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The Jurinea Cass. is one of the most important genera within Asteraceae and it comprises about 250 species in total. This genus is known for its numerous biological activities such as antioxidant, antimicrobial, antilipid peroxidation, anticholinesterase, antileishmanial activities. The aim of this study was to determine chemical composition and biological activities of ethanol and n-hexane extracts of three different Jurinea species. For this purpose, different parts of J. mollis, J. cadmea and J. pontica were extracted and totally six n-hexane and six ethanol extracts were obtained. Fatty acid content of n-hexane extracts was determined by GC-FID whereas phenolic and flavonoid content of ethanol extracts by LC-HRMS. Palmitic acid (16:0) was detected as the most abundant fatty acid in all n-hexane extracts with the rates ranging from 42.16%-55.08%, except flowers of J. mollis (JMF) and J. cadmea (JCF). LC-HRMS analysis showed the rutin content of all extracts was higher than other flavonoids, except of J. cadmea flowers, whereas apigenin-7-glucoside was found the most abundant in JCF. Cytotoxic effects of the extracts on HeLa and HEK-293 cells were determined by MTT method, and antioxidant activities were evaluated by DPPH and CUPRAC assays. Ethanol extract of J. mollis flowers significantly inhibited cancerous HeLa cells, with the IC 50 value of 9.683 μg/mL while it was more less toxic on healthy HEK-293 cells. Ethanol extracts of J. mollis flowers and J. mollis steams-leaves (JMSL) showed the highest antioxidant activity by a DPPH inhibition % of 45.516 ± 2.497 and 56.671 ± 1.496, respectively. JMF and JMSL have also the highest CUPRAC values (0.880 ± 0.067 and 1.085 ± 0.152 mmol TR/g DWE, respectively). Total flavonoid content was determined using aluminum chloride colorimetric assay while total tannin and phenolic content by Folin Chiocalteu's reagent. Results showed that JMSL has the highest total phenolic (108.359 ± 6.241 mg GAE/ G DWE) and flavonoid (32.080 ± 4.385 mg QE/ g DWE) contents whereas JMF has the highest tannin content (121.333 ± 17.889 mg TAE/ g DWE). In the light of these results, various parts of Jurinea species may be regarded as alternative sources for cytotoxic and/or antioxidant flavonoids, phenolics and unsaturated fatty acids that can arouse the interest of pharmaceutical, food and cosmetic industries., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Context: Capparis L. (Capparaceae) is grown worldwide. Caper has been used in traditional medicine to treat various diseases including rheumatism, kidney, liver, stomach, as well as headache and toothache., Objective: To isolate and elucidate of the secondary metabolites of the C. ovata extracts which are responsible for their anti-inflammatory activities., Materials and Methods: Buds, fruits, flowers, leaves and stems of C. ovata Desf. was dried, cut to pieces, then ground separately. From their dichloromethane/hexane (1:1) extracts, eight compounds were isolated and their structures were elucidated by NMR, mass spectroscopic techniques. The effects of compounds on the expression of inflammatory cytokines in SH-SY5Y cell lines were examined by qRT-PCR ranging from 4 to 96 µM. Cell viability was expressed as a percentage of the control, untreated cells., Results: This is a first report on isolation of triterpenoids and steroids from C. ovata with anti-inflammatory activity. One new triterpenoid ester olean-12-en-3β,28-diol, 3β-pentacosanoate ( 1 ) and two new natural steroids 5α,6α-epoxycholestan-3β-ol ( 5 ) and 5β,6β-epoxycholestan-3β-ol ( 6 ) were elucidated besides known compounds; oleanolic acid ( 2 ), ursolic acid ( 3 ), β-sitosterol ( 4 ), stigmast-5,22-dien-3β-myristate ( 7 ) and bismethyl-octylphthalate ( 8 ). mRNA expression levels as EC 10 of all the tested seven genes were decreased, particularly CXCL9 (19.36-fold), CXCL10 (8.14-fold), and TNF (18.69) by the treatment of 26 µM of compound 1 on SH-SY5Y cells., Discussion and Conclusions: Triterpenoids and steroids isolated from C. ovata were found to be moderate-strong anti-inflammatory compounds. Particularly, compounds 1 and 3 were found to be promising therapeutic agents in the treatment of inflammatory and autoimmune diseases.

