Antiproliferative Activity of Lignans from Olea ferruginea: In Vitro Evidence Supported by Docking Studies.

BACKGROUND: The aim of the current study was to investigate the anticancer potential of bioactive compounds isolated from the leaves of Olea ferruginea (O. ferruginea). Lignans from O. ferruginea were previously described to possess antibacterial, antileishmanial, and antioxidant properties. Nevertheless, the antiproliferative activity of cycloolivil (1), ferruginan (2), and ferruginan A (3) have not been investigated in depth. METHODS: The compounds were isolated from the ethyl acetate fraction of the leaves extract of O. ferruginea. The isolated molecules were evaluated for their anticancer activity against U-87 MG malignant glioma cells. In parallel, molecular docking studies were also performed to investigate the interaction of the compounds with a duplex DNA sequence and epidermal growth factor receptor (EGFR). RESULTS: In vitro tests showed that all three compounds inhibit U-87 MG malignant glioma cell proliferation dose-dependently in the µM range, and ferruginan A (3) was highlighted as the most promising compound of the set. Molecular docking studies showed that the compounds could interfere with double stranded DNA possessing a cisplatin 1,2-d(GpG) intrastrand cross-link and EGFR. CONCLUSIONS: Overall, the findings suggest that the tested compounds from O. ferruginea may represent a starting point for the identification of novel tools to inhibit glioma cell proliferation.

Edible mushrooms as potential functional foods in amelioration of hypertension.

Edible mushrooms are popular functional foods attributed to their rich nutritional bioactive constituent profile influencing cardiovascular function. Edible mushrooms are omnipresent in various prescribed Dietary Approaches to Stop Hypertension, Mediterranean diet, and fortified meal plans as they are rich in amino acids, dietary fiber, proteins, sterols, vitamins, and minerals. However, without an understanding of the influence of mushroom bioactive constituents, mechanism of action on heart and allergenicity, it is difficult to fully comprehend the role of mushrooms as dietary interventions in alleviating hypertension and other cardiovascular malfunctions. To accomplish this endeavor, we chose to review edible mushrooms and their bioactive constituents in ameliorating hypertension. Hypertension and cardiovascular diseases are interrelated and if the former is managed by dietary changes, it is postulated that overall heart health could also be improved. With a concise note on different edible varieties of mushrooms, a particular focus is presented on the antihypertensive potential of mushroom bioactive constituents, mode of action, absorption kinetics and bioavailability. Ergosterol, lovastatin, cordycepin, tocopherols, chitosan, ergothioneine, γ-aminobutyric acid, quercetin, and eritadenine are described as essential bioactives with hypotensive effects. Finally, safety concerns on allergens and limitations of consuming edible mushrooms with special reference to chemical toxins and their postulated metabolites are highlighted. It is opined that the present review will redirect toxicologists to further investigate mushroom bioactives and allergens, thereby influencing dietary interventions for heart health.

Enzyme Inhibitory Activities of Extracts and Carpachromene from the Stem of Ficus benghalensis.

Ficus benghalensis is one of the potential medicinal plants which is used locally for the treatment of various ailments such as diabetes, antiasthmatic, and wound healing. To provide a scientific background to these folklores, the current study was designed to evaluate the extract and isolated compound against various enzymes such as ureases, tyrosinase, and phosphodiesterase. The methanolic extract and carpachromene demonstrated a significant urease inhibition effect with maximum percent inhibition of 72.09 and 92.87%, respectively. Regarding the tyrosinase inhibition, the percent antagonist effect of carpachromene and the methanolic extract was 84.80 and 70.98%, respectively. The phosphodiesterase was also significantly antagonized by crude extract and carpachromene with a maximum percent inhibition of 82.98% and 89.54%, respectively. The docking study demonstrated that the carpachromene fits well into the active site of all three enzymes with significant interactions. Carpachromene might possess the potential to inhibit all three enzymes and can effectively treat different diseases associated with the hyperactivity of these enzymes. In conclusion, the crude extract and carpachromene exhibit significant urease, tyrosinase, and phosphodiesterase inhibitory activity which might be used against various diseases. In conclusion, the crude extract and carpachromene exhibit significant urease, tyrosinase, and phosphodiesterase inhibitory activity which might be used against diabetes and bronchoconstriction. Further, the current study provides scientific backup to the folklore (antidiabetic and antiasthmatic) of Ficus benghalensis.

