المؤلفون: Mona Alonazi, Assem Barakat, Taghreed M Al-Otaibi, Zainab M. Almarhoon, Nahed N. E. El-Sayed, Abir Ben Bacha, Vijay H. Masand

المصدر: Molecules, Vol 26, Iss 3121, p 3121 (2021)
Molecules; Volume 26; Issue 11; Pages: 3121

مصطلحات موضوعية: In silico, Lactate dehydrogenase A, lactate dehydrogenase A, Pharmaceutical Science, Organic chemistry, colorectal cancer, Analytical Chemistry, 03 medical and health sciences, chemistry.chemical_compound, 0302 clinical medicine, QD241-441, quinoxaline, Drug Discovery, Quinazoline, Physical and Theoretical Chemistry, Cytotoxicity, education, Quinazolinone, 030304 developmental biology, 0303 health sciences, education.field_of_study, dysbiosis, Warburg effect, In vitro, Multiple drug resistance, chemistry, Chemistry (miscellaneous), cyclooxygenase-2, 030220 oncology & carcinogenesis, Cancer research, Molecular Medicine, quinazoline, ADMET

الوصف: The pathogenesis of colorectal cancer is a multifactorial process. Dysbiosis and the overexpression of COX-2 and LDHA are important effectors in the initiation and development of the disease through chromosomal instability, PGE2 biosynthesis, and induction of the Warburg effect, respectively. Herein, we report the in vitro testing of some new quinoxalinone and quinazolinone Schiff’s bases as: antibacterial, COX-2 and LDHA inhibitors, and anticolorectal agents on HCT-116 and LoVo cells. Moreover, molecular docking and SAR analyses were performed to identify the structural features contributing to the biological activities. Among the synthesized molecules, the most active cytotoxic agent, (6d) was also a COX-2 inhibitor. In silico ADMET studies predicted that (6d) would have high Caco-2 permeability, and %HIA (99.58%), with low BBB permeability, zero hepatotoxicity, and zero risk of sudden cardiac arrest, or mutagenicity. Further, (6d) is not a potential P-gp substrate, instead, it is a possible P-gpI and II inhibitor, therefore, it can prevent or reverse the multidrug resistance of the anticancer drugs. Collectively, (6d) can be considered as a promising lead suitable for further optimization to develop anti-CRC agents or glycoproteins inhibitors.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fea7ea656c9a63e14bc63484d9973b6fTest
https://www.mdpi.com/1420-3049/26/11/3121Test

المؤلفون: Ramūnas Antanaitis, Mingaudas Urbutis, Mindaugas Televičius, Dovilė Malašauskienė, Vida Juozaitienė, Walter Baumgartner

المصدر: Sensors, Vol 21, Iss 1414, p 1414 (2021)
Sensors (Basel, Switzerland)

مصطلحات موضوعية: 040301 veterinary sciences, media_common.quotation_subject, In-line, Insemination, lcsh:Chemical technology, Biochemistry, Analytical Chemistry, 0403 veterinary science, chemistry.chemical_compound, Milk yield, Animal science, Pregnancy, Lactate dehydrogenase, Medicine, Animals, Lactation, lcsh:TP1-1185, Electrical and Electronic Engineering, Instrumentation, Progesterone, media_common, Sweden, 3-Hydroxybutyric Acid, L-Lactate Dehydrogenase, business.industry, Communication, 0402 animal and dairy science, Milking robot, food and beverages, biomarkers, 04 agricultural and veterinary sciences, medicine.disease, biosensors, 040201 dairy & animal science, Atomic and Molecular Physics, and Optics, Body condition scoring, Milk, chemistry, automated body condition scoring system, Herd, Cattle, Female, Reproduction, business

