial parts of
Hypericum perforatum possess remarkable wound healing and anti-inflammatory activities supporting the folkloric assertion of the plant in Turkish folk medicine. Flavonoids hyperoside, isoquercitrin, rutin and (−)-epicatechin and naphthoquinones (hypericins) were found as the active components of
Hypericum perforatum. On the other hand, ethanol extract of
Hypericum scabrum showed neither remarkable wound healing nor anti-inflammatory activity demonstrating the importance of correct plant species selection in therapeutic applications.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The antioxidant and mutagenic/antimutagenic activities of the fixed oils from Nigella sativa (NSO) and Nigella damascena (NDO) seeds, obtained by cold press‐extraction from the cultivar samples, were ...comparatively investigated for the first time. The antimutagenicity test was carried out using classical and modified Ames tests. The fatty acid composition of the fixed oils was characterized by gas chromatography–mass spectrometry (GC‐MS) while the quantification of thymoquinone in the fixed oils was determined by UPC2. The main components of the NSO and NDO were found to be linoleic acid, oleic acid, and palmitic acid. The results of the Ames test confirmed the safety of NSO and NDO from the viewpoint of mutagenicity. The results of the three antioxidant test methods were correlated with each other, indicating NDO as having a superior antioxidant activity, when compared to the NSO. Both NSO and NDO exhibited a significant protective effect against the mutagenicity induced by aflatoxin B1 in Salmonella typhimurium TA98 and TA100 strains. When microsomal metabolism was terminated after metabolic activation of the mycotoxin, a significant increase in antimutagenic activity was observed, suggesting that the degradation of aflatoxin B1 epoxides by these oils may be a possible antimutagenic mechanism. It is worthy to note that this is the first study to assess the mutagenicity of NSO and NDO according to the OECD 471 guideline and to investigate antimutagenicity of NDO in comparison to NSO against aflatoxin.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
Cytotoxic activity-guided isolation studies on the underground parts of Valeriana sisymbriifolia Vahl. led to the isolation of 12 secondary metabolites including two undescribed iridoids, ...sisymbriifolivaltrate and sisymbriifolioside, and two unreported sesquiterpene lactones, sisymbriifolins A and B. Chemical structures of the isolates were established by extensive 1D and 2D NMR analyses as well as HR-ESI-MS. The in vitro cytotoxic activities of the extract, sub-fractions and isolates on lung (A549), breast (MCF7), gastric (HGC27) and prostate (PC3) cancer cell lines were evaluated by MTS assay. Sisymbriifolivaltrate, didrovaltrate, valtrate, 7-homovaltrate and 1-α-acevaltrate exhibited promising cytotoxic activity on MCF7 cell line with IC50 values ranging from 2.5 to 12.3 μM, while valtrate demonstrated the best cytotoxicity against A549 cells with the IC50 value of 7.5 μM. Valtrate and 7-homovaltrate were found to exert noteworthy cytotoxicity towards HGC27 cell line (IC50 values: 2.3 and 3.7 μM, respectively), whereas valtrate, 7-homovaltrate and 1-α-acevaltrate (IC50 values: 2.3–9.7 μM) were found to be potent cytotoxic against PC3 cells. Among the tested compounds, particularly valepotriate-type iridoids were found to be the main cytotoxic principles of V. sisymbriifolia.
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•Twelve compounds including four undescribed ones were isolated from Valeriana sisymbriifolia.•Two drimane-type rare sesquiterpene lactones (3 and 4) were obtained from V. sisymbriifolia.•Chemotaxonomic significance of isolates within the genus was discussed.•Valepotriate-type iridoids (5–8) showed potent cytotoxicity towards panel of cancer cell lines.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NLZOH, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UILJ, UL, UM, UPCLJ, UPUK, ZAGLJ, ZRSKP
The aim of this study was to isolate the cytotoxic compounds from V. alliariifolia via activity‐guided isolation and to determine the mechanism of actions of the most potent ones. The crude EtOH ...extract as well as CHCl3 and AcOEt subextracts demonstrated remarkable cytotoxic activities against A549, MCF7, HGC27 and PC3 cancer cells. Sequential chromatographic separations on active subextracts yielded 14 secondary metabolites, including 11 iridoids (1–11) most of which belong to non‐glycosidic ester iridoids, two phenylpropanoids (12 and 13) and one lignan (14). The chemical structures of purified compounds were elucidated by NMR and MS analysis. Among the isolates, 7‐deisovaleroylvaltrate (3) was isolated for the first time as a natural product. According to the cytotoxic assay compounds, 2, 4–6 and 8 were found to be the potent cytotoxic compounds (IC50 <10 μM) against at least one of the tested cancer cell lines. Thus, 2, 4–6 and 8 were investigated for their effects on apoptotic, necrotic and autophagic pathways as well as cell cycle progression. They exerted anticancer activities by inducing different cell death mechanisms depending on the cancer cells. The results demonstrated that 2, 4–6 and 8 could be potential anticancer drug leads that deserve further in vivo and clinical studies on the way to discover novel natural compounds with anticancer properties.