Background: The role of Fe+2, Cu+2 and Zn+2 in facilitating aggregation of Amyloid β (Aβ) and consequently, the progression of Alzheimer's disease (AD) is well established., Objective: Development of non-toxic metal chelators is an emerging era in the treatment of AD, in which complete success has not been fully achieved. The purpose of this study was to determine plant extracts with high metal chelator and to encapsulate them in nano-micellar systems with the ability to pass through the Blood Brain Barrier (BBB)., Methods: Extracts of 36 different Anatolian plants were prepared, total phenolic and flavonoid contents were determined, and the extracts with high content were examined for their Fe+2, Cu+2 and Zn+2 chelating activities. Apolipoprotein E4 (Apo E) decorated nano-formulations of active extracts were prepared using Poly (Lactide-co-Glycolide) (PLGA) (final product ApoEPLGA) to provide BBB penetrating property., Results: Verbascum flavidum aqueous extract was found as the most active sample, incubation of which, with Aβ before and after metal-induced aggregation, resulted in successful inhibition of aggregate formation, while re-solubilization of pre-formed aggregates was not effectively achieved. The same results were obtained using ApoEPLGA., Conclusion: An optimized metal chelator nano-formulation with BBB penetrating ability was prepared and presented for further in-vivo studies., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Context: Origanum (Lamiaceae) has been used in food and pharmaceutical industries., Objective: Isolation and identification of bioactive compounds from Origanum rotundifolium Boiss. and investigation of their antiproliferative and antioxidant activities., Materials and Methods: The aerial part of O. rotundifolium was dried and powdered (1.0 kg ±2.0 g) then extracted with hexane, ethyl acetate, methanol and water. Solvent (3 × 1 L) was used for each extraction for a week at room temperature. The aqueous extract was partitioned with ethyl acetate (3 × 1 L) to yield the water/EtOAc extract subjected to chromatography to isolate the active compounds. The structures of isolated compounds were elucidated by 1 D, 2 D NMR and LC-TOF/MS., Results: Apigenin (1), ferulic acid (2), vitexin (3), caprolactam (4), rosmarinic acid (5), and globoidnan A (6) were isolated and identified. Globoidnan A (6), vitexin (3), and rosmarinic acid (5) revealed the excellent DPPH • scavenging effect with IC 50 values of 22.4, 31.4, 47.2 μM, respectively. Vitexin (3) (IC 50 3.6), globoidnan A (6) (IC 50 4.6), apigenin (1) (IC 50 8.9) and ferulic acid (2) exhibited more ABTS •+ activity than standard Trolox (IC 50 13.8 μg/mL). Vitexin (3) revealed the most antiproliferative activity against HeLa, HT29, C6 and Vero cells lines with IC 50 values of 35.6, 32.5, 41.6, 46.7 (μM), respectively., Discussion and Conclusion: Globoidnan A (6) has the most antioxidant effects on all assays. This has to do with the chemical structure of the compound bearing the acidic protons. Vitexin (3) could be a promising anticancer agent.