الوصف: The aim of the current study was to evaluate the relation of automatically determined body condition score (BCS) and inline biomarkers such as β-hydroxybutyrate (BHB), milk yield (MY), lactate dehydrogenase (LDH), and progesterone (mP4) with the pregnancy success of cows. The cows (n = 281) had 2.1 ± 0.1. lactations on average, were 151.6 ± 0.06 days postpartum, and were once tested with “Easy scan” ultrasound (IMV imaging, Scotland) at 30–35 d post-insemination. According to their reproductive status, cows were grouped into two groups: non-pregnant (n = 194 or 69.0% of cows) and pregnant (n = 87 or 31.0% of cows). Data concerning their BCS, mP4, MY, BHB, and LDH were collected each day from the day of insemination for 7 days. The BCS was collected with body condition score camera (DeLaval Inc., Tumba, Sweden); mP4, MY, BHB, and LDH were collected with the fully automated real-time analyzer Herd Navigator™ (Lattec I/S, Hillerød, Denmark) in combination with a DeLaval milking robot (DeLaval Inc., Tumba, Sweden). Of all the biomarkers, three differences between groups were significant. The body condition score (BCS) of the pregnant cows was higher (+0.49 score), the milk yield (MY) was lower (-4.36 kg), and milk progesterone in pregnant cows was (+6.11 ng/mL) higher compared to the group of non-pregnant cows (p < 0.001). The pregnancy status of the cows was associated with their BCS assessment (p < 0.001). We estimated that cows with BCS > 3.2 were 22 times more likely to have reproductive success than cows with BCS ≤ 3.2.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb2332ab57fb0f15cdbe997a06f41a78Test
https://www.mdpi.com/1424-8220/21/4/1414Test

المؤلفون: Blassan P. George, Rahul Chandran, Heidi Abrahamse

المصدر: Molecules, Vol 25, Iss 2900, p 2900 (2020)
Molecules
Volume 25
Issue 12

مصطلحات موضوعية: Male, Syzygium, Pharmaceutical Science, Pharmacology, 030226 pharmacology & pharmacy, Analytical Chemistry, chemistry.chemical_compound, Mice, 0302 clinical medicine, Adenosine Triphosphate, Drug Discovery, Edema, pain, Analgesics, Chemistry, Anti-Inflammatory Agents, Non-Steroidal, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, Toxicity, MCF-7 Cells, Plant Bark, Molecular Medicine, Female, medicine.symptom, medicine.drug_class, inflammatory mediators, Analgesic, Inflammation, Hoechst stain, Anti-inflammatory, Article, lcsh:QD241-441, 03 medical and health sciences, lcsh:Organic chemistry, In vivo, Lactate dehydrogenase, medicine, Toxicity Tests, Acute, Animals, Humans, granuloma tissue, Physical and Theoretical Chemistry, Rats, Wistar, Cell Proliferation, Plants, Medicinal, L-Lactate Dehydrogenase, Plant Extracts, Methanol, Organic Chemistry, lactate dehydrogenase, Antineoplastic Agents, Phytogenic, Carrageenan

الوصف: Cancer, pain and inflammation have long been a cause for concern amongst patients, clinicians and research scientists. There is an alarming increase in the demand for medicines suppressing these disease conditions. The present study investigates the role of Syzygium mundagam bark methanol (SMBM) extract against MCF-7 breast cancer cells, pain and inflammation. The MCF-7 cells treated with SMBM were analyzed for adenosine triphosphate (ATP), lactate dehydrogenase (LDH) levels, changes in cell morphology and nuclear damage. Hot plate, acetic acid and formalin-induced pain models were followed to determine the analgesic activity. Anti-inflammatory activity was studied using carrageenan, egg albumin and cotton pellet induced rat models. Microscopic images of cells in SMBM treated groups showed prominent cell shrinkage and nuclear damage. Hoechst stain results supported the cell death morphology. The decline in ATP (47.96%) and increased LDH (40.96%) content indicated SMBM induced toxicity in MCF-7 cells. In the in vivo study, a higher dose (200 mg/kg) of the extract was found to be effective in reducing pain and inflammation. The results are promising and the action of the extract on MCF-7 cells, pain and inflammation models indicate the potential of drugs of natural origin to improve current therapies.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::989c72e0c8876a1cd6d7f8b4a9574a30Test
https://www.mdpi.com/1420-3049/25/12/2900Test

