Can Carpobrotus edulis, heal incisional and excisional wounds on the skin?

OBJECTIVES: This study aimed to investigate the wound healing activity of liposomal Carpobrotus edulis powder extract (CEPE) formulation on incisional and excisional wounds in rat. BACKGROUND: In the event of any damage, the damaged tissue undergoes a process of regenerating itself, which is called wound healing. METHODS: Centella asiatica extract (CAE) was used as the reference molecule in the study. The wound healing process was tested by using the excisional and incisional wound model. On the 12th day of the study, maximum stress, stress, % of elongation values were evaluated in the incisional wound. Also; histological parameters and macroscopic photographic analyses were evaluated in the excisional wound. RESULTS: In the photo evaluations, the improvement was more prominent in both CAE and CEPE groups than in the control group. Histological evaluation showed that CEPE group had significant wound healing activity compared to the control and CAE groups. Axial tensile-elongation experiments in incisional wound tissue show that there was no significant difference between CAE and CEPE groups. CONCLUSION: Liposomal formulations of C.edulis extract were found to have positive effects on the healing process, both on excisional and incisional wound tissues (Tab. 2, Fig. 3, Ref. 30).

Assessment of plasma microRNA potentials as a non-invasive biomarker in patients with axial spondyloarthropathy.

OBJECTIVE: It is assumed that abnormally expressed MicroRNAs (miRNAs) may be present in the plasma of patients with radiographic axial spondyloarthropathy (rad-AxSpA). Thus, the present study was conducted with the aim of investigating the expression profile of miRNAs in patients with rad-AxSpA. PATIENTS AND METHODS: A total of 15 patients diagnosed with rad-AxSpA according to the Assessment of the SpondyloArthritis International Society (ASAS) classification criteria and nine healthy controls matched for age and gender were included in the study. Demographic data were collected, and disease activity was evaluated using the Bath Ankylosing Spondylitis Disease Activity Index (BASDAI). Peripheral blood samples were collected, and miRNAs were extracted. The expression of microRNAs was analyzed using quantitative Real Time-Polymerase Chain Reaction (qRT-PCR) by the miScript miRNA PCR Array Human Inflammatory Response and Autoimmunity. RESULTS: A total of 84 miRNA profiles were evaluated, and expressions in the study and control groups were compared. When compared to the control group, 6 miRNAs (miR-125b-5p, miR-144-3p, miR-19a-3p, miR-20a-5p, miR-29c-3p, miR-30b-5p) were detected to be upregulated, and 42 miRNAs were detected to be downregulated in the rad-AxSpA group. A p-value < 0.05 was accepted as statistically significant. A significant association was found between miR-145-5p and BASDAI (p = 0.04941). MiR-144-3p, miR-302b-3p, miR-381-3p, miR-497-5p, miR-511-5p, and miR-9-5p were found to be significantly upregulated in the HLA-B27+ patients (p = 0.03063). CONCLUSIONS: Abnormal miRNA expressions were detected in the plasma of the patients with rad-AxSpA. It was concluded that comprehensive studies should be continued to define these miRNAs as diagnostic biomarkers for rad-AxSpA in order to detect its association with Ankylosing Spondylitis disease activity.

The role of the eNOS G894T and T-786C gene polymorphism in the development of ascites in cirrhosis.

