Effects of Naphthoquinones from the Roots of Onosma Armeniacum Klokov on Wound Healing.

In Turkish folk medicine, the roots of Onosma armeniacum Klokov are used to heal wounds, burns, hemorrhoids, hoarseness, dyspnea, stomach ulcers, and abdominal aches. The objective was to evaluate the plant's ethnopharmacological applications using in vivo pharmacological experimental models. In vivo linear incision and circular excision the wound models were used to assess the wound healing activity along with histopathological investigation. The active component(s) were isolated and identified after being exposed to several chromatographic separation procedures on the primary extract. The n-hexane-dichloromethane mixture extract was subjected to chromatographic separation after the wound-healing activity was confirmed. Deoxyshikonin (1), ß,ß-dimethylacrylshikonin (2), α-methyl-n-butylshikonin (3), isovalerylshikonin (4), acetylshikonin (5), ß-hydroxyisovalerylshikonin (6), and 5,8-O-dimethylacetylshikonin (7) were identified as the structures of the isolated compounds. The efficacy of O. armeniacum to heal wounds was investigated in this study. Shikonin derivatives were identified as the primary active components of the roots by bioassay-guided fractionation and isolation procedures.

The Wound-Healing Potential of the Endemic Plant Helianthemum canum (L.) Baumg: Preclinical Studies Supported with Phytochemical Profiling.

The study's objective is to clarify the probable mechanisms underlying the wound-healing properties of Helianthemum canum L. (Cistaceae), a traditional anti-inflammatory and wound-healing medicine. LC/MS-MS was used to perform phytochemical analyses on a 70 % methanol extract of the plant's aerial parts. In vivo, linear incision and circular excision models were used to evaluate the wound healing activity. For anti-inflammatory effect, in vivo acetic acid capillary permeability assay and in vitro Interleukin 1, Interleukin 6, and Interferon É£ levels in LPS-induced FR skin fibroblast cell line were also evaluated. The extract significantly improved wound healing in experimental models, with tensile strength values of 27.8 % and a contraction value of 35.09 %. Histopathological examinations, hydroxyproline estimation, hyaluronidase, collagenase, and elastase enzyme inhibitory assays confirmed wound healing potential. Inflammatory cytokines were significantly inhibited in the LPS-induced FR cell line, with the highest effect seen on IL-6 (34.5±2.12 pg/mL). This study offered the first concrete proof that H. canum can be used to treat wounds by suggesting that the myricetin and quinic acid content identified by LCMS-MS analysis may be accountable for the effect of H. canum on wound contraction and hydroxyproline production.

Glyco-nanoparticles: New drug delivery systems in cancer therapy.

Cancer is known as one of the most common diseases that are associated with high mobility and mortality in the world. Despite several efforts, current cancer treatment modalities often are highly toxic and lack efficacy and specificity. However, the application of nanotechnology has led to the development of effective nanosized drug delivery systems which are highly selective for tumors and allow a slow release of active anticancer agents. Different Nanoparticles (NPs) such as the silicon-based nano-materials, polymers, liposomes and metal NPs have been designed to deliver anti-cancer drugs to tumor sites. Among different drug delivery systems, carbohydrate-functionalized nanomaterials, specially based on their multi-valent binding capacities and desirable bio-compatibility, have attracted considerable attention as an excellent candidate for controlled release of therapeutic agents. In addition, these carbohydrate functionalized nano-carriers are more compatible with construction of the intracellular delivery platforms like the carbohydrate-modified metal NPs, quantum dots, and magnetic nano-materials. In this review, we discuss recent research in the field of multifunctional glycol-nanoparticles (GNPs) intended for cancer drug delivery applications.

Bioactive Saponins of Primula vulgaris Huds. Promote Wound Healing through Inhibition of Collagenase and Elastase Enzymes: in Vivo, in Vitro and in Silico Evaluations.

