Biological Activities of the Fruit Essential Oil, Fruit, and Root Extracts of Ferula drudeana Korovin, the Putative Anatolian Ecotype of the Silphion Plant.

In the present study, preliminary phytochemical investigations were performed on the fruit essential oil and antioxidant-rich methanolic extracts of the fruits and roots of Ferula drudeana, the putative Anatolian ecotype of the Silphion plant, to corroborate its medicinal plant potential and identify its unique characteristics amongst other Ferula species. The essential oil from the fruits of the endemic species Ferula drudeana collected from Aksaray was analyzed by GC and GC/MS. The main components of the oil were determined as shyobunone (44.2%) and 6-epishyobunone (12.6%). The essential oil of the fruits and various solvent extracts of the fruits and roots of F. drudeana were evaluated for their antibacterial and anticandidal activity using microbroth dilution methods. The essential oil of the fruits, methanol, and methylene chloride extracts of the fruits and roots showed weak to moderate inhibitory activity against all tested microorganisms with MIC values of 78-2000 µg/mL. However, the petroleum ether extract of the roots showed remarkable inhibitory activity against Candida krusei and Candida utilis with MIC values of 19.5 and 9.75 µg/mL, respectively. Furthermore, all the samples were tested for their antioxidant activities using DPPH• TLC spot testing, online HPLC-ABTS screening, and DPPH/ABTS radical scavenging activity assessment assays. Methanolic extracts of the fruits and roots showed strong antioxidant activity in both systems.

The effect of continuous positive airway pressure treatment on inflammatory parameters and periostin levels in patients with obstructive sleep apnea syndrome.

BACKGROUND: The purpose of the study was to examine the effects of continuous positive airway pressure (CPAP) treatment on inflammation parameters in patients with obstructive sleep apnea syndrome (OSAS). METHODS: Patients aged 18 to 65 years who underwent polysomnography (PSG) in the sleep clinic between January 1, 2019, and December 31, 2019, were included in the study. Patients with severe OSAS initiated treatment with CPAP. Patients and control subjects were assessed for levels of periostin, TNF-alpha, TGF-beta, and IL-6. Patients were re-evaluated 3 months later. Comparisons for the serum markers were made between controls and patients of different severity of OSAS. Comparisons of serum markers were also made between baseline and 3 month follow-up.  RESULTS: A total of 92 patients were enrolled in the study, including 25 controls (apnea-hypopnea index or AHI < 5/h), 39 patents with mild to moderate OSAS who did not receive CPAP, and 28 patients with severe OSAS receiving CPAP treatment. When all three groups were compared, levels of periostin, TNF-alpha, TGF-beta, and IL-6, as inflammatory markers, were higher in the OSAS group, though not at a statistically significant level. In patients with severe OSAS, there were statistically significant decreases in the TGF-beta 1, TNF-alpha, and IL-6 values between baseline values and the same measures taken after 3 months of CPAP treatment. Periostin values also decreased after treatment, but this decrease was not at a significant level. CONCLUSION: Inflammatory parameters of patients with OSAS were significantly higher compared with healthy participants. Regression of inflammation was detected after CPAP treatment.

Neopapillarine, an Unusual Coumarino-Alkaloid from the Root Extract of Neocryptodiscus papillaris with Cytotoxic Activity on Renal Cancer Cells.

Several simple and prenylated coumarin derivatives were isolated from the dichloromethane extract of the root of Neocryptodiscus papillaris based on moderate cytotoxic activity of the extract in COLO205, KM12 and MCF7 cancer cells. While the major prenylated furanocoumarin derivatives and osthol isolated from the dichloromethane extract were responsible for the activity in the colon and breast cancer cell lines, the 4'-acylated osthol derivatives including a novel coumarino-alkaloid; neopapillarine) demonstrated selective cytotoxic activity in A498 and UO31 renal cancer cell lines.

Anatolicin, a Highly Potent and Selective Cytotoxic Sesquiterpene Coumarin from the Root Extract of Heptaptera anatolica.

Seven known sesquiterpene coumarins and a new sesquiterpene coumarin, anatolicin (8), were isolated from the dichloromethane extract of the roots of Heptaptera anatolica. Structures of these compounds were elucidated based on their spectral properties. While some of these sesquiterpene coumarins showed modest cytotoxic activity against COLO205, KM12, A498, UO31, and TC32 cancer cell lines, selective cytotoxicity of anatolicin (8) and 14'-acetoxybadrakemin (7) were observed at nanomolar level against the UO31 kidney cancer cell line.

Coumarin, anthroquinone and stilbene derivatives with anticholinesterase activity.

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are the key enzymes in pathogenesis of Alzheimer's disease (AD), which is characterized by a deficit in central cholinergic transmission. In the current study, AChE and BChE inhibitory activities of seven coumarin derivatives [umbelliferone (1), 4-methylumbelliferone (2), 4-hydroxycoumarin (3), scopoletin (4), 8-methoxypsoralen (5), bergapten (6), and iso-bergapten (7)], a furanocoumarin mixture obtained from Heracleum crenatifolium Boiss. (Umbelliferae), as well as of two anthroquinone derivatives [rhein (8) and aloe-emodine (9)] and one stilbene, rhapontin (10), were tested by the spectrophotometric method of Ellman using an ELISA microplate-reader at 1 mg mL(-1). Among them, the furanocoumarin mixture [(68.8 +/- 0.76)%], bergapten [(62.4 +/- 0.74)%], aloe-emodine [(57.2 +/- 1.32)%], scopoletin [(53.1 +/- 0.83)%], and 4-methylumbelliferone [(62.3 +/- 1.03)%] showed over 50% inhibition against AchE, while umbelliferone [(54.3 +/- 0.23)%], 4-methylumbelliferone [(80.9 +/- 1.17)%], scopoletin [(73.5 +/- 1.01)%], 8-methoxypsoralen [(67.1 +/- 0.98)%], as well as the furanocoumarin mixture [(76.7 +/- 0.95)%] had a notable anti-BChE effect.