OBJECTIVE: Increased nitric oxide (NO) production in cirrhotic patients causes splanchnic vasodilation, leading to the development of the hyperdynamic circulatory syndrome. One factor that influences plasma NO concentration is eNOS gene polymorphism; consequently, the aim of this study was to investigate whether the eNOS gene G894T and T-786C polymorphisms play any role in the development of ascites in such patients. PATIENTS AND METHODS: Three groups were created: 70 cirrhotic patients with ascites, 69 cirrhotic participants without ascites (stable cirrhosis), and 60 healthy controls. Polymorphisms were determined using polymerase chain reaction (PCR) and melting curve analysis. The plasma nitrite (NO marker) level was measured by deploying the spectrophotometric Griess reaction. RESULTS: Plasma nitrite levels in the cirrhosis with ascites and stable cirrhosis groups were significantly higher than in the controls (p < 0.0001). The frequency of GG, GT, and TT genotypes for the eNOS G894T polymorphism in the cirrhosis with ascites group was 55.7%, 38.6%, and 5.7% respectively, while in the stable cirrhosis group these figures were 60.9%, 36.2%, and 2.9%. In the controls, the distribution was 63.3%, 33.3%, and 3.3%, respectively. The frequency of TT, TC, and CC genotypes for the eNOS-786C polymorphism in the first group was 52.9%, 34.2%, and 12.9% respectively; in the second group, this was 46.4%, 42%, and 11.6%, and in the controls, 48.3%, 46.7%, and 5%. There were no significant differences in genotype and allele distributions of the eNOS-786C and eNOS G894T polymorphisms among the groups. CONCLUSIONS: Plasma nitrite concentration is enhanced in cirrhotic patients, and there is no relationship between the G894T and eNOS-786C polymorphisms and the development of ascites.

Cytotoxic and immunomodulatory effects of Ebenus boissieri Barbey on breast cancer cells.

We aimed to determine the cytotoxic and immunomodulatory effects of hydroalcoholic extracts of the roots and aerial parts of Ebenus boissieri (EB) on breast cancer MDA-MB231 cells and the non-cancerous human embryonic kidney cell line, 293T. Cell viability was determined by MTT assay, trypan blue exclusion, and Live/Dead Viability/Cytotoxicity assay. Apoptosis was evaluated by measuring the activity of caspase-2, 3, 6, 8, and 9. Tumor necrosis factor (TNF)-α and interferon (IFN)-g release was assayed by ELISA, and protein expression of caspase-3, TNF-a, and IFN-g was determined by western blot. The results of this study revealed that MDA-MB231 cell viability was reduced in a dose-dependent manner by the aerial and root extract of EB at 72 h with a half-maximal inhibitory concentration (IC50) of 41.1 ± 2.76 and 65 ± 1.09 µg/mL, respectively. In contrast, neither the aerial nor the root extracts of this plant inhibited the proliferation of 293T cells at doses up to 1000 µg/mL. There was a time-dependent increase in caspase activity, especially caspase-3 and caspase-9. The levels of TNF-aand IFN-g significantly increased in MDA-MB231 cells treated with aerial extract. In conclusion, the extracts of EB induced apoptosis in breast cancer cells by altering the levels of caspases, TNF-a, and IFN-g. The components and precise modes of action of EB have not yet been determined. However, potential antitumor and immunomodulatory activity was observed along with selectivity against cancer cells in vitro, suggesting that hydroalcoholic extracts of this plant are worthy of additional study.

XPD and XRCC1 gene polymorphism in patients with normal and abnormal cervical cytology by pap smear.

AIM: The purpose of the present study was to identify the role of abnormalities in DNA repair pathways by measuring the XPD and XRCC1 gene polymorphisms. MATERIALS AND METHODS: Thirty-five patients with abnormal cervical cytology (study group) and 10 women with normal cytology (control group) were included in the study. The polymorphisms of XRCC1 Arg194Trp, XRCC1 Arg399Gln and XPD Lys751Gln genes were investigated from the blood samples. RESULTS: There was no statistically significant difference in allele frequencies of XPD gene among the groups (p = 0.097), while XRCC1R399Q gene polymorphism was strikingly more frequent in the study group than that of control cases (p = 0.029). The prevalence of XRCC1R194W gene polymorphism on the other hand, was similar between the groups (p = 0.579). CONCLUSIONS: Patients with abnormal and normal cervical cytology have similar XPD gene polymorphism. However, the frequency of gene polymorphism in XRCC1 Arg 399 Gln codon was significantly higher in abnormal cervical cytology group.

Bioassay-guided isolation of kaempferol-3-O-beta-D-galactoside with anti-inflammatory and antinociceptive activity from the aerial part of Calluna vulgaris L.