المؤلفون: Prosper Kanyong, Francis D. Krampa, Yaw Aniweh, Gordon A. Awandare

المصدر: Sensors, Vol 20, Iss 3, p 799 (2020)
Sensors (Basel, Switzerland)

مصطلحات موضوعية: Computer science, Protozoan Proteins, Biosensing Techniques, Review, 02 engineering and technology, lcsh:Chemical technology, 01 natural sciences, Biochemistry, Analytical Chemistry, chemistry.chemical_compound, Glutamate Dehydrogenase, Fructose-Bisphosphate Aldolase, lcsh:TP1-1185, Malaria, Falciparum, Instrumentation, biology, Hemozoin, 021001 nanoscience & nanotechnology, Atomic and Molecular Physics, and Optics, 3. Good health, clinical diagnosis, 0210 nano-technology, Hemeproteins, Plasmodium falciparum, Early detection, Antigens, Protozoan, Computational biology, medical devices, Lactate dehydrogenase, parasitic diseases, medicine, Humans, Diagnostic biomarker, Electrical and Electronic Engineering, L-Lactate Dehydrogenase, Diagnostic Tests, Routine, Glutamate dehydrogenase, 010401 analytical chemistry, Aldolase A, biology.organism_classification, medicine.disease, biosensors, 0104 chemical sciences, chemistry, Clinical diagnosis, biology.protein, malaria biomarkers, biosensing, Biosensor, Malaria

الوصف: The impact of malaria on global health has continually prompted the need to develop more effective diagnostic strategies that could overcome deficiencies in accurate and early detection. In this review, we examine the various biosensor-based methods for malaria diagnostic biomarkers, namely; Plasmodium falciparum histidine-rich protein 2 (PfHRP-2), parasite lactate dehydrogenase (pLDH), aldolase, glutamate dehydrogenase (GDH), and the biocrystal hemozoin. The models that demonstrate a potential for field application have been discussed, looking at the fabrication and analytical performance characteristics, including (but not exclusively limited to): response time, sensitivity, detection limit, linear range, and storage stability, which are first summarized in a tabular form and then described in detail. The conclusion summarizes the state-of-the-art technologies applied in the field, the current challenges and the emerging prospects for malaria biosensors.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a846a7f06f611d466c348bfad0dce96Test
https://www.mdpi.com/1424-8220/20/3/799Test

المؤلفون: Aneta Ostróżka-Cieślik, Barbara Dolińska, Florian Ryszka

المصدر: Molecules
Molecules, Vol 26, Iss 3465, p 3465 (2021)
Volume 26
Issue 11

مصطلحات موضوعية: prolactin, endocrine system, Antioxidant, Swine, preservation, Sodium, medicine.medical_treatment, Potassium, Pharmaceutical Science, chemistry.chemical_element, Cold storage, Zinc, Kidney, Article, perfusion, Analytical Chemistry, 03 medical and health sciences, chemistry.chemical_compound, QD241-441, Ischemia, Lactate dehydrogenase, Drug Discovery, medicine, Animals, Aspartate Aminotransferases, Physical and Theoretical Chemistry, 030304 developmental biology, Cryopreservation, 0303 health sciences, Creatinine, Chromatography, L-Lactate Dehydrogenase, zinc, 030302 biochemistry & molecular biology, Organic Chemistry, Alanine Transaminase, Organ Preservation, Biolasol, Prolactin, chemistry, Chemistry (miscellaneous), Molecular Medicine, renal, hormones, hormone substitutes, and hormone antagonists