Since ancient times, Capparis species have been widely used in traditional medicine to treat various diseases. Our recent investigations have suggested Capparis ovata's potential anti-neuroinflammatory application for the treatment of multiple sclerosis (MS). The present study was designed to precisely determine the underlying mechanism of its anti-neuroinflammatory effect in a mouse model of MS. C. ovata water extract (COWE) was prepared using the plant's fruit, buds, and flower parts (Turkish Patent Institute, PT 2012/04,093). We immunized female C57BL/6J mice with MOG35-55/CFA. COWE was administered at a daily dose of 500mg/kg by oral gavage either from the day of immunization (T1) or at disease onset (T2) for 21days. Gene expression analysis was performed using a Mouse Multiple Sclerosis RT² Profiler PCR Array, and further determinations and validations of the identified genes were performed using qPCR. Whole-genome transcriptome profiling was analyzed using Agilent SurePrint G3 Mouse GE 8X60K microarrays. Immunohistochemical staining was applied to brain sections of the control and treated mice to examine the degree of degeneration. COWE was further fractionated and analyzed phytochemically using the Zivak Tandem Gold Triple Quadrupole LC/MS-MS system. COWE remarkably suppressed the development of EAE in T1, and the disease activity was completely inhibited. In the T2 group, the maximal score was significantly reduced compared with that of the parallel EAE group. The COWE suppression of EAE was associated with a significantly decreased expression of genes that are important in inflammatory signaling, such as TNFα, IL6, NF-κB, CCL5, CXCL9, and CXCK10. On the other hand, the expression of genes involved in myelination/remyelination was significantly increased. Immunohistochemical analysis further supported these effects, showing that the number of infiltrating immune cells was decreased in the brains of COWE-treated animals. In addition, differential expression profiling of the transcriptome revealed that COWE treatment caused the down regulation of a group of genes involved in the immune response, inflammatory response, antigen processing and presentation, B-cell-mediated immunity and innate immune response. Collectively, these results suggest anti-neuroinflammatory mechanisms by which COWE treatment delayed and suppressed the development of EAE and ameliorated the disease in mice with persistent clinical signs., (Copyright © 2016 Elsevier B.V. All rights reserved.)

Context: In Turkey, Veronica species (Plantaginaceae) have been used as a diuretic and for wound healing in traditional medicine., Objective: To examine the fatty acid and essential oil profiles, the antioxidant, anticholinesterase, antimicrobial, and DNA damage effects of Veronica thymoides P.H. Davis subsp. pseudocinerea M.A. Fischer as a potential source of natural active compounds., Materials and Methods: GC/MS was used to analyze essential oil and fatty acid obtained from whole plant. The antioxidant activity was evaluated by the β-carotene-linoleic acid test system, DPPH-free and ABTS cation radicals scavenging, and cupric reducing antioxidant capacity assays. The anticholinesterase and antimicrobial activities were determined by Ellman and broth macrodillution methods, respectively. The effect of the methanol extract on DNA cleavage was investigated., Results: Hexatriacontene (21.0%) was found to be the main constituent in essential oil, and linoleic acid (25.2%) and palmitic acid (20.6%) in fatty acid. Methanol extract demonstrated the best IC50 values in lipid peroxidation (49.81 ± 0.31 µg/ml) and DPPH-free radical scavenging activity (15.32 ± 0.17 µg/ml). Methanol and water extracts possessed strong ABTS cation radical scavenging activity with IC50 values 9.15 ± 0.28 and 8.90 ± 0.1  µg/ml, respectively. The acetone extract exhibited moderate butyrylcholinesterase inhibitory activity. The highest antimicrobial activity was determined in methanol extract against Escherichia coli with 31.25 µg/ml MIC value. Inhibition of methanol extract on plasmid DNA cleavage by OH radicals was found to be 93.32% at 500 µg/ml., Conclusion: The methanol extract having strong antioxidant and DNA damage effects could be investigated phytochemically to find natural active compounds.

Trifolium nigrescens was researched for its chemical constituents for the first time. Bioassay-guided isolation of the EtOAc extract from the leaves of T. nigrescens resulted in the purification of a new biflavone, 4''',5,5″,7,7″-pentahydroxy-3',3'''-dimethoxy-3-O-β-d-glucosyl-3″,4'-O-biflavone (1) along with eleven known compounds consisting of three phenolics (2-4), and eight flavonoid glycosides (5-12). Their structures were determined by extensive 1D and 2D NMR, and MS data analyses. The isolated compounds were evaluated for their antioxidant activity and inhibitory activity on mushroom tyrosinase. Highly potent inhibitions were found by compounds 7 (IC50 = 0.38 mM), 8 (IC50 = 0.19 mM), and 12 (IC50 = 0.26 mM) when compared with standard tyrosinase inhibitors kojic acid (IC50 = 0.67 mM) and l-mimosine (IC50 = 0.64 mM). The antioxidative effect of the isolated compounds and the extracts were determined by using β-carotene-linoleic acid, DPPH(•) scavenging, ABTS(+•) scavenging, superoxide scavenging, and CUPRAC assays. The experimental findings indicated that all the compounds demonstrated activity in all antioxidant activity tests employed except for the compounds 2-6. Compounds 2-6 showed moderate activity only in ABTS(+•) scavenging assay. The new compound 1 exhibited better activity than standard α-tocopherol in DPPH(•) scavenging, and ABTS(+•) scavenging assays. The results show that T. nigrescens can be regarded as a potential source of antioxidant compounds and tyrosinase inhibitors of significance in both the pharmaceutical and food industries.

