Enhancement of Female Rat Fertility via Ethanolic Extract from Nigella sativa L. (Black Cumin) Seeds Assessed via HPLC-ESI-MS/MS and Molecular Docking.

The characteristic chemical composition of Nigella seeds is directly linked to their beneficial properties. This study aimed to investigate the phytochemical composition of Nigella sativa seeds using a 100% ethanolic extract using HPLC-ESI-MS/MS. Additionally, it explored the potential biological effects of the extract on female rat reproduction. Follicle Stimulating Hormone (FSH), Luteinizing Hormone (LH), Estrogen (E2), and Progesterone (P4) hormone levels were also assessed, along with the morphological and histological effects of the extract on ovarian, oviductal, and uterine tissues. Molecular docking was performed to understand the extract's activity and its role in regulating female reproduction by assessing its binding affinity to hormonal receptors. Twenty metabolites, including alkaloids, saponins, terpenes, flavonoids, phenolic acids, and fatty acids, were found in the ethanolic extract of N. sativa seeds through the HPLC-ESI-MS/MS study. The N. sativa seed extract exhibited strong estrogenic and LH-like activities (p < 0.05) with weak FSH-like activity. Furthermore, it increased the serum levels of LH (p < 0.05), P4 hormones (p < 0.001), and E2 (p < 0.0001). Molecular docking results displayed a strong interaction with Erß, LH, GnRH, and P4 receptors, respectively. Based on these findings, N. sativa seeds demonstrated hormone-like activities, suggesting their potential as a treatment for improving female fertility.

Encapsulated polycaprolactone with triazole derivatives and selenium nanoparticles as promising antiproliferative and anticancer agents.

Background and purpose: Polycaprolactone nanocapsules incorporated with triazole derivatives in the presence and absence of selenium nanoparticles were prepared and evaluated as antiproliferative and anticancer agents. Polycaprolactone nanoparticles were prepared using the emulsion technique. Experimental approach: The prepared capsules were characterized using FT-IR, TEM and DLS measurements. The synthesized triazolopyrimidine derivative in the presence and absence of selenium nanoparticles encapsulated in polycaprolactone was tested for its in vitro antiproliferative efficiency towards human breast cancer cell line (MCF7) and murine fibroblast normal cell line (BALB/3T3) in comparison to doxorubicin as a standard anticancer drug. Key results: The results indicated that encapsulated polycaprolactone with selenium nanoparticles (SeNPs) and triazole-SeNPs were the most potent samples against the tested breast cancer cell line (MCF7). On the other hand, all compounds showed weak or moderate activities towards the tested murine fibroblast normal cell line (BALB/3T3). Conclusion: As the safety index (SI) was higher than 1.0, it expanded the way for newly synthesized compounds to express antiproliferative efficacy against tumour cells. Hence, these compounds may be considered promising ones. However, they should be examined through further in-vivo and pharmacokinetic studies.

Evaluation of renal function in children undergoing extracorporeal shock wave lithotripsy.

PURPOSE: The effect of extracorporeal shock wave lithotripsy on the growing kidneys of young children has always been a concern. We determined whether shock wave lithotripsy causes renal parenchymal scarring or affects glomerular filtration rate in children. MATERIALS AND METHODS: This prospective study included 100 children with renal stones who presented to the shock wave lithotripsy unit at our institution between March 2005 and March 2008. A total of 28 children had multiple stones in the same kidney. All children with bilateral renal stones had 1 kidney cleared of stones by percutaneous nephrolithotomy before undergoing shock wave lithotripsy. A total of 138 stones were subjected to shock wave lithotripsy. All children underwent radionuclide scan of the renal parenchyma using dimercapto-succinic acid, and glomerular filtration rate was estimated using diethylenetriamine pentaacetic acid before extracorporeal shock wave lithotripsy and 6 months afterward. Children with renal scarring due to previous surgery or vesicoureteral reflux were excluded from the study. The number of shock wave lithotripsy sessions to achieve stone-free status and the dose of shock waves used were recorded for each patient. RESULTS: No patient demonstrated renal parenchymal scarring on dimercapto-succinic acid scan or any statistically significant change in glomerular filtration rate on diethylenetriamine pentaacetic acid scan up to 6 months after shock wave lithotripsy. CONCLUSIONS: Shock wave lithotripsy is a safe modality for treating renal calculous disease in children up to 16 years old, with no impact on long-term kidney function.