In vitro anticholinesterase activity of various alkaloids.

In the current study, a number of alkaloids including retamine, cytisine, and sparteine (quinolizidine-type), yohimbine and vincamine (indole-type), scopolamine and atropine (tropane-type), colchicine (tropolone-type), allantoin (imidazolidine-type), trigonelline (pyridine-type) as well as octopamine, synephrine, and capsaicin (exocyclic amine-type) were tested in vitro for their inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) at 1 mg/ml concentration by the Ellman method using an ELISA microplate reader. Among the alkaloids tested, only capsaicin exerted a remarkable inhibitory effect towards both AChE and BChE [(62.7 +/- 0.79)% and (75.3 +/- 0.98)%, respectively]. While the rest of the alkaloids did not show any significant inhibition against AChE, three of the alkaloids, namely retamine, sparteine, and yohimbine, exerted a noteworthy anti-BChE effect as compared to galanthamine, the reference drug.

Screening of various phenolic acids and flavonoid derivatives for their anticholinesterase potential.

Alzheimer's disease (AD), the most common form of dementia, is a neurodegenerative disease characterized by progressive cognitive deterioration together with declining activities of daily living and neuropsychiatric symptoms or behavioural changes. The oldest, on which most currently available drug therapies are based, is known as the "cholinergic hypothesis" and suggests that AD begins as a deficiency in the production of the neurotransmitter acetylcholine. Therefore, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors have gained a great popularity for the treatment of AD. In this study, we screened in vitro inhibitory activities of a number of phenolic acids (chlorogenic, caffeic, gallic, and quinic acids) as well as of various flavonoid derivatives (genistein, biochanin A, naringin, apigenin, quercetin, luteolin-7-O-rutinoside, kaempferol-3-O-galactoside, diosmin, silibinin, and silymarin) against AChE and BChE at 1 mg/ml concentration using a microplate-reader assay based on the Ellman method. Among them, only quercetin showed a substantial inhibition (76.2%) against AChE, while genistein (65.7%), luteolin-7-O-rutinoside (54.9%), and silibinin (51.4%) exerted a moderate inhibition on BChE.

Antitrypanosomal and antileishmanial activities of flavonoids and their analogues: in vitro, in vivo, structure-activity relationship, and quantitative structure-activity relationship studies.

Trypanosomiasis and leishmaniasis are important parasitic diseases affecting millions of people in Africa, Asia, and South America. In a previous study, we identified several flavonoid glycosides as antiprotozoal principles from a Turkish plant. Here we surveyed a large set of flavonoid aglycones and glycosides, as well as a panel of other related compounds of phenolic and phenylpropanoid nature, for their in vitro activities against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania donovani. The cytotoxicities of more than 100 compounds for mammalian L6 cells were also assessed and compared to their antiparasitic activities. Several compounds were investigated in vivo for their antileishmanial and antitrypanosomal efficacies in mouse models. Overall, the best in vitro trypanocidal activity for T. brucei rhodesiense was exerted by 7,8-dihydroxyflavone (50% inhibitory concentration [IC50], 68 ng/ml), followed by 3-hydroxyflavone, rhamnetin, and 7,8,3',4'-tetrahydroxyflavone (IC50s, 0.5 microg/ml) and catechol (IC50, 0.8 microg/ml). The activity against T. cruzi was moderate, and only chrysin dimethylether and 3-hydroxydaidzein had IC50s less than 5.0 microg/ml. The majority of the metabolites tested possessed remarkable leishmanicidal potential. Fisetin, 3-hydroxyflavone, luteolin, and quercetin were the most potent, giving IC50s of 0.6, 0.7, 0.8, and 1.0 microg/ml, respectively. 7,8-Dihydroxyflavone and quercetin appeared to ameliorate parasitic infections in mouse models. Generally, the test compounds lacked cytotoxicity in vitro and in vivo. By screening a large number of flavonoids and analogues, we were able to establish some general trends with respect to the structure-activity relationship, but it was not possible to draw clear and detailed quantitative structure-activity relationships for any of the bioactivities by two different approaches. However, our results can help in directing the rational design of 7,8-dihydroxyflavone and quercetin derivatives as potent and effective antiprotozoal agents.

Five-year evaluation of premarital screening program for hemoglobinopathies in the province of Mersin, Turkey.

The prevalences of hemoglobin S (HbS) and ß-thalassemia (ß-thal) are high in Mersin, Turkey. In this study, the results of a five-year premarital screening program in Mersin province are reported. A total of 79,000 persons including 31,498 couples were screened in this program. Hematological analyses and electrophoresis were done to identify carriers. The results were given confidentially and at-risk couples were counselled on reproductive options and prenatal diagnosis. The carrier rates of hemoglobins (Hb) (HbS, HbD, HbE) and of ß-thal were 1.21%, 0.17%, 0.04% and 2.04%, respectively. One hundred and thirty-four couples were at-risk, of whom 67.2% had health insurance. Twenty-seven couples did not become pregnant, six were divorced and 11 could not be reached. Of the 135 pregnancies, 80 had prenatal diagnosis. Five stillbirths occurred, and 18 homozygous babies were born to couples that did not seek prenatal diagnosis. Two families with prenatal diagnosis had affected babies: one was a late referral and the other due to religious reasons. For a successful screening program, emphasis must be on extensive and intensive informative programs for the public as a whole. Prenatal diagnosis should be offered free of charge as a basic public service. For a healthy population, knowledge and a shared responsibility between the public and the government are necessary.