الوصف: Zinc is an effective anti-inflammatory and antioxidant trace element. The aim of this study was to analyse the protective effect of zinc and zinc–prolactin systems as additives of preservation solutions in the prevention of nephron damage caused during ischemia. The study used a model for storing isolated porcine kidneys in Biolasol®. The solution was modified with the addition of Zn at a dose of 1 µg/L and Zn: 1 µg/L with prolactin (PRL): 0.1 µg/L. After 2 h and 48 h of storage, the levels of alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, sodium, potassium, creatinine and total protein were determined. Zinc added to the Biolasol® composition at a dose of 1 µg/L showed minor effectiveness in the protection of nephrons. In turn, Zn2+ added to Biolasol + PRL (PRL: 0.1 µg/L) acted as a prolactin inhibitor. We do not recommend the addition of Zn(II) (1 µg/L) and Zn(II) (1 µg/L) + PRL (0.1 µg/L) to the Biolasol solution.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91c6de6d597a52c2f083f5b2a9e346b6Test
https://doi.org/10.3390/molecules26113465Test

المؤلفون: Predeepkumar Narayanappa Shiroorkar, Imran Kazmi, Kumar Shiva Gubbiyappa, Obaid Afzal, Nagaraja Sreeharsha, Fahad A. Al-Abbasi, Abdulmalik Saleh Alfawaz Altamimi

المصدر: Molecules, Vol 25, Iss 5622, p 5622 (2020)
Molecules
Volume 25
Issue 23

مصطلحات موضوعية: Male, PTEN, animal diseases, Pharmaceutical Science, Pharmacology, Analytical Chemistry, Protein Carbonylation, Rats, Sprague-Dawley, sepsis, chemistry.chemical_compound, 0302 clinical medicine, Drug Discovery, Tensin, Cecum, 0303 health sciences, biology, medicine.diagnostic_test, Cell Death, TOR Serine-Threonine Kinases, Heart, Glutathione, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, mTOR, Molecular Medicine, puncture, Cardiomyopathies, STAT3 Transcription Factor, Cardiotonic Agents, Punctures, cecum ligation, Article, Sepsis, lcsh:QD241-441, 03 medical and health sciences, Western blot, tangeretin, lcsh:Organic chemistry, Lactate dehydrogenase, NLR Family, Pyrin Domain-Containing 3 Protein, medicine, Autophagy, Animals, Physical and Theoretical Chemistry, Protein kinase B, Ligation, PI3K/AKT/mTOR pathway, 030304 developmental biology, business.industry, Myocardium, AKT, Organic Chemistry, PTEN Phosphohydrolase, medicine.disease, Flavones, Disease Models, Animal, chemistry, biology.protein, Tyrosine, Creatine kinase, business, Proto-Oncogene Proteins c-akt

الوصف: Sepsis aggregates undesirable immune response causing depression of ventricular myocardium and diastolic dysfunction. This present study examined the effect of a plant-derived flavone tangeretin (TG) on autophagy and reduction in myocardial dysfunction. The sepsis was induced by cecum ligation and puncture (CLP) in male Sprague&ndash
Dawley rats. Abnormal changes were seen in the heart after the sepsis induction. These abnormalities were analyzed based on the cardiac markers, namely Cardiac myosin light chain-1 (cMLC1) and Cardiac troponin I (cTnl), echocardiography, and plasma parameters, like Lactate dehydrogenase (LDH) and Creatinine kinase (CK). Microanatomy of the heart was studied using hematoxylin and eosin stained histopathological samples of cardiac tissue. Western blot technique was used to detect the nature and extent of protein with the amount of a specific RNA (gene expression) in the cardiac homogenate. Oxidative damage was analyzed using redox marker, reduced glutathione. This study successfully showed that TG attenuated sepsis-induced myocardial dysfunction by inhibiting myocardial autophagy via silencing the Phosphatase and tensin homolog (PTEN) expression and acting on the AKT/mTOR pathway. The present findings supported that TG is a novel cardioprotective therapeutic target for sepsis induced myocardial dysfunction.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f83ce38d2ea0a5388fbccdd114955b5Test
https://www.mdpi.com/1420-3049/25/23/5622Test