Calluna vulgaris L. (Ericaceae) is used for the treatment of various inflammatory ailments in traditional medicines. In order to evaluate this ethnobotanical information, its anti-inflammatory and antinociceptive activities were studied using in vivo experimental models in mice. The ethanolic extract of the plant was first fractionated into five extracts; namely, n-hexane, chloroform, ethyl acetate (EtOAc), n-butanol, and water fractions. Among them, the EtOAc Fr. was found to be the most effective and was further subjected to bioassay-guided fractionation and isolation procedures. After successive column chromatography applications, on Sephadex LH-20 and silica gel, a component, which is responsible for the above-mentioned activities of this species of Turkish origin, was isolated and its structure was elucidated as kaempferol-3-O-beta-D-galactoside, a common flavonol derivative by means of spectral techniques.

Micronucleus frequency in peripheral blood lymphocytes and exfoliated buccal cells of untreated cancer patients.

Some genetic diseases may increase the cellular instability. Since most human tumors have some genetic base, this study was undertaken for the genetic instability in cancer patients by micronucleus analysis, a mutation-screening test, which is more practical and economic technique than metaphase analysis carried out for chromosomal aberrations. Genetic changes were assessed in untreated cancer patients (lung, stomach and colon cancer) by different genotoxical screening methods; the cytokinesis-block micronucleus test and the buccal mucosa cell micronucleus test. The evaluation of micronuclei number in peripheral blood lymphocytes and buccal cells showed a genomic instability in somatic cells. There was a significant increase in the number of micronuclei in cancer patients prior to the initiation of chemotherapy, and/or radiotherapy compared with healthy human subjects. Furthermore, there was no significant difference between smokers and non-smoking groups or male and female groups. These results suggest that cancer in humans is characterized by an increase of chromosomal damage and thus, the micronucleus assay carried out here may be useful in routine cytogenetic studies of cancer.

Bioassay-guided evaluation of anti-inflammatory and antinociceptive activities of pistachio, Pistacia vera L.

The ethanolic and aqueous extracts prepared from different parts of Pistacia vera L. (Anacardiaceae) as well as its oleoresin were evaluated for their in vivo anti-inflammatory and antinociceptive activities. Among the extracts screened, only the oleoresin was shown to possess a marked anti-inflammatory activity against carrageenan-induced hind paw edema model in mice without inducing any gastric damage at both 250 and 500 mg/kg doses whereas the rest of the extracts were totally inactive. While the oleoresin was found to display significant antinociceptive activity at 500 mg/kg dose, the ethanolic and aqueous extracts belonging to fruit, leaf, branch and peduncle of Pistacia vera did not exhibit any noticeable antinociception in p-benzoquinone-induced abdominal contractions in mice. Fractionation of the oleoresin indicated the n-hexane fraction to be active, which further led to recognition of some monoterpenes, mainly alpha-pinene (77.5%) by capillary gas chromatography-mass spectrometry (GC-MS) as well as the oleoresin itself. alpha-Pinene was also assessed for its antinociceptive and anti-inflammatory activities in the same manner and exerted a moderate anti-inflammatory effect at 500 mg/kg dose.

Synthesis and analgesic and antiinflammatory activity of methyl 6-substituted-3(2h)-pyridazinone-2-ylacetate derivatives.

A series of methyl 6-substituted-3(2H)-pyridazinone-2-ylacetates 9 were synthesized and their analgesic and anti-inflammatory effects were evaluated in the phenylbenzoquinone-induced writhing test (PBQ test) and carrageenan-induced paw edema method, respectively. Side effects of the compounds were examined on gastric mucosa. None of the compounds showed gastric ulcerogenic effect compared with reference nonsteroidal anti-inflammatory drugs. Methyl 6-(4-(4-fluorophenyl)piperazine)-3(2H)-pyridazinone-2-ylacetate 9e was found to be more active than acetylsalicylic acid (ASA). Methyl 6-(4-(2-ethoxyphenyl)piperazine)-3(2H)-pyridazinone-2-ylacetate 9c has shown an anti-inflammatory activity as compared to the standard compound indometacin at the carrageenan-induced paw edema method.A significant dependence of the anti-inflammatory effect on the substituents has been observed. The pharmacological study of these compounds confirms that modification of the chemical group at the position 6 of the 3(2H)-pyridazinone system influences analgesic and anti-inflammatory activities. The structures of these new pyridazinone derivatives were confirmed by their IR and (1)H-NMR spectra and elemental analysis.