Primula vulgaris Huds. leaves and roots were used to treat skin damage and inflammation in Anatolian Folk Medicine. This study aimed to assess the ethnopharmacological use of the plant using in vivo, in vitro, and in silico test models. Linear incision and circular excision wound models were used to determine the in vivo wound-healing potential of the plant extracts and fractions. In vitro assays including hyaluronidase, collagenase, and elastase inhibitory activities were carried out for the active compounds to discover their activity pathways. Structure-based molecular modeling was performed to understand inhibitory mechanisms regarding collagenase and elastase at the molecular level. The butanol fraction of the roots of P. vulgaris showed the highest wound-healing activity. Through activity-guided fractionation and isolation techniques, primulasaponin I (1) and primulasaponin I methyl ester (2) were stated as the major active compounds. These compounds exerted their activities through the inhibition of collagenase and elastase enzymes. Primulasaponin I methyl ester isolated from butanol fraction was found to be the strongest agent, especially with the values of 29.65 % on collagenase and 38.92 % on elastase inhibitory activity assays, as well as molecular docking studies. The present study supports scientific data for the traditional use of P. vulgaris and the wound healing properties of the plant can be referred to secondary metabolites as especially saponins found in the roots.

Oxidative Stress and Marine Carotenoids: Application by Using Nanoformulations.

Carotenoids are natural fat-soluble pigments synthesized by plants, algae, fungi and microorganisms. They are responsible for the coloration of different photosynthetic organisms. Although they play a role in photosynthesis, they are also present in non-photosynthetic plant tissues, fungi, and bacteria. These metabolites have mainly been used in food, cosmetics, and the pharmaceutical industry. In addition to their utilization as pigmentation, they have significant therapeutically applications, such as improving immune system and preventing neurodegenerative diseases. Primarily, they have attracted attention due to their antioxidant activity. Several statistical investigations indicated an association between the use of carotenoids in diets and a decreased incidence of cancer types, suggesting the antioxidant properties of these compounds as an important factor in the scope of the studies against oxidative stress. Unusual marine environments are associated with a great chemical diversity, resulting in novel bioactive molecules. Thus, marine organisms may represent an important source of novel biologically active substances for the development of therapeutics. Marine carotenoids (astaxanthin, fucoxanthin, ß-carotene, lutein but also the rare siphonaxanthin, sioxanthin, and myxol) have recently shown antioxidant properties in reducing oxidative stress markers. Numerous of bioactive compounds such as marine carotenoids have low stability, are poorly absorbed, and own very limited bioavailability. The new technique is nanoencapsulation, which can be used to preserve marine carotenoids and their original properties during processing, storage, improve their physiochemical properties and increase their health-promoting effects. This review aims to describe the role of marine carotenoids, their potential applications and different types of advanced nanoformulations preventing and treating oxidative stress related disorders.

Isolation and identification of triterpenes from Anthemis austriaca Jacq. through bioactivity-guided fractionation on polycystic ovary syndrome rat model.

PURPOSE: This study aimed to assess the activity of A. austriaca flowers in treating polycystic ovary syndrome (PCOS) in rats. METHODS: A letrozole-induced PCOS rat model was used to evaluate the activity potential of A. austriaca flowers. For this purpose, extracts of different polarity were prepared from A. austriaca flowers using n-hexane, ethyl acetate, and methanol. Serum luteinizing hormone, follicle-stimulating hormone, progesterone, testosterone, estradiol, serum leptin, lipid, and glucose levels were tested. Moreover, the antioxidant activity was evaluated by calculating superoxide dismutase, malondialdehyde, catalase, and glutathione peroxidase levels. Following the biological activity studies, phytochemical studies were conducted on the active extract to detect the compound(s) responsible for the activity. RESULTS: The treatment with n-hexane extract contributed to regulating serum gonadotropin and steroid hormone levels. The plasma level of high-density lipoprotein cholesterol was significantly higher than that of the control group, while the levels of low-density lipoprotein cholesterol, leptin, and glucose were significantly lower than those of the control group. Also, the n-hexane extract showed significant antioxidant activity in the PCOS rat model. Since the n-hexane extract was found to be active, isolation studies were performed on this extract and three main fractions were obtained from the n-hexane extract. Those fractions also were tested on letrozole-induced PCOS rat model. As a result, three triterpenoids, ß-amyrin palmitate, taraxasterol acetate, and taraxasterol were isolated and identified from Fr. B which is the most active fraction. CONCLUSION: n-Hexane extract and Fr. B obtained from this extract showed statistically significant activity in the letrozole-induced PCOS rat model and three triterpene-type compounds were isolated from Fr. B.