المؤلفون: Jung Sook Jin, MinJeong Kim, Syng-Ook Lee, Sung-Jin Bae, Ki-Tae Ha, Hee-Jin Choi, Dongryeol Ryu, Jung Ho Han

المصدر: Molecules
Volume 26
Issue 6
Molecules, Vol 26, Iss 1579, p 1579 (2021)

مصطلحات موضوعية: Male, Phytochemicals, Administration, Oral, Pharmaceutical Science, AMP-Activated Protein Kinases, Pharmacology, Sanguisorba, Analytical Chemistry, Sanguisorba officinalis L, Mice, 0302 clinical medicine, Sanguisorba officinalis, Drug Discovery, Glycolysis, 0303 health sciences, education.field_of_study, biology, Chemistry, glycolysis, Physical Functional Performance, Medicine, Korean Traditional, Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, herbal medicine, Officinalis, Molecular Medicine, medicine.symptom, Myoblasts, Skeletal, Lactate dehydrogenase A, Alpha (ethology), Inflammation, Article, LDHA, Cell Line, lcsh:QD241-441, 03 medical and health sciences, lcsh:Organic chemistry, medicine, Animals, Lactic Acid, Physical and Theoretical Chemistry, education, 030304 developmental biology, Plants, Medicinal, Muscle fatigue, Plant Extracts, Organic Chemistry, physical performance, biology.organism_classification, Enzyme assay, Mice, Inbred C57BL, Exercise Test, Physical Endurance, biology.protein, Lactate Dehydrogenase 5, Phytotherapy

الوصف: Muscle fatigue is induced by an acute or chronic physical performance inability after excessive physical activity often associated with lactate accumulation, the end-product of glycolysis. In this study, the water-extracted roots of Sanguisorba officinalis L., a herbal medicine traditionally used for inflammation and diarrhea, reduced the activities of lactate dehydrogenase A (LDHA) in in vitro enzyme assay myoblast C2C12 cells and murine muscle tissue. Physical performance measured by a treadmill test was improved in the S. officinalis-administrated group. The analysis of mouse serum and tissues showed significant changes in lactate levels. Among the proteins related to energy metabolism-related physical performance, phosphorylated-AMP-activated protein kinase alpha (AMPKα) and peroxisome proliferator-activated receptor-coactivator-1 alpha (PGC-1α) levels were enhanced, whereas the amount of LDHA was suppressed. Therefore, S. officinalis might be a candidate for improving physical performance via inhibiting LDHA and glycolysis.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e31725dd12bf86567d40ea446447ca6Test
https://doi.org/10.3390/molecules26061579Test

المؤلفون: Maged E. Mohamed, Nancy S. Younis

المصدر: Molecules, Vol 24, Iss 10, p 1929 (2019)
Molecules
Volume 24
Issue 10

مصطلحات موضوعية: Male, Myocardial Infarction, Pharmaceutical Science, Blood Pressure, Pharmacology, Analytical Chemistry, Rats, Sprague-Dawley, chemistry.chemical_compound, Electrocardiography, 0302 clinical medicine, Drug Discovery, Medicine, Myocardial infarction, Receptor, Creatine Kinase, 0303 health sciences, Membrane Glycoproteins, biology, NF-kappa B, Chemistry (miscellaneous), 030220 oncology & carcinogenesis, cardiovascular system, Molecular Medicine, Sesquiterpenes, heat shock protein 60, Creatine, Protective Agents, Article, lcsh:QD241-441, 03 medical and health sciences, lcsh:Organic chemistry, Lactate dehydrogenase, Animals, cardiovascular diseases, Physical and Theoretical Chemistry, 030304 developmental biology, Adaptor Proteins, Signal Transducing, Polycyclic Sesquiterpenes, Biological Products, L-Lactate Dehydrogenase, business.industry, isoproterenol, Organic Chemistry, medicine.disease, MyD88, TLR2, chemistry, toll-like receptors, TRIF, Myeloid Differentiation Factor 88, biology.protein, TLR4, Creatine kinase, β-caryophyllene, business