Phyto- and Bio-Chemical evaluation of Diospyros kaki L. cultivated in Egypt and its biological activities.

Diospyros kaki L. or Costata cultivar is the main persimmon variety progressively consumed in the Egyptian market and exportation. The objective of this study was to investigate the bioprotective effects of the alcoholic extract of fruits as well as leaves of D. kaki using in-vivo rat models. Petroleum ether extracts of fruits and leaves were analytically characterized for saponifiable and unsaponifiable compounds by GC/MS. Main flavonoids were chromatographically isolated from 80% aqueous methanol extract of leaves. Chemical evaluation for fruits and leaves namely, content of moisture, ash, proteins, fatty acids, amino acids, fat and water soluble vitamins, minerals, carotenoids was carried out. Total antioxidant activity was determined by radical scavenging effects using DPPH assay. The effect on biochemical parameters and its biological activity were also performed. Results revealed the identification of the major compounds of saponifiable and unsaponifiable matters of fruits and leaves. Scopoletin, as well as, kaempferol, luteolin, rutin and apigenin 7-O-glucoside were isolated and identified. It showed that this plant can provide a good nutritional value and it is safe regarding the kidney and liver functions, good source that help in enhancing the antioxidant defense against free radicals. No abnormal effects were found in lipids profile on experimental animals and there were good results in the ratio of HDL and LDL cholesterol. Also, this plant can help in optimizing blood sugar, enhancing the level of blood haemoglobin. It is concluded that D. kaki displays a good source of nutrients and bioactive compounds that may contribute to its therapeutic benefits against the risk of disease complications.

Brassica juncea L. (Mustard) Extract Silver NanoParticles and Knocking off Oxidative Stress, ProInflammatory Cytokine and Reverse DNA Genotoxicity.

Detoxification is one of the main vital tasks performed by the liver. The purpose of this study was to investigate whether mustard in its normal or nanoparticles could confer a protective/therapeutic effect against TAA-induced acute liver failure in experimental animal models. Mustard ethanolic extract was analyzed by HPLC/MS. To induce liver failure, male rats were injected with 350 mg/kg bw TAA IP, then treated orally with a dose of 100 mg/kg for 15 d of mustard extract and its nanoform before and following induction. The levels of serum liver functions, total cholesterol (TCHo), total glyceride (TG), total bilirubin (TBIL), hepatic malonaldhyde (MDA) and nitric oxide (NO),glutathione (GSH), sodium oxide dismutase (SOD), as well as tumor necrosis factor (TNF-α,) and interleukin 6 (IL-6), were estimated. DNA genotoxicity and hepatic pathology, and immunohistologic (IHC) changes were assayed. The antioxidant content of Phenolic acids, flavonoids in mustard ethanolic extract substantially decreased the levels of ALT, AST, ALP and rehabilitated the histopathological alterations. In addition, nanoforms of mustard ethanol extract have notably increased the levels of GSH, SOD and significantly reduced the levels of MDA. The expression levels of TNF-α and IL-6 in serum and tissue were markedly downregulated. DNA genotoxicity was significantly reversed. Mustard introduced a protective and medicinal effect against TAA in both its forms.

Phyto- and Bio-Chemical evaluation of Diospyros kaki L. cultivated in Egypt and its biological activities / Avaliação fito e bioquímica de Diospyros kaki L. cultivado no Egito e suas atividades biológicas

Abstract Diospyros kaki L. or Costata cultivar is the main persimmon variety progressively consumed in the Egyptian market and exportation. The objective of this study was to investigate the bioprotective effects of the alcoholic extract of fruits as well as leaves of D. kaki using in-vivo rat models. Petroleum ether extracts of fruits and leaves were analytically characterized for saponifiable and unsaponifiable compounds by GC/MS. Main flavonoids were chromatographically isolated from 80% aqueous methanol extract of leaves. Chemical evaluation for fruits and leaves namely, content of moisture, ash, proteins, fatty acids, amino acids, fat and water soluble vitamins, minerals, carotenoids was carried out. Total antioxidant activity was determined by radical scavenging effects using DPPH assay. The effect on biochemical parameters and its biological activity were also performed. Results revealed the identification of the major compounds of saponifiable and unsaponifiable matters of fruits and leaves. Scopoletin, as well as, kaempferol, luteolin, rutin and apigenin 7-O-glucoside were isolated and identified. It showed that this plant can provide a good nutritional value and it is safe regarding the kidney and liver functions, good source that help in enhancing the antioxidant defense against free radicals. No abnormal effects were found in lipids profile on experimental animals and there were good results in the ratio of HDL and LDL cholesterol. Also, this plant can help in optimizing blood sugar, enhancing the level of blood haemoglobin. It is concluded that D. kaki displays a good source of nutrients and bioactive compounds that may contribute to its therapeutic benefits against the risk of disease complications.