Anticancer Potential of Furanocoumarins: Mechanistic and Therapeutic Aspects.

Cancer is one of the most extreme medical conditions in both developing and developed countries around the world, causing millions of deaths each year. Chemotherapy and/or radiotherapy are key for treatment approaches, but both have numerous adverse health effects. Furthermore, the resistance of cancerous cells to anticancer medication leads to treatment failure. The rising burden of cancer overall requires novel efficacious treatment modalities. Natural medications offer feasible alternative options against malignancy in contrast to western medication. Furanocoumarins' defensive and restorative impacts have been observed in leukemia, glioma, breast, lung, renal, liver, colon, cervical, ovarian, and prostate malignancies. Experimental findings have shown that furanocoumarins activate multiple signaling pathways, leading to apoptosis, autophagy, antioxidant, antimetastatic, and cell cycle arrest in malignant cells. Additionally, furanocoumarins have been shown to have chemo preventive and chemotherapeutic synergistic potential when used in combination with other anticancer drugs. Here, we address different pathways which are activated by furanocoumarins and their therapeutic efficacy in various tumors. Ideally, this review will trigger interest in furanocoumarins and their potential efficacy and safety as a cancer lessening agents.

Combretastatins: An Overview of Structure, Probable Mechanisms of Action and Potential Applications.

Combretastatins are a class of closely related stilbenes (combretastatins A), dihydrostilbenes (combretastatins B), phenanthrenes (combretastatins C) and macrocyclic lactones (combretastatins D) found in the bark of Combretum caffrum (Eckl. & Zeyh.) Kuntze, commonly known as the South African bush willow. Some of the compounds in this series have been shown to be among the most potent antitubulin agents known. Due to their structural simplicity many analogs have also been synthesized. Combretastatin A4 phosphate is the most frequently tested compounds in preclinical and clinical trials. It is a water-soluble prodrug that the body can rapidly metabolize to combretastatin A4, which exhibits anti-tumor properties. In addition, in vitro and in vivo studies on combretastatins have determined that these compounds also have antioxidant, anti-inflammatory and antimicrobial effects. Nano-based formulations of natural or synthetic active agents such as combretastatin A4 phosphate exhibit several clear advantages, including improved low water solubility, prolonged circulation, drug targeting properties, enhanced efficiency, as well as fewer side effects. In this review, a synopsis of the recent literature exploring the combretastatins, their potential effects and nanoformulations as lead compounds in clinical applications is provided.

Sedative Effects of Latexes Obtained from Some Lactuca L. Species Growing in Turkey.

Lactuca L. species belong to the Asteraceae family and these plants are traditionally used for therapeutic purposes around the world. The dried milky latex of L. serriola is known as "lettuce oil" and is used as a sedative in Turkey. This study aimed to evaluate the sedative effects and analyze the chemical compositions of latexes obtained from some Lactuca species growing in Turkey. The sedative effects were evaluated through various behavioral tests on mice. For this purpose, latexes were obtained from L. glareosa Boiss., L. viminea (L.) J. Presl and C. P, L. mulgedioides (Vis and Pancic) Boiss. and Kotschy ex. Boiss., L. saligna L., and L. serriola L. The latex from L. saligna showed the highest sedative effects, whilst L. serriola and L. viminea latexes also displayed significant sedative effects compared to the control group at a dose of 100 mg/kg. However, the latexes from L. glareosa and L. mulqedioides did not exhibit any sedative effects on mice. Characteristic sesquiterpene lactones (lactucin, lactucopicrin, 11,13ß-dihydrolactucin, and 11,13ß-dihydrolactucopicrin) were determined qualitatively and quantitatively by high-performance liquid chromatography (HPLC). Lactucin was identified as the main component.