Natural and commercial antibiotic comparison with drugs modeling cell integrity cell stability of Bio-Kinetics changes under morphological topographies cells with lower toxicological characteristics for multidrug resistances problem.

Antibacterial drug-resistant strains are a serious problem of bacterial treatments nowadays and have a concern. The plant exacts of Adhatoda vasica and Calotropis procera are well-known for their role as antibiotic agents. The extraction of novel antibiotic compounds was done by HPLC-DAD, their yield is quantified by numerous solvents. The complete biological activity with antioxidants, bio-kinematicof four compounds of B-Sitosteryl linoleate, Myristyl diglucoside, D-Triglucopyranoside, and S- allylcysteine acids were studied. The supercritical fluid extraction techniques were the best strategies for higher yield, accuracy clarity, and inter, intra process of all four compounds. A. vasica and C. procera samples and investigated in six different solvents. D-Triglucopyranoside (13.81 ± 0.48%), Myristyl diglucoside (11.81 ± 0.41%), B- Sitosteryl linoleate (12.81 ± 0.48%), and s-allylcysteine acids (14.81 ± 0.31%) were higher. The design and action of compounds were applied to proper compartmental pharmacokinetic modelling for in-depth design understanding. The morphology and structure of bacterial cells with the extracted compounds upheld the permeability of cell membranes, membrane integrity, and membrane potential and lower the bacterial binding capacity the infectious index was measured in transmission electron microscopy (TEM) and their alteration process. Plants have well upheld the cellular permeability The toxicity test was performed on both extracted samples with concentrations (1, 0.4, and 0.8%). The areas under plasma half-life of compounds with their solubility, abortion level were higher in four compounds showed the potential of novel antibiotics. The novel medicinal plants used as antibiotics could be the best sources of infection control as a source of future medicines with antibacterial potential solving multidrug issues of bacteria in the world.

In vitro and in silico studies on clinically important enzymes inhibitory activities of flavonoids isolated from Euphorbia pulcherrima.

Introduction: The genus Euphorbia is known to contain diterpenoids, and several isolated compounds which exhibited biological activities including significant multidrug resistance reversal effects. This work is focused on the isolation, in vitro and in silico studies of two natural bio-active flavonoids (1 & 2) isolated from Euphorbia pulcherrima bark for the very first time.Methods: The phytochemical investigation resulted in the identification of two flavonoids: 3,5,7-trihydroxy-2-(4-hydroxy-3-methoxyphenyl)-6-methoxy-4H-chromen-4-one (1) and 2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-6-methoxy-4H-chromen-4-one (2), which were isolated for the first time from Euphorbia pulcherrima.Results: The chemical structures of the two isolated compounds were confirmed by 1H NMR, 13C NMR, and ESI-HRMS spectral data. The Bioactivity activity of these compounds was evaluated; results revealed that compounds 1 & 2 exhibit promising urease inhibitory potential with IC50 values of 15.3 ± 2.13 µM and 19.0 ± 2.43 µM, respectively, whereas the positive control thiourea had an IC50 of 21.0 ± 0.23 µM. Similarly, these compounds were also evaluated against the tyrosinase enzyme; results showed that compound 1 displays significant inhibitory activity with an IC50 value of 48.7 ± 2.19 µM, whereas compound 2 exhibited a moderate effect with an IC50 value of 74.8 ± 1.79 µM, when compared with the standard (alpha-kojic acid, IC50 = 47.6 ± 0.67 µM). Additionally, compounds 1 and 2 also exhibited anti-glycation and phosphodiesterase inhibitory activities.Conclusion: Studies dealing with the drug like properties such as in silico screening (docking study) was also carried out to discover the structural features of both compounds 1 and 2. Results indicated that the docking scores of compounds 1 and 2 are in agreement with their IC50 values. Key messagesIsolation and characterization of two bioactive flavonoids (1 and 2) from Euphorbia pulcherrima.In silico and in vitro enzyme inhibition studies were conducted to identify the therapeutic potential of flavonoids 1 and 2.Drug-like properties were calculated to discover important pharmacophoric features.

