Investigation of the lipophilic extract of the Indonesian sponge Strepsichordaia lendenfeldi afforded three new ceramides, given the names strepsiamides A–C (1–3). The compounds showed cytotoxic activities against L5187Y and Hela cell lines. All structures were unambiguously established by 1D and 2D NMR spectroscopic and mass (EI-, APCI- and GC-MS) spectrometric data.
The quorum sensing inhibitory (QSI) and antimicrobial potentials of the total methanol extract (TME) and different extractives as well as the sesquiterpenes: dehydrodihydrocostus lactone (1), dehydrocostus lactone (2), arbusculin A (3), santamarine (4), reynosin (5), and specioic acid (6) isolated from Costus speciosus rhizomes were evaluated. The CHCl3:EtOAc (1:1), EtOAc, and TME fractions exhibited potent antibacterial activity toward B. cereus with inhibition zone diameter 13 mm. While the CHCl3 fraction showed strong activity towards S. aureus and B. cereus with inhibition zone diameter 11 and 19 mm, respectively. Moreover, the TME and CHCl3 fractions have strong activity towards C. albicans with inhibition zone diameter 15 and 12 mm, respectively. Compound 5 showed prominent activity towards B. cereus (MIC 385 μg/mL). However, 6 exhibited significant activity with MIC values of 150, 400, and 550 μg/mL towards S. aureus, E. coli, and B. cereus, respectively. Moreover, it showed potent antifungal effect towards C. albicans (MIC 320 μg/mL). Most of the tested fractions had QSI activity against C. violaceum. Only compound 6 exhibited moderate QSI effect with disappearance of violet pigment. In addition, compounds 1-6 were evaluated for their in vitro antiproliferative activity towards KB, BT-549, SK-MEL, and SKOV-3 cancer cell lines.
Background: Liver diseases are a common cause of mortality and morbidity over the world. It is caused mainly by toxic chemicals and chemotherapeutic agents. Costus speciosus (Koen ex. Retz.) (Zingiberaceae) is widely employed in various traditional medicines for the prevention and treatment of different aliments. The purpose of this study is to assess the protective effect of C. speciosus rhizomes MeOH extract against the injury of the liver induced by paracetamol (PA) in mice.
Material and Methods: The mice were pretreated for seven days with distilled H2O, silymarin 12 mg/kg or 100 and 200 mg/kg MeOH extract. Then, PA (750 mg/kg) was also intra-peritoneal administrated once a day. Animals were euthanatized 24 h after the damage inducement. The levels of the serum enzymes aspartate aminotransferase (AST), alkaline phosphatase (ALP), alanine aminotransferase (ALT), and aspartate aminotransferase, in addition to the tumor necrosis factor-alpha (TNF-α), were determined. Moreover, the histopathological examination was carried out.
Results: Administration of the MeOH extract (200 mg/kg) showed improvement in the toxic effects of PA through significant fall on the serum markers enzymes of liver damage: AST, ALT, and ALP, as well as TNF-α, compared to silymarin. In parallel, the histopathological profile in the mice` liver also proved that extract markedly minimized the PA toxicity and maintained the liver tissues` histoarchitecture to near the normal ones more than that achieved by silymarin.
Conclusion: The findings suggested that C. speciosus extract acts as a potential hepatoprotective agent against PA-induced liver toxicity. This hepato-protection effect may be due to the existence of steroids, saponins, different glycosides, and phenolic compounds in C. speciosus.
The genus Hylocereus (family Cactaceae) includes about 16 species. Now its reputation is spreading everywhere in the world due to its fruit (pitaya or pitahaya or dragon fruit), which is one of the most popular and widely used functional foods in the world. The fruit is a wealthy provenance of vitamins, minerals, antioxidants, and fiber. The ethno-pharmacological history of this genus indicated that it possesses antioxidant, anticancer, antimicrobial, hepato-protective, antihyperlipidemic, antidiabetic, and wound healing activities. Furthermore, it has been used for the treatment of cough, asthma, hyperactivity, tuberculosis, bronchitis, mumps, diabetes, and cervical lymph node tuberculosis. Different chemical constituents have been reported from this genus as betalains, flavonoids, phenolic acids, phenylpropanoids, triterpenes, sterols, fatty acids, etc. The current review focuses on the uses, botanical characterization, chemical constituents, nutritional importance, biological activities, and safety of Hylocereus species. Also, biosynthetic pathways of betalains have been discussed. Practical applications Pitaya fruit is one of the most known fruit that is commercially grown in different countries of the world for its nutritional advantages. It has acquired a wide acceptance for its pharmacological actions against a variety of ailments. The present review revealed that pitaya contains various bioactive phytoconstituents which might participate directly or indirectly in their highlighted biological effects. Therefore, these compounds can be taken into account as favorable candidates for the development of effective and novel pharmaceutical leads. Deep phytochemical studies of pitaya fruit and its pharmacological effects, especially the mechanism of action of its constituents to clarify the relation between traditional uses and pharmacological activities will obviously be the focus of further research.