الوصف: Myocardial infarction (MI) remains one of the major causes of mortality around the world. A possible mechanism involved in myocardial infarction is the engagement of Toll-like receptors (TLRs). This study was intended to discover the prospective cardioprotective actions of &beta
caryophyllene, a natural sesquiterpene, to ameliorate isoproterenol (ISO)-induced myocardial infarction through HSP-60/TLR/MyD88/NF&kappa
B pathway. &beta
Caryophyllene (100 or 200 mg/kg/day orally) was administered for 21 days then MI was induced via ISO (85 mg/kg, subcutaneous) on 20th and 21st days. The results indicated that ISO induced a significant infarcted area associated with several alterations in the electrocardiogram (ECG) and blood pressure (BP) indices and caused an increase in numerous cardiac indicators such as creatine phosphokinase (CPK), creatine kinase-myocardial bound (CK-MB), lactate dehydrogenase (LDH), and cardiac tropinine T (cTnT). In addition, ISO significantly amplified heat shock protein 60 (HSP-60) and other inflammatory markers, such as TNF-&alpha
IL-I&beta
and NF&kappa
B, and affected TLR2 and TLR4 expression and their adaptor proteins
Myeloid differentiation primary response 88 (MYD88), and TIR-domain-containing adapter-inducing interferon-&beta
(TRIF). On the other hand, consumption of &beta
caryophyllene significantly reversed the infarcted size, ECG and BP alterations, ameliorated the ISO elevation in cardiac indicators
it also notably diminished HSP-60, and subsequently TLR2, TLR4, MYD88, and TRIF expression, with a substantial reduction in inflammatory mediator levels. This study revealed the cardioprotective effect of &beta
caryophyllene against MI through inhibiting HSP-60/TLR/MyD88/NF&kappa
B signaling pathways.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::349906ff7bff4ee71a12bae95b7bdbe1Test
https://www.mdpi.com/1420-3049/24/10/1929Test

المؤلفون: Abdulhakeem S. Alamri, Majid Alhomrani, Walaa F. Alsanie, Syed Mohammed Basheeruddin Asdaq

المصدر: Molecules
Volume 26
Issue 17
Molecules, Vol 26, Iss 5137, p 5137 (2021)

مصطلحات موضوعية: Thiobarbituric acid, Myocardial Infarction, Pharmaceutical Science, Pharmacology, Antioxidants, Analytical Chemistry, Rats, Sprague-Dawley, chemistry.chemical_compound, QD241-441, Drug Discovery, Disulfides, Carvedilol, biology, garlic oil, Diallyl disulfide, NF-b p65, catalase, Heart, diallyl disulfide, Allyl Compounds, IL-1β, Chemistry (miscellaneous), Molecular Medicine, medicine.drug, Cardiotonic Agents, carvedilol, Thiobarbituric Acid Reactive Substances, cardiac troponin C, Article, Superoxide dismutase, Isoprenaline, Lactate dehydrogenase, medicine, TBARS, Animals, SOD, Physical and Theoretical Chemistry, Garlic, IL-6, Superoxide Dismutase, Tumor Necrosis Factor-alpha, Myocardium, Organic Chemistry, Isoproterenol, Rats, Disease Models, Animal, chemistry, TNF-α, biology.protein, Creatine kinase

