Actinomycetes are a rich source for secondary metabolites with a diverse array of biological activities. Among the various genera of actinomycetes, the genus Saccharopolyspora has long been recognized as a potential source for antibiotics and other therapeutic leads that belong to diverse classes of natural products. Members of the genus Saccharopolyspora have been widely reported from several natural sources including both terrestrial and marine environments. A plethora of this genus has been chemically investigated for the production of novel natural products with interesting pharmacological effects. Therefore, Saccharopolyspora is considered one of the pharmaceutical important genera that could provide further chemical diversity with potential lead compounds. In this review, the literature from 1976 until December 2018 was covered, providing a comprehensive survey of all natural products derived from this genus and their semi-synthetic derivatives along with their biological activities, whenever applicable. Moreover, the biological diversity of Saccharopolyspora species and their habitats were also discussed.
A new cyclic pentapeptide, cotteslosin C (1), a new aflaquinolone, 22-epi-aflaquinolone B (3), and two new anthraquinones (9 and 10), along with thirty known compounds (2, 4 – 8, 11 – 34) were isolated from a co-culture of the sponge-associated fungus Aspergillus versicolor with Bacillus subtilis. The new metabolites were only detected in the co-culture extract, but not when the fungus was grown under axenic conditions. Furthermore, the co-culture extract exhibited an enhanced accumulation of the known constituents versicolorin B (14), averufin (16), and sterigmatocyctin (19) by factors of 1.5, 2.0, and 4.7, respectively, compared to the axenic fungal culture. The structures of the isolated compounds were elucidated on the basis of 1D and 2D NMR spectra and mass spectrometry as well as by comparison with literature data. The absolute configuration of compounds 3, 9, and 10 was determined by ECD (electronic circular dichroism) analysis aided by TDDFT-ECD (time-dependent density functional theory electronic circular dichroism) calculations. Compounds 15, 18 – 21, and 26 exhibited strong to moderate cytotoxic activity against the mouse lymphoma cell line L5178Y, with IC50 values ranging from 2.0 to 21.2 µM, while compounds 14, 16, 31, 32, and 33 displayed moderate inhibitory activities against several gram-positive bacteria, with MIC values ranging from 12.5 to 50 µM.
The genus Aspergillus is widely distributed in terrestrial and marine environments.
The Chelonaplysilla genus possesses a numerous bioactive diterpenes with antiinflammatory and cytotoxic effects. The current study aimed to assess the chemical composition of C. erecta crude extract (CECE) based on its metabolomic profile that has been integrated with neural network-based virtual screening and molecular docking using liquid chromatography with high resolution mass spectrometry (LCHR-MS). In addition to the estimation of the antitumor activity of the same extract via anti-interleukin-17A (IL-17) action, along with its formulated spanlastics preparation. The CECE markedly displayed growth inhibition for HepG-2 cells at IC 50 value 16.5 ± 0.8 μg/mL, whereas the spanlastic formulation revealed more eminent antitumor effect against Caco-2 cells (IC 50 = 2.8 ± 0.03 μg/mL). Among the dereplicated compounds, macfarlandin F ( 16) and pourewanone ( 25) demonstrated the highest potential with co-crystallized ligand 63O within the active site of IL-17A in molecular docking studies. These findings rationalized the antitumor mechanism of marine organism for future chemotherapeutic applications. Experimental Sponge materialThe marine sponge Chelonaplysilla erecta was collected by Prof. D. Hajjar and A. A. Makki, from the Red Sea, Jeddah side. The sponge possessed an upright growing skeleton with long and thick spongin fibres. Characteristically, the dendritic fibres anastomose frequently with each other in agreement with previous literature (Tsurnamal 2013). The specimens were washed then with 1% phosphate buffered saline (PBS), immediately on the boat. The specimens with their label were wrapped in aluminium foil and placed on ice, then stored at -80 °C until further processing. The specimen's surface peel was removed and immersed in xylene for 24 hours. DPX (Dibutyl Phthalate Polystyrene Xylene) was used to mount a permanent slide of the peel. Under a stereo microscope, a single fibre with its base and branches intact was extracted from the sponge for species identification. Sponge samples were identified by Prof. Dr. El-Sayd Abed El-