Inhibitory activity of Podospermum canum and its active components on collagenase, elastase and hyaluronidase enzymes.

Present study is aimed to investigate in vitro inhibitory effects of the extract prepared from the aerial parts of Podospermum canum (syn: Scorzonera cana var. jacquiniana) (Asteraceae) on hyaluronidase, collagenase, and elastase enzymes using a bioassay-guided fractionation. Inhibitory effects of the extract, sub-extracts, fractions obtained by column chromatography, and isolated compounds on collagenase, elastase, and hyaluronidase were performed by using in vitro enzyme inhibitory assays based on spectrophotometric evaluation. The methanolic extract obtained from P. canum exhibited strong inhibitory activities on elastase and collagenase while the insignificant activity was observed on hyaluronidase. Through bioactivity-guided fractionation, the ethyl acetate and remaining water sub-extracts obtained from the methanolic extract displayed significant inhibitory activities on collagenase and elastase, while petroleum ether and chloroform extracts did not show any inhibitory activity. Eleven known compounds: arbutin, 6́-O-caffeoylarbutin, cichoriin, 3,5-dicaffeoylquinic acid methyl ester, apigenin 7-O-ß-glucoside, luteolin 7-O-ß-glucoside, apigenin 7-O-ß-rutinoside, isoorientin, orientin, vitexin, procatechuic acid, and new compound 4-hydroxy-benzoic acid 4-(6-O-α-rhamnopyranosyl-ß-glucopyranosyl) benzyl ester have been obtained from ethyl acetate sub-extract. Results of the present study have revealed that apigenin 7-O-ß-glucoside, luteolin 7-O-ß-glucoside, apigenin 7-O-ß-rutinoside, and isoorientin showed potent enzyme inhibitory activities. However, methanolic extract of P. canum displayed a greater inhibitory activity than fractions and isolated compounds both on collagenase and elastase.

Effective eradication of pinworms (Syphacia obvelata and Aspiculuris tetraptera) with Polygonum cognatum Meissn.

Polygonum cognatum Meissn. (Polygonaceae) is a wild edible plant known locally as "solucanotu, madimak" in Turkey and it has been used for various purposes, such as diuretic and antidiabetic, as well to treat oxyuris and worms internally in humans. The present study was carried out to investigate the anthelmintic activity of various extracts were obtained from the aerial parts of P. cognatum in order to justify its traditional usage in Turkish folk medicine. n-Hexane, ethyl acetate and methanol extracts were prepared from the aerial parts of the plant, successively. The anthelmintic potentials of these extracts were evaluated on mice naturally infected with Syphacia obvelata and Aspiculuris tetraptera. Cellophane perianal tape test and fecal flotation test were used for the activity screening. The results were compared with control and reference groups. In addition to all these experiments, the total amount of phenolic compounds and tannin contents thought to be responsible for the activity were evaluated for all extracts. According to the results, it has been found that the methanolic extract reduced the number of S. obvelata (66.8%) and A. tetraptera (73.4%) eggs. Moreover, the methanolic extract include higher amount of total phenolic compound (48.75 ±â€¯0.82 mg of GA/g of extract) and tannin (30.04 ±â€¯0.22 mg TA/g of extract) than n-Hexane (17.21 ±â€¯0.75 mg of GA/g of extract; 6.82 ±â€¯0.41 mg TA/g of extract) and ethyl acetate (25.06 ±â€¯0.94 mg of GA/g of extract; 10.29 ±â€¯0.34 mg TA/g of extract); therefore the anthelmintic activity could be related to these constituents. The present study explored the anthelmintic potential of P. cognatum. Further studies should be conducted into the mechanism of these compounds' against helminths. This study can be an important step in the discovery of new anthelmintic agents.

Assessment of Antidepressant Effect of the Aerial Parts of Micromeria myrtifolia Boiss. & Hohen on Mice.