Background and Aims: Ankaferd Blood Stopper (ABS) is a herbal extract obtained from five different plants. It has a therapeutic potential for the management of external hemorrhage and controlling gastrointestinal bleeding. However, ABS's effects are not unknown on gastrointestinal systems. The aim of this study was to assess the effect of short- and long-term systemic exposure and gastrointestinal safety following the oral administration of high-dose ABS in rats., Methods: Eighteen healthy adult male rats were included into the study. The rats were divided into 4 groups: group A was fed with high dose ABS (2ml/Kg) for one week, group B for one month, group C for three months and group D's diet did not contain any ABS. On termination of the ABS treatment, the gastrointestinal system from the esophagus to the anus and the liver were surgically removed and histological investigated., Results: During the study period, there was no mortality; signs of intoxication in any of the studied groups. No gastrointestinal tissue fibrosis, dysplasia, or metaplasia was detectable in any of the groups. The stomach had a normal morphology in all groups. However, the other gastrointestinal tract sections showed mucosal inflammation, goblet cell decrements, and intra-epithelial lymphocyte infiltration. The most common changes were mucosal inflammation in all rats in group B and C. Frequency of inflammation was greater in groups B and C in comparison to group A (P= 0.001). Loss of goblet cell and intra-epithelial lymphocyte infiltration were not significantly different between groups A and B (P=0.308 and P=0.189, respectively). However, there was significantly higher intra-epithelial lymphocyte infiltration in group C than in group A (P=0.04). Histopathological examination of the liver showed no inflammation, fibrosis, bile duct destruction or proliferation in any of the groups. However, each groups revealed vascular dilatation and erythrocyte accumulation at the sinusoidal structures of the liver., Conclusions: ABS seems to be a safe agent and it can be used for hemorrhage originated from gastric lesions. Further work needs to be done to establish whether ABS leads to be used to stop gastrointestinal bleeding.

Ankaferd Blood Stopper (ABS) is an herbal extract that enhances mucosal healing. The aim of this study was to investigate the efficacy of ABS on the healing of the esophagus and prevention of stricture development after esophageal caustic injuries in rats. The study included 50 rats. Rats were divided into five groups: group 1 (no injury, sham surgery), group 2 (injury + no ABS + study after 2 weeks of injury), group 3 (injury + ABS + study after 2 weeks of injury), group 4 (injury + no ABS + study after 4 weeks of injury), and group 5 (injury + ABS + study after 4 weeks of injury). Standard esophageal burn injury was created by applying 50% NaOH solution to distal esophagus of about 1.5 cm. To rats in the sham group, isotonic solution was given instead of NaOH. ABS (2 mL/day) was given via oral route to group 3 and 5 rats. Fourteen days (group 2 and 3) and 28 days (group 4 and 5) later, all the live rats were killed. The distal esophageal segments of all rats were removed and divided into two equal parts for biochemical and histopathological examination. Mortality rate, weight changes, inflammation, stenosis index (SI), and biochemical measurements were evaluated. The SI was found as 0.31 ± 0.03 in group 1, 0.533 ± 0.240 in group 2, 0.568 ± 0.371 in group 3, 0.523 ± 0.164 in group 4, and 0.28 ± 0.03 in group 5. The SI and inflammation in ABS-treatment group 5 was significantly lower than that in non-treatment group 4 (P= 0.005). There were no significant differences between inflammation and SI among other groups. The mortality rate was 14.2% in group 1, 37.5% in untreated group 2, 14.2% in ABS-treated group 3, 80% in untreated group 4, and 33.3% in ABS-treated group 5. The mortality rate in group 4 was significantly higher than other groups (P= 0.025). Decrease rates in mean body weights of the groups were as follows: group 1, 1%; group 2, 15%; group 3, 14%; group 4, 46%; and group 5, 15%. Biochemical tests other than albumin and creatinine were comparable among the groups. Treatment with ABS prevents inflammation, scar formation, weight loss, and mortality in esophageal caustic injuries. Additional studies to evaluate the clinical benefits of ABS in esophageal caustic injury are recommended., (© 2011 Copyright the Authors. Journal compilation © 2011, Wiley Periodicals, Inc. and the International Society for Diseases of the Esophagus.)