Callus formation and cucurbitacin B accumulation in Ecballium elaterium callus cultures.

Ecballium elaterium fruit juice is used for the treatment of sinusitis in Turkish folk medicine. The aim of this study was to increase the yield of cucurbitacin B, an anti-inflammatory compound previously isolated in various organs of E. elaterium, through tissue culture techniques. Higher yields of cucurbitacin B (1.126%) were obtained from the first subculture calluses from stem nodes in the presence of benzyl adenine (BA; 1 mg/l) and naphtalene acetic acid (NAA; 0.1 mg/l) in comparison with the yields obtained from plant material (0.01%).

Synthesis and pharmacological activities of some new 2-[1-(6-methoxy-2-naphthyl)ethyl]-6-(substituted)benzylidene thiazolo[3,2-b]-1,2,4-triazole-5(6H)-one derivatives.

In this study, thirteen new compounds having a 2-[1-(6-methoxy-2-naphthyl)ethyl]-6-(substituted)benzylidenethiazolo[3,2-b]- 1,2,4-triazole-5(6H)-one structure were synthesised using N-[2-(6-methoxy-2-naphthyl)propanoyloxysuccinimide, N-[2-(6-methoxy-2-naphthyl)propanoyl]thiosemicarbazide and 3-[1-(6-methoxy-2-naphthyl)ethyl]-5-mercapto-1,2,4-triazole. The structures and physical properties of the compounds were elucidated by IR, 1H NMR, mass spectroscopy and elemental analysis. The antiinflammatory activity and gastric ulceration potential of the compounds were tested using naproxen as a reference compound.

Comparative evaluation of the flavonoid content in officinal Tiliae flos and Turkish lime species for quality assessment.

Lime flowers are used for various medicinal purposes in phytotherapy. Flavonoids, volatile oil and mucilage components are known as the active ingredients. In European Pharmacopoeia (EP), a simple thin-layer chromatographic (TLC) technique, which based on the analysis of the flavonoid composition was defined for the qualitative analysis of the drug. In this study, flavonoid composition in the flowers, bracts and leaves of the officinal species, Tilia platyphyllos were studied using a reversed-phase high performance liquid chromatographic (HPLC) technique, in order to develop a rapid, reliable and accurate method for quantitative analysis. The results were further compared with in those parts of two common species growing in Turkey, Tilia rubra and Tilia argentea. Results of the present study revealed that flavonoid composition of each lime species possesses a specific fingerprint HPLC chromatogram depending upon the parts used and evaluation of the data might be helpful in the quality assurance as well as determination of adulteration of the crude drug.

Synthesis of some thiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones and their novel Michael addition products with anti-inflammatory activities.

In this study, 21 new compounds having 2-methyl-6-benzylidenethiazolo[3,2-b]-1,2,4-triazol-5(6H)-one (2-4) and 2-methyl-6-(alpha-aminobenzyl)thiazolo[3,2-b]-1,2,4-triazole-5-ol (2a-4g) structures were synthesized. The structures of the compounds were proved by spectral and elemental analysis. All of the compounds synthesized were tested for their anti-inflammatory actively and ulcerogenic potential in mice at 10, 20 and 40 mg/kg dose levels. Compound 4b showed higher anti-inflammatory activity than the analogue derivatives and indometacin (CAS 53-86-1), used as a reference drug, at 10 mg/kg dose level. Generally, the compounds were found to be more reliable than indometacin since they did not cause any reaction in the stomach.

Traditional medicine in Turkey X. Folk medicine in Central Anatolia.

Traditional medicine used in Central Anatolia; Ankara, Kayseri, Nigde and south-eastern parts of Karaman and Konya provinces have been studied. Two hundred and ninety one folk remedies obtained from 103 plant species belonging to 40 families and 4 animal species are reported with their vernacular names, parts used, methods of preparing remedies and therapeutic usage.

In vitro inhibitory effects of Daphne oleoides ssp. oleoides on inflammatory cytokines and activity-guided isolation of active constituents.