In this study, the chemical investigation of Tetraena aegyptia (Zygophyllaceae) led to the identification of a new megastigmene derivative, tetraenone A ((2S, 5R, 6R, 7E)-2-hydroxy-5,6-dihydro-β-ionone) (1), along with (3S, 5R, 6S, 7E)-3-hydroxy-5,6-epoxy-5,6-dihydro-β-ionone- (2), 3,4-dihydroxy-cinnamyl alcohol-4-glucoside (3), 3β,19α-dihydroxy-ursan-28-oic acid (4), quinovic acid (5), p-coumaric acid (6), and ferulic acid (7), for the first time. The chemical structures of 1–7 were confirmed by analysis of their 1D and 2D NMR and HRESIMS spectra and by their comparison with the relevant literature. The absolute configurations of 1 and 2 were assigned based on NOESY interactions and ECD spectra. Conformational analysis showed that 1 existed exclusively in one of the two theoretically possible chair conformers with a predominant s-trans configuration for the 3-oxobut-1-en-1-yl group with the ring, while the half-chair conformer had a pseudo-axial hydroxy group that was predominant over the other half-chair conformation. Boat conformations were not among the most stable conformations, and the s-trans isomerism was in favor of s-cis configuration. In silico investigation revealed that 1 and 2 had more favorable binding interactions with Mpro rather than with TMPRSS2. Accordingly, molecular dynamic simulations were performed on the complexes of compounds 1 and 2 with Mpro to explore the stability of their interaction with the target protein structure. Compounds 1 and 2 might offer a possible starting point for developing covalent inhibitors of Mpro of SARS-CoV-2.
Metabolic syndrome (MetS) represents a worldwide problem. Drugs used in MetS target different symptoms, like excessive body weight, insulin resistance, hyperglycemia, dyslipidemia, or hypertension. Peroxisome proliferator-activated receptors (PPAR) regulate the gene expression involved in lipid metabolism, inflammation, and adipogenesis. Activation of PPARγ has become a target of interest to counter hyperglycemia linked with MetS and type 2 diabetes (T2DM).The current review intended to summarize reported research on medicinal plants, or their bioactive constituents, with PPARγ-activating potential.The research team searched the literature up to 2016 using electronic databases- ScienceDirect, PubMed, Google-Scholar, SpringerLink, Scopus, and Wiley-for publications on medicinal plants with promising PPARγ modulators using keywords diabetes mellitus, natural products, peroxisome proliferator-activated receptors, metabolic syndrome, adipogenesis.This study was conducted in the Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia, Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo, Egypt, and Department of Pharmacognosy and Pharmaceutical Chemistry, College of Pharmacy, Taibah University, Al Madinah, Al Munawwarah, Saudi Arabia.Several natural products were considered to be good ligands for PPARγ. The PPARγ agonistic activity of over 100 plants covered in this review was supported by experimental evidence. Some of the plants and their constituents had been studied for their possible mechanisms of action.Findings discussed in this review highlighted PPARγ's role as an organizer of lipid metabolism and glucose homeostasis, thus supporting its function as a target for antidiabetic agents. The discovery that some natural compounds and plants could activate PPARγ opens up the prospect for future development of strategies to take advantage of its therapeutic potential in diabetes. Therefore, the current review could provide significant information for biotechnological or pharmaceutical applications in targeted drug delivery and design.
The dataset contain a total of 28,000 RGB images belonging to a total of 28 classes. The data was collected from around 50 participants from Zagazig university. The ages of participants are ranging from 15 to 35 years. The images was captured by two mobile phones namely Realme 6, Realme 7, Realme 8. The images were resized into size of 224*224. The inital version of data is available privately on our page: https://www.kaggle.com/datasets/deepologylab/esl-net