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BFBNIB, FZAB, GIS, IJS, KILJ, NLZOH, NUK, OILJ, SBCE, SBMB, UL, UM, UPUK
► The ethanol extract Cistus laurifolius caused remarkable acetylcholinesterase inhibition. ► The n-butanol and ethyl acetate fractions showed potent antioxidant activity. ► Total phenol and ...flavonoid contents were well-correlated with antioxidant activity. ► Three isolated flavonoid derivatives were also tested in the same manner. ► 3,7-O-dimethylkaempferol (3) was found to be the most potent in antioxidant activity assays.
In the current study, the n-hexane, chloroform, ethyl acetate, water, and n-butanol fractions obtained from the main ethanol extract of Cistus laurifolius L. were evaluated for their cholinesterase inhibitory effects against acetyl- (AChE) and butyrylcholinesterase (BChE), at 50, 100, and 200μg/ml, using an ELISA microplate reader. The antioxidative effect of the extract and fractions was also determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, ferrous ion-chelation capacity, and ferric-reducing antioxidant power (FRAP) test systems. Total phenol and flavonoid contents of the extract and fractions were calculated using Folin-Ciocalteau and aluminium chloride reagents. Three flavonoid derivatives; 3-O-methylquercetin (1), 3,7-O-dimethylquercetin (2), and 3,7-O-dimethylkaempferol (3) isolated from the CHCl3 fraction were also tested in the same manner. Our experimental findings indicated that the ethanol extract exerted the highest AChE inhibition (80.07±1.06% at 200μg/ml). The ethyl acetate and n-butanol fractions displayed the best activity against DPPH and FRAP assays.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
The in vitro anti-inflammatory activity profile of the Nerium oleander flower EtOH extract/its subextracts (n-hexane, CH 2Cl 2, EtOAc, remaining H 2O) were evaluated on LPS induced Raw 264.7 ...macrophages. The effects of the crude EtOH extract and its subextracts on nitric oxide (NO) production and cell viability were determined. The most active subextract was determined to be the EtOAc subextract without exerting any toxicity towards Raw 264.7 macrophages. This subextract significantly inhibited NO production of Raw 264.7 macrophages after LPS induction (62.56±1.91% at 200 µg/mL concentration). The levels of iNOS were reduced up to 67.50%. Moreover, this subextract slightly reduced the phosphorylation levels of MAP kinases (p-ERK, p-JNK, p-38). The highest inhibition was observed for ERK phosphorylation, which was inhibited by 20.53% at 200 µg/mL concentration. Through activity-guided fractionation procedures, kaempferol, kaempferol 3-O-β-glucopyranoside and chlorogenic acid were isolated as the main active components. The structures of the active compounds were determined by 2D-NMR techniques and HRMS analysis. All compounds significantly inhibited NO productions. Results of the present study supported the traditional use of N. oleander flowers to treat inflammatory complaints.
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CEKLJ, IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
Hypericum perforatum L., olive oil, Origanum and Salvia species are used for inflammatory disorders and wound healing in traditional Turkish medicine. A new ointment formulation was developed to ...ensure more efficient wound healing based on the traditional knowledge.
Hypericum perforatum L. (Hypericaceae), olive oil (Oleaceae), Origanum Tourn ex L. and Salvia L. species (Lamiaceae) are used against inflammatory disorders and for healing of skin wounds in traditional Turkish medicine. A new ointment formulation was developed to provide more efficient wound healing activity. The content of the formulation was as follows; olive oil extract of flowering aerial parts of Hypericum perforatum L., olive oil, an equivalent mixture of Origanum majorana L. and Origanum minutiflorum Schwrd. et Davis essential oils (Origani aetheroleum), Salvia triloba L. essential oil. The aim of the present study is to assess the wound healing potential of this new formulation by using in vivo and in vitro models as well as histopathological methods.
For the evaluation of wound healing potential of this formulation (HPP crème mit Rotöl ointment) in vivo wound healing experimental models were employed on rats and mice and the efficiency was comparatively assessed against a reference ointment Madecassol®. Tissue sections were also evaluated histopathologically. Furthermore, the wound healing activity of each component was also investigated individually to determine the improvement in the healing capacity of the formulation.
