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Authors = Büşra Karpuz

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13 pages, 932 KiB  
Article
The Anthelmintic Activity of Nepeta racemosa Lam. Against Gastrointestinal Nematodes of Sheep: Rosmarinic Acid Quantification and In Silico Tubulin-Binding Studies
by Büşra Karpuz Ağören, Mahmut Sinan Erez, Esma Kozan, Aydın Dağyaran, Mevlüt Akdağ, Eduardo Sobarzo-Sánchez and Esra Küpeli Akkol
Pathogens 2025, 14(1), 77; https://doi.org/10.3390/pathogens14010077 - 15 Jan 2025
Viewed by 1609
Abstract
Gastrointestinal nematodes (GINs) inflict significant economic losses on sheep and goat farming globally due to reduced productivity and the development of anthelmintic resistance. Sustainable control strategies are urgently needed including the exploration of medicinal plants as safer alternatives to chemical anthelmintics. This genus [...] Read more.
Gastrointestinal nematodes (GINs) inflict significant economic losses on sheep and goat farming globally due to reduced productivity and the development of anthelmintic resistance. Sustainable control strategies are urgently needed including the exploration of medicinal plants as safer alternatives to chemical anthelmintics. This genus of plants is used for anti-inflammatory, antioxidant, and antimicrobial activities. In this study, we aimed to evaluate the anthelmintic activities of Nepeta racemosa Lam. MeOH extract, n-hexane, dichloromethane (DCM), ethyl acetate (EtOAc), n-buthanol (n-BuOH) and aqueous (H2O) subextracts, and quantify rosmarinic acid in the active extract by the HPLC method, and perform in silico molecular docking studies of rosmarinic acid to examine its binding interactions with tubulin. The anthelmintic activity of the plant extracts on gastrointestinal nematode eggs and larvae (L3) of the sheep was assessed using in vitro test methods such as the egg hatch assay and larval motility assay, conducted over a 24 h period (1, 2, 3, 4, 6, 8, 24). All extracts exhibited 100% effectiveness in the egg hatch inhibition assay, regardless of concentration (50–1.5625 mg/mL). The EtOAc subextract shows the highest effectiveness at 79.66%, followed by the MeOH extract at 74.00%, water at 64.00%, n-hexane at 67.00%, and DCM at 61.00%, and the lowest effectiveness is observed with n-BuOH at 51.66% in the larval motility assay. The major compound of EtOAc extract, the most active extract of N. racemosa, was determined as rosmarinic acid and its amount in the extract was determined as 14.50 mg/100 mg dry extract. The amount of rosmarinic acid in the MeOH extract was found to be 0.21 mg/100 mg dry extract. n-Hexane, DCM, n-BuOH, and H2O extracts’ rosmarinic acid content was lower than the LOQ value. As tubulin plays an important role in the mechanism of anthelmintics, the major compound of the most active extract (NR-EtOAc) rosmarinic acid was docked onto the colchicine-binding site of the tubulin (5OV7) protein. Rosmarinic acid showed a similar activity spectrum to the anthelmintic drug albendazole. The discovery of low-cost and low-toxicity anthelmintic compounds is very important. Full article
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16 pages, 2087 KiB  
Article
The Phytochemical Profile and Biological Activity of Malva neglecta Wallr. in Surgically Induced Endometriosis Model in Rats
by Esra Küpeli Akkol, Büşra Karpuz, Gizem Türkcanoğlu, Fatma Gül Coşgunçelebi, Hakkı Taştan, Michael Aschner, Anurag Khatkar and Eduardo Sobarzo-Sánchez
Molecules 2022, 27(22), 7869; https://doi.org/10.3390/molecules27227869 - 15 Nov 2022
Cited by 5 | Viewed by 2918
Abstract
Leaves and aerial parts of Malva neglecta Wallr. have been traditionally used in Anatolia for the treatment of pain, inflammation, hemorrhoids, renal stones, constipation, and infertility. This study investigated the effects of M. neglecta leaves in a rat endometriosis model. The dried plant [...] Read more.