Resumo Diospyros kaki L. ou Costata é a principal variedade de caqui progressivamente consumida no mercado e exportação egípcia. O objetivo deste estudo foi investigar os efeitos bioprotetores do extrato alcoólico de frutos e folhas de D. kaki utilizando modelos de ratos "in vivo". Extratos de éter de petróleo provenientes de frutos e folhas foram caracterizados analiticamente para compostos saponificáveis ​​e insaponificáveis ​​por GC/MS. Os principais flavonoides foram isolados cromatograficamente, a partir de 80% de extrato aquoso de folhas de metanol. Foi realizada avaliação química de frutos e folhas, ou seja, de teor de umidade, cinzas, proteínas, ácidos graxos, aminoácidos, vitaminas lipossolúveis e solúveis em água, minerais, carotenoides. Foi caracterizada a atividade antioxidante, utilizando ensaio (DPPH). O efeito nos parâmetros bioquímicos e sua atividade biológica também foram analisados. Os resultados revelaram a identificação dos principais compostos saponificáveis e insaponificáveis de frutos e folhas. Escopoletina, bem como kaempferol, luteolina, rutina e apigenina 7-O-glicosídeo foram isolados e identificados. Também demonstraram que esta planta pode proporcionar um bom valor nutricional e é segura em relação às funções renais e hepáticas, boa fonte que ajuda a melhorar a defesa antioxidante contra os radicais livres. Não foram encontrados efeitos anormais no perfil lipídico em testes em animais, e houve um efeito satisfatório na relação de colesterol HDL e LDL. Além disso, esta planta pode ajudar na otimização do açúcar no sangue, aumentando o nível de hemoglobina. Conclui-se que o D. kaki apresenta uma boa fonte de nutrientes e de compostos bioativos que contribuem para seus benefícios terapêuticos e contra o risco de complicações de doenças.

Phyto- and Bio-Chemical evaluation of Diospyros kaki L. cultivated in Egypt and its biological activities

Abstract Diospyros kaki L. or Costata cultivar is the main persimmon variety progressively consumed in the Egyptian market and exportation. The objective of this study was to investigate the bioprotective effects of the alcoholic extract of fruits as well as leaves of D. kaki using in-vivo rat models. Petroleum ether extracts of fruits and leaves were analytically characterized for saponifiable and unsaponifiable compounds by GC/MS. Main flavonoids were chromatographically isolated from 80% aqueous methanol extract of leaves. Chemical evaluation for fruits and leaves namely, content of moisture, ash, proteins, fatty acids, amino acids, fat and water soluble vitamins, minerals, carotenoids was carried out. Total antioxidant activity was determined by radical scavenging effects using DPPH assay. The effect on biochemical parameters and its biological activity were also performed. Results revealed the identification of the major compounds of saponifiable and unsaponifiable matters of fruits and leaves. Scopoletin, as well as, kaempferol, luteolin, rutin and apigenin 7-O-glucoside were isolated and identified. It showed that this plant can provide a good nutritional value and it is safe regarding the kidney and liver functions, good source that help in enhancing the antioxidant defense against free radicals. No abnormal effects were found in lipids profile on experimental animals and there were good results in the ratio of HDL and LDL cholesterol. Also, this plant can help in optimizing blood sugar, enhancing the level of blood haemoglobin. It is concluded that D. kaki displays a good source of nutrients and bioactive compounds that may contribute to its therapeutic benefits against the risk of disease complications.