Diabetes mellitus (DM) is a complicated condition that is accompanied by a plethora of metabolic symptoms, including disturbed serum glucose and lipid profiles. Several herbs are reputed as traditional medicine to improve DM. The current study was designed to explore the chemical composition and possible ameliorative effects of Ocimum forskolei on blood glucose and lipid profile in high-fat diet/streptozotocin-induced diabetic rats and in 3T3-L1 cell lines as a first report of its bioactivity. Histopathological study of pancreatic and adipose tissues was performed in control and treatment groups, along with quantification of glucose and lipid profiles and the assessment of NF-κB, cleaved caspase-3, BAX, and BCL2 markers in rat pancreatic tissue. Glucose uptake, adipogenic markers, DGAT1, CEBP/α, and PPARγ levels were evaluated in the 3T3-L1 cell line. Hesperidin was isolated from total methanol extract (TME). TME and hesperidin significantly controlled the glucose and lipid profile in DM rats. Glibenclamide was used as a positive control. Histopathological assessment showed that TME and hesperidin averted necrosis and infiltration in pancreatic tissues, and led to a substantial improvement in the cellular structure of adipose tissue. TME and hesperidin distinctly diminished the mRNA and protein expression of NF-κB, cleaved caspase-3, and BAX, and increased BCL2 expression (reflecting its protective and antiapoptotic actions). Interestingly, TME and hesperidin reduced glucose uptake and oxidative lipid accumulation in the 3T3-L1 cell line. TME and hesperidin reduced DGAT1, CEBP/α, and PPARγ mRNA and protein expression in 3T3-L1 cells. Moreover, docking studies supported the results via deep interaction of hesperidin with the tested biomarkers. Taken together, the current study demonstrates Ocimum forskolei and hesperidin as possible candidates for treating diabetes mellitus.
Broccoli (Brassica oleracea) is reported to possess antioxidant activity that could potentially prevent oxidative damage to tissues caused by many diseases. In the present study, we investigated the preventive effect of broccoli leaf by-product extract (BL) on gentamicin-induced renal and hepatic injury by measuring tissue antioxidant activities and morphological apoptotic changes. Broccoli leaf was thoroughly extracted with 70% methanol to yield the total methanol extract (TME). The total phenolic content (TPC) was determined. Thirty male rats were divided into five groups (six animals/group). Group I received phosphate-buffered saline orally, while group II was treated with gentamicin (100 mg/kg i.p. intraperitoneal) for ten days. Group III and group IV animals were given BL (200 mg/kg and 400 mg/kg, respectively) plus gentamicin treatment. Group V received L-cysteine (1 mmole/kg) plus gentamicin. Antioxidant and biochemical parameters, such as transaminase (AST), alanine transaminase (ALT) and alkaline phosphatase (ALP), creatinine, and urea, and mRNA expression levels of tumor necrosis factor alpha (TNF-α), interleukin-1β (IL-1β), and nuclear factor kappa B (NFkB) were determined in various groups, along with the quantification of inflammatory and apoptotic cells in hepatic and renal tissues. Malondialdehyde (MDA), glutathione (GSH), and superoxide dismutase (SOD) levels were determined in liver and renal samples. Histopathological studies of the liver and kidneys were also carried out. The TME was subjected to various and repeated techniques of chromatography to yield caffeic acid, gallic acid, and methyl gallate. The TPC was 6.47 mg Gallic Acid Equivalent/g of dry extract. Gentamicin increased the levels of serum AST, ALT, ALP, creatinine, and urea. The MDA and GSH contents and theactivity levels of the antioxidant enzyme SOD decreased in liver and kidney samples with gentamicin administration. BL administration dose-dependently prevented the alteration in biochemical parameters and was supported by low levels of tubular and glomerular injuries induced by gentamicin. This study valorizes the potential of BL as a preventive candidate in cases of gentamicin-induced liver and kidney toxicity and recommends further clinical studies using BL to validate its utilization for human consumption and as a source of phenolics for nutraceutical and pharmaceutical purposes.
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