Garlic (Allium sativum L.): Its Chemistry, Nutritional Composition, Toxicity, and Anticancer Properties.

The current review discuss the chemistry, nutritional composition, toxicity, and biological functions of garlic and its bioactive compounds against various types of cancers via different anticancer mechanisms. Several scientific documents were found in reliable literature and searched in databases viz Science Direct, PubMed, Web of Science, Scopus, and Research Gate were carried out using keywords such as "garlic", "garlic bioactive compounds", "anticancer mechanisms of garlic", "nutritional composition of garlic", and others. Garlic contains several phytoconstituents with activities against cancer, and compounds such as diallyl trisulfide (DATS), allicin, and diallyl disulfide (DADS), diallyl sulfide (DAS), and allyl mercaptan (AM). The influence of numerous garlic- derived products, phytochemicals, and nanoformulations on the liver, oral, prostate, breast, gastric, colorectal, skin, and pancreatic cancers has been studied. Based on our search, the bioactive molecules in garlic were found to inhibit the various phases of cancer. Moreover, the compounds in this plant also abrogate the peroxidation of lipids, activity of nitric oxide synthase, epidermal growth factor (EGF) receptor, nuclear factor-kappa B (NF-κB), protein kinase C, and regulate cell cycle and survival signaling cascades. Hence, garlic and its bioactive molecules exhibit the aforementioned mechanistic actions, and thus, they could be used to inhibit the induction, development, and progression of cancer. The review describes the nutritional composition of garlic, its bioactive molecules, and nanoformulations against various types of cancers, as well as the potential for developing these agents as antitumor drugs.

Marine oil spill detection using Synthetic Aperture Radar over Indian Ocean.

Four oil spill events over the Indian Ocean including Chennai, Sharjah, Al Khiran and Mubarak Village are analyzed using Sentinel-1 satellite data. General National Oceanic and Atmospheric Administration (NOAA) Operational Modeling Environment (GNOME) model is utilized for oil spills trajectory production, whereas oil spills weathering processes are modeled using Automated Data Inquiry for Oil Spill (ADIOS). Synthetic Aperture Radar (SAR) based oil spill detection technique provided reliable results at the wind speed between 3 to 9 m/s for all events. Maximum oil spill movement (33 km) from the source point is observed in the Al Khiran, whereas evaporation rate of crude (degraded) oil is observed as high (low). The Near Real Time (NRT) detection of oil spill using SAR imagery needs high computational power, however, provides better results. This study concludes that SAR based oil spill detection is a cost-effective technique and can be utilized for mapping of oil spills.

In vivo analgesic, anti-inflammatory, and sedative activity and a molecular docking study of dinaphthodiospyrol G isolated from Diospyros lotus.

BACKGROUND: Analgesic, anti-inflammatory, and sedative drugs are available with potential side effects such as peptic ulcer and addiction among other things. In this regard, research is underway to find safe, effective, and economical drugs free of these side effects. In this study, an isolated natural product from Diospyros lotus, was tested for the aforementioned bioactivities. OBJECTIVES: To evaluate analgesic, anti-inflammatory, and sedative potential of D. lotus extracts in animal paradigms using BALB/c mice as experimental model. METHODS: Analgesic, anti-inflammatory and sedative activities of dinaphthodiospyrol G (1) isolated from the chloroform fraction of D. lotus were evaluated using different experimental procedures. Anti-inflammatory effect was evaluated using the carrageenan and histamine-induced paw edema, whereas the antinociceptive effect was quantified by means of the hot plate analgesiometer. On the other hand, the sedative effect was determined using animal assay for screening the locomotors effects of compound 1. Compound 1 was also subjected to molecular modeling studies against cyclooxygenase enzymes. RESULTS: Results from this investigation showed that the extract is devoid of anti-inflammatory and antinociceptive potentials but has a significant sedative effect, whereas the tested compound exhibited 55.23 and 78.34% attenuation in paw edema by carrageenan and histamine assays, respectively. A significant (p < 0.001) and dose-dependent antinociceptive and sedative effects were demonstrated by the isolated compound. Molecular docking and dynamics simulation studies of the isolated compound against cyclooxygenase enzyme indicated that compound 1 forms specific interactions with key residues in the active site of the target receptor, which validates the potential use of the isolated compound as cyclooxygenase inhibitor. CONCLUSIONS: Compound 1 exhibited remarkable analgesic, anti-inflammatory, and sedative activities. These findings strongly justify the traditional use of D. lotus in the treatment of inflammation, pain, and insomnia.