Leaves and aerial parts of Malva neglecta Wallr. have been traditionally used in Anatolia for the treatment of pain, inflammation, hemorrhoids, renal stones, constipation, and infertility. This study investigated the effects of M. neglecta leaves in a rat endometriosis model. The dried plant material was extracted with n-hexane, ethyl acetate, and methanol, successively. Experimental endometriosis was surgically induced in six-week-old female, non-pregnant, Wistar albino rats by autotransplant of endometrial tissue to the abdominal wall. After twenty-eight days, rats were evaluated for a second laparotomy. Endometrial foci areas were assessed, and intraabdominal adhesions were scored. Rats were divided into five groups as control, n-hexane, ethyl acetate, methanol, and aqueous extracts, as well as reference. At the end of the treatment, all rats were sacrificed and endometriotic foci areas and intraabdominal adhesions were re-evaluated and compared with the previous findings. Moreover, peritoneal fluid was collected to detect tumor necrosis factor- α (TNF-α), vascular endothelial growth factor (VEGF), and interleukin-6 (IL-6) levels, and cDNA synthesis, and a quantitative real-time polymerase chain reaction (PCR) test was done. The phytochemical content of the most active extract was determined using High-Performance Liquid Chromatography (HPLC). Both endometrial volume and adhesion score decreased significantly in the group treated with methanol extract. In addition, significant decreases were observed in TNF-α, VEGF, and IL-6 levels in animals administered methanol extract. HPLC results showed that the activity caused by the methanol extract of M. neglecta was due to the polyphenols. Taken together, these novel findings indicate that M. neglecta may be a promising alternative for the treatment of endometriosis. Full article
(This article belongs to the Special Issue Natural Products: Biological and Pharmacological Activity)
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25 pages, 2599 KiB  
Review
Coumarins and Coumarin-Related Compounds in Pharmacotherapy of Cancer
by Esra Küpeli Akkol, Yasin Genç, Büşra Karpuz, Eduardo Sobarzo-Sánchez and Raffaele Capasso
Cancers 2020, 12(7), 1959; https://doi.org/10.3390/cancers12071959 - 19 Jul 2020
Cited by 385 | Viewed by 17639
Abstract
Cancer is one of the most common causes of disease-related deaths worldwide. Despite the discovery of many chemotherapeutic drugs that inhibit uncontrolled cell division processes for the treatment of various cancers, serious side effects of these drugs are a crucial disadvantage. In addition, [...] Read more.
Cancer is one of the most common causes of disease-related deaths worldwide. Despite the discovery of many chemotherapeutic drugs that inhibit uncontrolled cell division processes for the treatment of various cancers, serious side effects of these drugs are a crucial disadvantage. In addition, multi-drug resistance is another important problem in anticancer treatment. Due to problems such as cytotoxicity and drug resistance, many investigations are being conducted to discover and develop effective anticancer drugs. In recent years, researchers have focused on the anticancer activity coumarins, due to their high biological activity and low toxicity. Coumarins are commonly used in the treatment of prostate cancer, renal cell carcinoma and leukemia, and they also have the ability to counteract the side effects caused by radiotherapy. Both natural and synthetic coumarin derivatives draw attention due to their photochemotherapy and therapeutic applications in cancer. In this review, a compilation of various research reports on coumarins with anticancer activity and investigation and a review of structure-activity relationship studies on coumarin core are presented. Determination of important structural features around the coumarin core may help researchers to design and develop new analogues with a strong anticancer effect and reduce the potential side effects of existing therapeutics. Full article
(This article belongs to the Special Issue Medicinal Plants and Their Active Ingredients in Cancer)
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13 pages, 653 KiB  
Article
Sedative and Anxiolytic Activities of Opuntia ficus indica (L.) Mill.: An Experimental Assessment in Mice
by Esra Küpeli Akkol, Mert Ilhan, Büşra Karpuz, Yasin Genç and Eduardo Sobarzo-Sánchez
Molecules 2020, 25(8), 1844; https://doi.org/10.3390/molecules25081844 - 16 Apr 2020
Cited by 34 | Viewed by 5410
Abstract
Ethnobotanical field surveys revealed the use of fruits of Opuntia ficus indica (L.) Mill. for treating diabetes, burns, bronchial asthma, constipation, kidney stones, and rheumatic pains and as a sedative in Turkish folk medicine. This study aimed to verify the efficacy of the [...] Read more.
Ethnobotanical field surveys revealed the use of fruits of Opuntia ficus indica (L.) Mill. for treating diabetes, burns, bronchial asthma, constipation, kidney stones, and rheumatic pains and as a sedative in Turkish folk medicine. This study aimed to verify the efficacy of the fruits of O. ficus indica experimentally and to define components responsible for the activity using bioassay-guided procedures. The crude methanolic extract of the fruits was sequentially fractionated into five subextracts: n-hexane, dichloromethane, ethyl acetate, n-butanol, and water. Further experiments were carried out on the most active subextract, that is, the ethyl acetate (EtOAc) subextract, which was further subjected to fractionation through successive column chromatographic applications on Sephadex LH-20. For activity assessment, each extract or fraction was submitted to bioassay systems; traction test, fireplace test, hole-board test, elevated plus-maze test, and open-field test were used for sedative and anxiolytic effects, and a thiopental-induced sleeping test was used for the hypnotic effect. Among the subextracts obtained from the methanolic extract, the EtOAc subextract showed significant sedative and anxiolytic effects in the bioassay systems. From the EtOAc subextract, major components were isolated, and their structures were determined as isorhamnetin, isorhamnetin 3-O-glucoside, isorhamnetin 3-O-rutinoside, and kaempferol 3-O-rutinoside using spectral techniques. In conclusion, this study confirmed the claimed use of the plant against anxiety in Turkish folk medicine. Full article
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