The ointments of HPP crème mit Rotöl and Hypericum perforatum L. demonstrated the highest activities on both wound models when compared to reference ointment Madecassol®, while the other ingredients did not show any remarkable wound healing effect. However, the efficacy of the formulation was remarkably higher than the Hypericum L. ointment alone which was also confirmed by histopathological evaluation. On the other hand, the formulation did not reduce elastase activity in vitro, but inhibited the collagenase activity. HPP crème mit Rotöl also exerted bactericidal and candicidal activities.
The experimental studies revealed that HPP crème mit Rotöl formulation displays remarkable wound healing activity. To be acting on the different stages of wound healing process could be considered as a beneficial effect of the formulation for the treatment of wounds.
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GEOZS, IJS, IMTLJ, KILJ, KISLJ, NUK, OILJ, PNG, SAZU, SBCE, SBJE, UL, UM, UPCLJ, UPUK
Antimicrobial properties of ethnobotanically valuable lichens are well recognized but it is not known how exactly their therapeutic effects on microbial infections occur. Pseudomonas aeruginosa is an ...opportunistic Gram-negative pathogen and its nosocomial strains are responsible for high mortality and morbidity rates. It coordinates pathogenesis and virulence via four quorum sensing (QS) mechanisms called las, rhl, pqs and iqs. The objective of this study is to investigate and report the utilization of lichens for QS inhibition against P. aeruginosa. The inhibitory potentials of Ramalina farinacea (L.) Ach. and Platismatia glauca (L.) W.L. Culb. & C.F. Culb extracts were tested against QS systems of P. aeruginosa using biosensor strains (lasB-gfp, rhlA-gfp and pqsA-gfp). All tested lichen acetone extracts have shown inhibitory effects on las, rhl and pqs QS systems. The percentages of QS inhibition were detected between 75.21% and 92.42% for las, 50.62% and 64.22% for rhl, 47.61% and 69.35% for pqs systems. The highest inhibition was detected for the extracts of R. farinacea collected from Bursa-Alaçam. We concluded that these lichen species have significant anti-QS potentials against P. aeruginosa and they can be further evaluated as alternative biosources in medicine.
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BFBNIB, GIS, IJS, IZUM, KILJ, KISLJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
Phytochemical investigations on the EtOH extract of Clematis viticella led to the isolation of six flavonoid glycosides, isoorientin (1), isoorientin 3′-O-methyl ether (2), quercetin ...7-O-α-L-rhamnopyranoside (3), quercetin 3,7-di-O-α-L-rhamnopyranoside (4), manghaslin (5) and chrysoeriol 7-O-β-D-glucopyranoside (6), one phenylethanol derivative, hydroxytyrosol (7), along with three phenolic acids, caffeic acid (8), (E)-p-coumaric acid (9) and p-hydroxybenzoic acid (10). The structures of the isolates were elucidated on the basis of NMR and HR-MS data. All compounds were isolated from C. viticella for the first time. Compounds 7 and 8 showed significant anti-inflammatory activity at 100 μM by reducing the release of NO in LPS-stimulated macrophages comparable to positive control indomethacin. Compounds 3 and 7 exhibited anti-inflammatory activity through lowering the levels of TNF-α while 1, 3 and 5 decreased the levels of neopterin better than the positive controls.
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BFBNIB, GIS, IJS, KISLJ, NUK, PNG, UL, UM, UPUK
In this study, qualitative and quantitative analysis of commercially available food supplements composed of olive leaf extract and herbal tea products containing olive leaf were evaluated by ...High-Performance Thin-Layer Chromatography (HPTLC) and a newly developed and validated High-Performance Liquid Chromatographic (HPLC) method for their quality assessment. In addition, leaves of two varieties of Olea europaea L. (var. europaea and var. sylvestris) grown in Turkey which were assigned as reference plant materials and their chemical compositions were also comparatively analyzed by HPTLC. Then HPTLC fingerprints of reference plant materials were compared to the marketed olive leaf samples. For quantification of oleuropein and luteolin 7-O-glucoside (L7G) contents in the samples, a simple and fast HPLC method was developed and validated. Consequently, in water and hydroalcoholic extracts of O. europaea var. europaea leaves, oleuropein contents were found to be 15.89% (w/w) and 15.84% (w/w), while L7G contents were 0.75% and 1.23%, respectively. For the reference materials, oleuropein in O. europaea L. var. sylvestris leaves was found to be 12.77% (w/w, in water extract) and 12.36%(w/w, in hydroalcoholic extract), while the concentration of L7G was 0.51% (w/w) and 0.83% (w/w) in water and hydroalcoholic extracts, respectively. Qualitative analysis of the commercial products revealed that fraud was detected in three of eight olive leaf herbal tea bag brands and two of ten olive leaf food supplements. These samples were found either devoid of oleuropein or they had different HPTLC fingerprint profiles than the reference samples.
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IZUM, KILJ, NUK, PILJ, PNG, SAZU, UL, UM, UPUK
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