الوصف: In isoprenaline (ISO)-induced myocardial infarcted rats, garlic oil (GO) and its main ingredient, diallyl disulfide (DADS), were examined for cardioprotective effects when used with carvedilol (CAR). GO, DADS and CAR were given to rats in their respective groups, either alone or together, with the addition of isoprenaline (3 mg/kg/day, subcutaneously) during the last 10 days of treatment. At the end of 14 days of treatment, blood samples were collected, the hearts were excised under anesthesia and weighed. Heart tissue homogenate was used to measure superoxide dismutase (SOD), catalase (CAT), and thiobarbituric acid reactive substances (TBARS). Furthermore, the serum activities of cardiac markers, including lactate dehydrogenase, creatine kinase, and cardiac troponin, were checked. Moreover, inflammatory markers including tumor necrosis factor alpha, interleukin one beta, interleukin six, and kappa bp65 subunit were assessed. Rats that received GO, DADS, and CAR exhibited a significant increase in the cardiac antioxidant enzyme activities with a simultaneous decrease in serum cardiac markers enzymes and inflammatory markers. The TBARS were significantly reduced in rats that received treatment. The addition of carvedilol to GO or DADS significantly elevated antioxidant activities and decreased the release of cardiac enzymes into blood circulation. Both DADS and GOl were almost similar in efficacy, indicating the potential role of DADS in garlic oil-mediated cardioprotection. Combining GO or DADS with CAR increased CAR’s cardioprotective impact and protected rats from developing ISO-induced myocardial infarction.

وصف الملف: application/pdf

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f3ea53bee2f0e1105aaf16257c2224cTest
https://doi.org/10.3390/molecules26175137Test

المؤلفون: Nasir Tajuddeen, Heinrich C. Hoppe, Tarryn Swart, Fanie R. van Heerden

المصدر: Molecules, Vol 26, Iss 3875, p 3875 (2021)
Molecules

مصطلحات موضوعية: Plasmodium falciparum, malaria, Pappea capensis, Pharmaceutical Science, Sapindaceae, Pappea, 01 natural sciences, Article, Analytical Chemistry, HeLa, Antimalarials, chemistry.chemical_compound, QD241-441, antiplasmodial, Lactate dehydrogenase, parasitic diseases, Drug Discovery, Humans, HeLa cells, Malaria, Falciparum, Physical and Theoretical Chemistry, Cytotoxicity, biology, Traditional medicine, Cytotoxins, 010405 organic chemistry, Organic Chemistry, Resazurin, biology.organism_classification, 0104 chemical sciences, Plant Leaves, 010404 medicinal & biomolecular chemistry, chemistry, Phytochemical, Chemistry (miscellaneous), flavonoids, Molecular Medicine, Apiaceae

الوصف: Ethnobotanical surveys indicate that the Masai and Kikuyu in Kenya, the Venda in South Africa, and the Gumuz people of Ethiopia use Pappea capensis for the treatment of malaria. The present study aimed to investigate the phytochemical and antiplasmodial properties of the plant leaves. The bioactive compounds were isolated using chromatographic techniques. The structures were established using NMR, HRMS, and UV spectroscopy. Antiplasmodial activity of P. capensis leaf extract and isolated compounds against chloroquine-sensitive 3D7 P. falciparum was evaluated using the parasite lactate dehydrogenase assay. Cytotoxicity against HeLa (human cervix adenocarcinoma) cells was determined using the resazurin assay. The extract inhibited the viability of Plasmodium falciparum by more than 80% at 50 µg/mL, but it was also cytotoxic against HeLa cells at the same concentration. Chromatographic purification of the extract led to the isolation of four flavonoid glycosides and epicatechin. The compounds displayed a similar activity pattern with the extract against P. falciparum and HeLa cells. The results from this study suggest that the widespread use of P. capensis in traditional medicine for the treatment of malaria might have some merits. However, more selectivity studies are needed to determine whether the leaf extract is cytotoxic against noncancerous cells.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eca3b5bd490b810137f1fb9a241be066Test
https://doi.org/10.3390/molecules26133875Test