The currently available antidepressant agents necessitate the development of newer alternatives because of their serious adverse effects and costs. Traditional medicinal knowledge is likely the key that opens the door to discover new medicines. In Turkish folk medicine, the infusion prepared from aerial parts of Micromeria myrtifolia Boiss. & Hohen is used as pleasure and medicinal tea for its relaxing action. The present research was conceived to confirm the antidepressant's potential of this traditional medicinal plant. In this process, first of all, the collected and shade-dried aerial parts of M. myrtifolia were powdered and then, extracted using solvents with different polarity as follows; n-hexane, ethyl acetate (EtOAc), and methanol (MeOH). The antidepressant activity of the extracts was evaluated by using several in vivo and in vitro experimental models of depression. When the data obtained from the control and experimental groups were compared, it was determined that the MeOH extract was the most active. The active components of this extract were isolated and identified utilizing various chromatographic separation techniques. The MeOH extract was applied to reversed phase (RP-18) column chromatography to obtain five main fractions and they were tested on antidepressant activity models. The isolated compounds from the obtained fractions were elucidated as rosmarinic acid (1), myricetin (2), apigenin (3), and naringenin (4) which were assumed to be responsible for the antidepressant activity of the aerial parts. According to the results, rosmarinic acid, myricetin, apigenin, and naringenin showed statistically significant activity on forced swimming test and tetrabenazine-induced ptosis models, whereas only rosmarinic acid showed statistically significant activity on the tail suspension test. Apigenin displayed the highest inhibitory activity on MAO A and B enzymes. Studies in the future should be performed to investigate the antidepressant activity mechanism of these natural compounds. The current research could be an important step in the development of the new agents that can be used in the treatment of depression.

Promising activity of Anthemis austriaca Jacq. on the endometriosis rat model and isolation of its active constituents.

Anthemis austriaca Jacq. flowers are traditionally used to alleviate abdominal pain, hemorrhoids, ovary diseases and pneumonia. This study aimed to investigate the effects of A. austriaca flowers, which are frequently used in gynecological disorders, on the rat endometriosis model. The rat endometriosis model was used to evaluate the potential activity of the plant in endometriosis. The dried plant material was extracted with n-hexane, ethyl acetate (EtOAc), and methanol (MeOH), successively. The obtained extracts from A. austriaca flowers were applied to the rats. The adhesion scores, endometrial foci areas, and cytokine levels of the peritoneal fluids were measured on surgical induction of endometriosis in rats. The adhesion scores, endometriotic volume, and cytokine levels of the peritoneal fluids were reduced in the EtOAc, MeOH, and buserelin acetate-treated (reference) groups. The MeOH extract reduced the adhesion scores and endometrial foci areas from 3.1 to 1.1 (p < 0.01) and from 86.4 to 40.5 (p < 0.01), respectively and also the MeOH extract reduced tumor necrosis factor (TNF)-α, vascular endothelial growth factor (VEGF), and interleukin (IL)-6 levels of the peritoneal fluids from 13.7 to 3.8 (p < 0.01), from 28.4 to 16.3 (p < 0.05) and from 50.2 to 24.3 (p < 0.01), respectively. Therefore, isolation studies were conducted on the EtOAc and MeOH extracts. After the MeOH extract was fractionated using RP-18 column, the obtained subfractions were evaluated again on the endometriosis rat model. Subfractions A and C of the MeOH extract displayed statistically significant activity on the endometriosis rat model. Phytochemical investigation resulted in the isolation of 4-ß-D-glucopyranosyloxy-6-methyl-2H-pyran-2-one (1) from Fr. A and quercetin (2), apigenin-7-O-(3″-O-acetyl)-ß-D-glucopyranoside (3), apigenin-7-O-(6″-O-acetyl)-ß-D-glucopyranoside (4), apigenin-7-O-ß-D-glucopyranoside (5), quercetin-7-O-ß-D-glucopyranoside (6) from Fr. C. Moreover, ß-sitosterol-3-O-ß-D-glucopyranoside (7) was isolated from the EtOAc extract. As a conclusion, the MeOH extract obtained from A. austriaca flowers contributed to the regression of endometriosis. In addition, flavonoids and sterols of the plant were detected as the possible compounds responsible for the activity.