Prangos platychlaena has been used in traditional medicine in eastern Turkey. It stops bleeding and heals the scars when applied externally. When the isolated coumarins were tested against bacterial strains, only a slight activity was obtained.

A simplified hplc system is described for the detection of compounds capable of binding to DNA. Compounds known to interact with DNA were found to invoke a positive response with this system, and the concentration-dependence and sensitivity were determined. When applied to 17 randomly selected plant extracts, five elicited a positive response and, of these, four were subsequently found to be cytotoxic with cultured KB or P-388 cells. As described in a companion paper, one of these extracts (derived from Albizia amara) has been further processed and found to contain a group of structurally-unique macrocyclic alkaloids that demonstrate a variety of biological activities. Therefore, this approach should prove a value in facilitating the identification of plant extracts that contain substances capable of binding to DNA and the subsequent activity-directed fractionation for the procurement of active principles. As a prescreen or monitor, these relatively uncomplicated hplc procedures can be used in laboratories not prepared to perform more complicated or costly bioassay techniques. Thus, the pool of potentially active novel chemical substances to be considered for more advanced testing could be increased.

Salvia hypargeia Fisch. et Mey. (Lamiaceae) root extract, among 16 Salvia extracts, showed the highest activity against the human ovarian cancer cell line. Bioactivity-guided fractionation of this plant extract has yielded four abietane-type diterpenes [5,6-didehydro-7-hydroxytaxodone (1), 14-deoxycoleon U (= 6-hydroxysalvinolone) (2), demethylcryptojaponol (3), and salvicanaric acid (4)] two triterpenes (lupeol and lupeol-3-acetate), and a fatty acid mixture consisting mainly of palmitic acid (51.6%) and palmitoleic acid (6.4%). Compounds 2 and 3 were found to be active against A2780 human ovarian cancer cell line with IC50 values of 3.9 and 1.2 μ g/mL, respectively, and the fatty acid composition was the most active part of the extract (IC50 = 0.6 μ g/mL). [ABSTRACT FROM AUTHOR]

This is the first study on phytochemical analysis and biological evaluation of Hypericum capitatum Choisy var. capitatum (HCC) endemic to Turkey with exception of essential oil analysis. Hyperoside and isoquercetin (25.7 ± 0.02 and 17.8 ± 0.02 μg/mg extract, respectively) were determined as the main compounds of the methanol extract. The major compounds of essential oil of HCC were found to be spathulenol and iso-longifolene (12.9% and 11.2%, respectively), and linoleic and palmitic acids (26.8% and 18.3%, respectively) were the main fatty acids. The methanol extract whose antioxidant activities studied for the first time was found to have moderate activity in β-carotene bleaching method (IC 50 :41.69 ± 1.29 μg/mL) and was found to be the most active extract in scavenging of DPPH free radical (IC 50 :16.82 ± 0.58 μg/mL) and ABTS cation radical (IC 50 :9.24 ± 0.28 μg/mL) and CUPRAC assays. Among the prepared four extracts of HCC, the methanol extract showed highest activity against Escherichia coli with an MIC value of 10 μg/mL, and the methanol extract was also found to have high DNA damage protective activity. The methanol extract exhibited high butyrylcholinesterase inhibitory activity (70.74%). Thus, H. capitatum var. capitatum can be regarded as a potential natural antioxidant, antimicrobial, anticholinesterase source and DNA damage inhibitor. [ABSTRACT FROM AUTHOR]