Resumo Diospyros kaki L. ou Costata é a principal variedade de caqui progressivamente consumida no mercado e exportação egípcia. O objetivo deste estudo foi investigar os efeitos bioprotetores do extrato alcoólico de frutos e folhas de D. kaki utilizando modelos de ratos in vivo. Extratos de éter de petróleo provenientes de frutos e folhas foram caracterizados analiticamente para compostos saponificáveis e insaponificáveis por GC/MS. Os principais flavonoides foram isolados cromatograficamente, a partir de 80% de extrato aquoso de folhas de metanol. Foi realizada avaliação química de frutos e folhas, ou seja, de teor de umidade, cinzas, proteínas, ácidos graxos, aminoácidos, vitaminas lipossolúveis e solúveis em água, minerais, carotenoides. Foi caracterizada a atividade antioxidante, utilizando ensaio (DPPH). O efeito nos parâmetros bioquímicos e sua atividade biológica também foram analisados. Os resultados revelaram a identificação dos principais compostos saponificáveis e insaponificáveis de frutos e folhas. Escopoletina, bem como kaempferol, luteolina, rutina e apigenina 7-O-glicosídeo foram isolados e identificados. Também demonstraram que esta planta pode proporcionar um bom valor nutricional e é segura em relação às funções renais e hepáticas, boa fonte que ajuda a melhorar a defesa antioxidante contra os radicais livres. Não foram encontrados efeitos anormais no perfil lipídico em testes em animais, e houve um efeito satisfatório na relação de colesterol HDL e LDL. Além disso, esta planta pode ajudar na otimização do açúcar no sangue, aumentando o nível de hemoglobina. Conclui-se que o D. kaki apresenta uma boa fonte de nutrientes e de compostos bioativos que contribuem para seus benefícios terapêuticos e contra o risco de complicações de doenças.

Phospholipase C and protein kinase C-ß 2 mediate insulin-like growth factor II-dependent sphingosine kinase 1 activation.

We recently reported that IGF-II binding to the IGF-II/mannose-6-phosphate (M6P) receptor activates the ERK1/2 cascade by triggering sphingosine kinase 1 (SK1)-dependent transactivation of G protein-coupled sphingosine 1-phosphate (S1P) receptors. Here, we investigated the mechanism of IGF-II/M6P receptor-dependent sphingosine kinase 1 (SK1) activation in human embryonic kidney 293 cells. Pretreating cells with protein kinase C (PKC) inhibitor, bisindolylmaleimide-I, abolished IGF-II-stimulated translocation of green fluorescent protein (GFP)-tagged SK1 to the plasma membrane and activation of endogenous SK1, implicating PKC as an upstream regulator of SK1. Using confocal microscopy to examine membrane translocation of GFP-tagged PKCα, ß1, ß2, δ, and ζ, we found that IGF-II induced rapid, transient, and isoform-specific translocation of GFP-PKCß2 to the plasma membrane. Immunoblotting of endogenous PKC phosphorylation confirmed PKCß2 activation in response to IGF-II. Similarly, IGF-II stimulation caused persistent membrane translocation of the kinase-deficient GFP-PKCß2 (K371R) mutant, which does not dissociate from the membrane after translocation. IGF-II stimulation increased diacylglycerol (DAG) levels, the established activator of classical PKC. Interestingly, the polyunsaturated fraction of DAG was increased, indicating involvement of phosphatidyl inositol/phospholipase C (PLC). Pretreating cells with the PLC inhibitor, U73122, attenuated IGF-II-dependent DAG production and PKCß2 phosphorylation, blocked membrane translocation of the kinase-deficient GFP-PKCß2 (K371R) mutant, and reduced sphingosine 1-phosphate production, suggesting that PLC/PKCß2 are upstream regulators of SK1 in the pathway. Taken together, these data provide evidence that activation of PLC and PKCß2 by the IGF-II/M6P receptor are required for the activation of SK1.

Synthesis, antitumor activity and molecular docking study of novel sulfonamide-Schiff's bases, thiazolidinones, benzothiazinones and their C-nucleoside derivatives.

A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiff's bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or thiosalicylic acids afforded the corresponding 2-arylthiazolidin-4-one or 2-arylbenzothiazin-4-one derivatives 5a-e and/or 6a-e, respectively. Some representative examples of the newly prepared compounds showed considerable cytotoxic effect against breast carcinoma cell line MCF7 and cervix carcinoma cell line HELA in comparison with 5-flurouracil and doxorubicin. AutoDock molecular docking into PTK has been done for lead optimization of the compounds in study as potential PTK inhibitors.