The evaluation of sterile solutions of Ilwensisaponin A and C from Verbascum pterocalycinum var. mutense Hub.-Mor. on antiviral, antinociceptive and anti-inflammatory activities.

Antiviral, antinociceptive and anti-inflammatory activities of the 1% sterile solutions of Ilwensisaponin A and C isolated from the methanolic extract of the flowers of Verbascum pterocalycinum var. mutense Hub.-Mor. were investigated. Antiviral activities of sterile solutions were evaluated against Bovine Herpes Virus Type-1 (BHV-1) (Cooper strain). Both solutions showed cytotoxic effects. However, none of the sterile solutions showed antiviral activity with CPE values. Anti-inflammatory and antinociceptive response were obtained at doses of 100 mg/kg. The results of the evaluation of the anti-inflammatory activities induced by carrageenan showed that these sterile solutions possess active constituents and diminish cyclooxygenase activitiy. In addition, antinociceptive activities using p-benzoquinone-induced writhing model in mice of tested solutions were found to show notable activity in statistical analysis without inducing any apparent acute toxicity as well as gastric damage. To the best of our knowledge, this study is the first investigation of antiviral, anti-inflammatory and antinociceptive activities of sterile solutions of Ilwensisaponin A and C isolated from Verbascum pterocalycinum var. mutense Hub.-Mor. growing in Turkey.

Evaluation of the chemopreventive effects of Ankaferd Bloodstopper in 7,12-dimethylbenz[a]anthracene-induced oral epithelial dysplasia.

OBJECTIVES: Ankaferd BloodStopper® (ABS) is an herbal extract which has been used historically as a hemostatic agent in traditional Turkish medicine. ABS comprises of standardized mixture of herbs Thymus vulgaris, Glycyrrhiza glabra, Vitis vinifera, Alpinia officinarum, and Urtica dioica. In addition to its hemostatic effects, the herb ABS contains some other biological effects including antioxidant and antitumoral properties. The aim of this study is to investigate the chemopreventive effects of ABS in 7,12-dimethylbenz[a]anthracene (DMBA)-induced oral epithelial dysplasia. MATERIALS AND METHODS: A total of 40 Sprague Dawley rats were randomly divided into four groups. Group 1 animals received DMBA alone, and group 2 animals received both DMBA and Ankaferd. Group 3 animals received ABS alone while group 4 animals served as control group and received only liquid paraffine. All animals were sacrificed, and tissue samples were analyzed histologically at the end of the experimental period (14 weeks). RESULTS: Histological studies have shown that the buccal pouches of animals treated with DMBA alone revealed severe dysplasia while only mild or no dysplasia were noticed in DMBA + ABS group. Ankaferd were administered to animals and control group showed no dysplasia or other oral lesions. CONCLUSION: The results suggest that Ankaferd Bloodstopper® has chemopreventive effect against DMBA-induced oral epithelial dysplasia. CLINICAL RELEVANCE: Ankaferd Bloodstopper® could be used as a supportive treatment option of cancer in oral and maxillofacial surgery since it possesses chemopreventive effect.

Anticholinesterase, antioxidant, analgesic and anti-inflammatory activity assessment of Xeranthemum annuum L. and isolation of two cyanogenic compounds.