Aerial parts of Daphne oleoides Schreber ssp. oleoides (Thymelaeaceae) are used to treat rheumatoid arthritis and lumbago in Turkish folk medicine. In order to evaluate folkloric utilization, in vitro inhibitory effects of the ethyl acetate extract and fractions obtained from this extract on interleukin 1 (IL-1alpha, IL-1beta) and tumour necrosis factor (TNF-alpha) biosynthesis were studied. Through chemical isolation techniques and activity-guided fractionation process, seventeen compounds were isolated and their structures were elucidated (numbered 1-17). Diterpenoids genkwadaphnin (3) and 1,2-dehydrodaphnetoxin (6) and a coumarin derivative daphnetin (9) showed potent inhibitory activity and were found to be the main active ingredients. Furthermore, gnidilatin (4), gnidilatin-20 palmitate (5), genkwadaphnin-20-palmitate (7) and gnidicin-20-palmitate (8), having diterpenoid structure, and eudesmine (12), wikstromol (13) and matairesinol (14), having lignan structure, were determined to possess moderate inhibitory activity and may have a contributory role in the effect of the remedy.

Isolation and characterization of free radical scavenging flavonoid glycosides from the flowers of Spartium junceum by activity-guided fractionation.

Spartium junceum L. (Fabaceae) flowers are used for the treatment of peptic ulcers in Turkish folk medicine. The possible superoxide dismutase-like activity of the extracts, fractions and constituents obtained through activity-guided fractionation were studied by using in vitro electron spin resonance spectrometry, in order to explain the role of antioxidant principles in the potent antiulcerogenic activity of the extract. Despite the fact that the triterpene, spartitrioside, which was previously reported as the active antiulcerogenic constituent of the flowers was found almost inactive, the flavonoid-rich fractions showed potent antioxidant activity. Five flavonoid glycosides bearing catechol structure in ring B were isolated from the butanol extract and their structures were elucidated using 1H- and 13C-NMR techniques as isoquercitrin (quercetin 3beta-glucoside) (1,); luteolin 4'beta-glucoside (2); quercetin 3, 4'-diglucoside (3); azaleatin 3beta-glucoside (quercetin 5-methylether 3beta-glucoside) (4), quercetin 4'beta-glucoside (5). Flavonoids (2) and (4) showed the highest in vitro antioxidant activity with 22.59 and 19.08 U/ml, respectively.

Hepatoprotective effects of Turkish folk remedies on experimental liver injury.

Seven plants which are used in Turkish folk medicine were studied for possible hepatoprotective effects. These plants are Carduus acanthoides and C. nutans (Asteraceae), Cichorium intybus (Asteraceae), Fumaria asepalae and F. vailantii (Fumariaceae), Gentiana olivieri (Gentianaceae) and Plantago lanceolata (Plantaginaceae). Stems, bracts and receptaculum of Cynara scolymus were used as natural reference drugs. Effects of the ethanolic extracts were studied using the carbon tetrachloride-induced hepatotoxicity model in rats. The extracts of F. vailantii and G. olivieri significantly prevented the elevation of plasma and hepatic malondialdehyde formation (evidence of lipid peroxidation) as well as enzyme levels (AST and ALT) in acute liver injury, which might be ascribed to their potent hepatoprotective activity. Liver sections were also studied histopathologically to confirm the biochemical results.

6-Benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones substituted withibuprofen: synthesis, characterization and evaluation of anti-inflammatory activity.

In this study, the synthesis of 3-[1-(4-(2-methylpropyl)phenyl)ethyl]-1,2,4-triazole-5-thione (2) and its condensed derivatives 6-benzylidenethiazolo[3,2-b]-1,2, 4-triazole-5(6H)-ones (2a-u) are described. The structures of the compounds were elucidated by spectral and elemental analysis. In the pharmacological studies, anti-inflammatory activities of these compounds have been screened. Among the compounds examined, the compounds 2 and 2g possessed the most prominent and consistent activity. In gastric ulceration studies the synthesized compounds were generally found to be safe at a 200 mg/kg dose level.

Labdane diterpenoids from Marrubium globosum ssp. globosum.

A new labdane type diterpenoid, marrubiglobosin, was isolated from the aerial parts of Marrubium globosum ssp. globosum together with the known diterpenoids, marrubiin and marrubinone B. The structure of this new compound was elucidated by spectral methods.