CONTEXT: Xeranthemum annuum L. (Asteraceae) (XA) is an ornamental and medicinal species with limited bioactivity and phytochemical data. OBJECTIVE: Identification of anticholinesterase, antioxidant, anti-inflammatory and analgesic effects of the flower and root-stem (R-S) extracts of XA. MATERIALS AND METHODS: Anticholinesterase (at 100 µg mL-1) and antioxidant (at 1000 µg mL-1) effects of various extracts were evaluated via microtiter assays, while anti-inflammatory and analgesic effects of the R-S extracts were tested using carrageenan-induced hind paw oedema (100 and 200 mg kg-1) and p-benzoquinone (PBQ) writhing models (200 mg kg-1) in male Swiss albino mice. The R-S ethanol extract of XA was subjected to isolation studies using conventional chromatographic methods. RESULTS: Most of the extracts showed inhibition over 85% against butyrylcholinesterase and no inhibition towards acetylcholinesterase. The flower chloroform and the R-S ethyl acetate extracts were most effective (97.85 ± 0.94% and 96.89 ± 1.09%, respectively). The R-S ethanol extract displayed a remarkable scavenging activity against DPPH (77.33 ± 1.99%) and in FRAP assay, while the hexane extract of the R-S parts possessed the highest metal-chelating capacity (72.79 ± 0.33%). The chloroform extract of the R-S caused a significant analgesic effect (24.4%) in PBQ writhing model. No anti-inflammatory effect was observed. Isolation of zierin and zierin xyloside, which were inactive in anticholinesterase assays, was achieved from the R-S ethanol extract. DISCUSSION AND CONCLUSION: This is the first report of anticholinesterase, antioxidant, analgesic and anti-inflammatory activities and isolation of zierin and zierin xyloside from XA. Therefore, XA seems to contain antioxidant and BChE-inhibiting compounds.

Phytochemical analyses and effects of Alchemilla mollis (Buser) Rothm. and Alchemilla persica Rothm. in rat endometriosis model.

PURPOSE: The aim of the present study is to evaluate the treatment potential of Alchemilla mollis (Buser) Rothm. and Alchemilla persica Rothm. in the experimentally induced endometriosis model in rats. METHODS: Endometriosis was surgically induced in rats by autotransplanting endometrial tissue to abdominal wall. Thirty-six rats were randomly divided into six groups. The groups were orally treated with the methanol:water (80:20) extracts of aerial parts and roots of A. mollis and A. persica. Buserelin acetate (20 mg) was used as the reference drug. The phytochemical contents of the most active extracts were determined by high performance liquid chromatography. RESULTS: The cystic formation was determined to be significantly decreased with the aerial part extract of A. mollis. A reduction in the endometrioma was also determined for the aerial part extract of A. persica group. However, significant reduction on the levels of cytokine were recorded for the A. mollis aerial part extract group. Therefore, the phytochemical contents of the aerial part extracts of A. mollis. and A. persica were analyzed. CONCLUSION: The results of the present study revealed that the aerial part extracts of A. mollis and A. persica could be beneficial in the treatment of endometriosis.

Biochemical and biomechanical assessment of effects of L-carnitine on oral mucosal wounds.

OBJECTIVES: The present study aimed to investigate the oral mucosal wound healing potential of L-carnitine in a rat model. MATERIALS AND METHODS: Twenty-four Wistar-albino rats were divided into 4 groups: control group (group I), L-carnitine groups (100 and 200 mg/kg/day, intraperitoneally) (groups II and III), and vitamin E group (100 mg/kg/day, intraperitoneally) (group IV). A 1.5-cm linear incision was created on the buccal mucosa of each rat and was left to heal by secondary intention. On the tenth day, rats were anesthetized and sacrificed. The tensile strength of wound was measured with a tensiometer. Hydroxyproline (HYP) and malondialdehyde (MDA) levels in wound were assayed by spectrophotometry. Results were statistically analyzed using a one-way ANOVA analysis (p ≤ 0.001). RESULTS: In the analysis of tissue samples, there was a statistically significant decrease in MDA levels in group II (p < 0.01) and group IV (p < 0.001). Wound tension strength that was seen in groups II (57.88 %) and IV (48.71 %) was better than group III (33.39 %). Hydroxyproline levels in group II (46.98 ± 1.37) was higher than groups III (29.40 ± 1.64) and IV (38.83 ± 1.41). CONCLUSION: Although there was a tendency toward faster healing in the groups receiving L-carnitine, it may have a dose-related positive effect for wound healing. CLINICAL RELEVANCE: With the advantages of having positive effects on wound healing, being a natural substance in the body, being easy to procure, and having a practical usage, L-carnitine may be clinically feasible for human oral mucosal wounds.

Evaluation of the anti-obesity effect of Sambucus nigra L. (elderberry) and Vitex agnus-castus L. (chasteberry) extracts in high-fat diet-induced obese rats.

The aim of this study was to investigate the effects of S. nigra L. and V. agnus-castus L. plants on obesity in vivo. Extracts were prepared from S. nigra leaves, flowers, fruits and from V. agnus-castus leaves, flowers, and fruits using 100% water and 70% ethanol. The total phenol and flavonoid contents of the extracts were quantified spectrophotometrically. The findings revealed that the ethanol extracts of V. agnus-castus and S. nigra flowers had the highest phenolic content, while the ethanol extracts of S. nigra flowers and V. agnus-castus leaves had the highest flavonoid content. Qualification and quantification of the phenolic contents of the extracts were carried out using liquid chromatography-high resolution mass spectrometry (LC-HRMS) analyses. The study investigated the effects of various extracts on plasma levels of leptin, insulin, triiodothyronine (T3), thyroxine (T4), triglycerides, high-density lipoprotein (HDL), low-density lipoprotein (LDL) and lipase enzyme in obesity-induced rats. The results showed that the ethanol extract of V. agnus-castus flowers, as well as the ethanol and water extracts of V. agnus-castus leaves, resulted in body weight reduction in rats with obesity. Additionally, these extracts were found to decrease serum levels of LDL, triglycerides, leptin, lipase, TNF-α, and IL-1ß while increasing levels of HDL and adiponectin. The LC-HRMS results demonstrated that all three extracts exhibited relatively high concentrations of luteolin-7-glycoside and kaempferol, in comparison to the other extracts. The ethanol extract of V. agnus-castus flowers contained 653.04 mg/100 g of luteolin-7-glycoside and 62.63 mg/100 g of kaempferol. The ethanol extract of V. agnus-castus leaves contained 1,720.26 mg/100 g of luteolin-7-glycoside and 95.85 mg/100 g of kaempferol. The water extract of V. agnus-castus leaves contained 690.49 mg/100 g of luteolin-7-glycoside and 194.41 mg/100 g of kaempferol. The study suggests that the ethanol extract of V. agnus-castus flowers and leaves, as well as the water extract of V. agnus-castus leaves, may have potential benefits in treating obesity. However, further controlled clinical studies are necessary to evaluate the clinical efficacy of V. agnus-castus in treating obesity and investigate the in vivo anti-obesogenic effects of luteolin-7-glycoside and kaempferol separately, both in their pure form and in combination.

Hybrid Caffeic Acid-Based DHFR Inhibitors as Novel Antimicrobial and Anticancer Agents.

A novel series of 1,2,4-triazole analogues of caffeic acid was designed, synthesized, characterized, and assessed for their capacity to inhibit DHFR, as well as their anticancer and antimicrobial properties. A molecular docking analysis was conducted on DHFR, utilizing PDB IDs 1U72 and 2W9S, aiming to design anticancer and antimicrobial drugs, respectively. Among all the synthesized derivatives, compound CTh7 demonstrated the highest potency as a DHFR inhibitor, with an IC50 value of 0.15 µM. Additionally, it exhibited significant cytotoxic properties, with an IC50 value of 8.53 µM. The molecular docking analysis of the CTh7 compound revealed that it forms strong interactions with key residues of homo sapiens DHFR such as Glu30, Phe34, Tyr121, Ile16, Val115, and Phe31 within the target protein binding site and displayed excellent docking scores and binding energy (-9.9; -70.38 kcal/mol). Additionally, synthesized compounds were screened for antimicrobial properties, revealing significant antimicrobial potential against bacterial strains and moderate effects against fungal strains. Specifically, compound CTh3 exhibited notable antibacterial efficacy against Staphylococcus aureus (MIC = 5 µM). Similarly, compound CTh4 demonstrated significant antibacterial activity against both Escherichia coli and Pseudomonas aeruginosa, with MIC values of 5 µM for each. A docking analysis of the most active antimicrobial compound CTh3 revealed that it forms hydrogen bonds with Thr121 and Asn18, a π-cation bond with Phe92, and a salt bridge with the polar residue Asp27.