Chrysin: Pharmacological and therapeutic properties.

Chrysin is a promising phytochemical that is categorized under the class of flavonoids based on its chemical structure. Naturally, it is widely present in propolis, honey, passion fruit, and even in mushrooms and other plant sources, whereas its synthetic counterparts are also being employed for pharmacological purposes. It has widely been employed in treatment of various degenerative disorders and provides cytotoxic and anti-inflammatory functions. Its antioxidant and disease preventing abilities are attributed to its structural diversity arising in ring-A and absence of oxygenation in B and C ring. In this review, the scientific studies are being reported emphasizing benefits and its allied health claims on chrysin in numerous metabolic malfunctions.

Proanthocyanidins: A comprehensive review.

Proanthocyanidins are condensed tannins with various pharmacological properties. These phytochemicals are considered as 'offense and defense molecules because of their human health benefits. The validation of their diverse health aspects, namely, antioxidant, anticancer, antidiabetic, neuroprotective, and antimicrobial has earned them repute in thermochemistry. Proanthocyanidins are oligo- or polymers of monomeric flavan-3-ols produced as an end product of flavonoid biosynthetic pathway. Agricultural wastes and food processing wastes contain immense amount of proanthocyanidins, exploitation of which can be a sustainable source of dietary supplements and functional ingredients. The current review article discusses recent developments in the health promoting properties of proanthocyanidins and the associated hurdles.

Vitex negundo induces an anticonvulsant effect by inhibiting voltage gated sodium channels in murine Neuro 2A cell line.

Vitex negundo (Vn) extract is famous for the treatment of neurological diseases such as migraine and epilepsy. These neurological diseases have been associated with abnormally increased influx of sodium ions into the neurons. Drugs that inhibit voltage gated sodium channels can be used as potent anti-epileptics. Till now, the effects of Vn on sodium channels have not been investigated. Therefore, we have investigated the effects of methalonic fraction of Vn extract in Murine Neuro 2A cell line. Cells were cultured in a defined medium with or without the Vn extract (100 µg/ml). Sodium currents were recorded using whole-cell patch clamp method. The data show that methanolic extract of Vn inhibited sodium currents in a dose dependent manner (IC50 =161µg/ml). Vn (100 µg/ml) shifted the steady-state inactivation curve to the left or towards the hyper polarization state. However, Vn did not show any effects on outward rectifying potassium currents. Moreover, Vn (100 µg/ml) significantly reduced the sustained repetitive (48±4.8%, P<0.01) firing from neonatal hippocampal neurons at 12 DIV. Hence, our data suggested that inhibition of sodium channels by Vn may exert pharmacological effects in reducing pain and convulsions.

Anaemia: the neglected female health problem in developing countries.

BACKGROUND: Anaemia is arguably the biggest female health problems in developing countries. The world is still to fully fathom the extent and gravity of the problem. This problem aggravates particularly during and after pregnancies due to increased nutritional demands and inadequate iron supply and is therefore more widespread in parous segments of female population. Objective of this study was to determine prevalence of anaemia in apparently healthy parous female population of Abbottabad and investigate underlying causes. METHODS: This descriptive, cross-sectional study was conducted from October 2001 to March 2011 in Abbottabad. Women reporting for various surgical procedures were investigated for anaemia by obtaining history through a structured performa, specifically designed to identify the underlying causes. Sixteen thousand women of childbearing age (20-40 years) were included in the study; 14,800 with history of at least one pregnancy and remaining with no previous pregnancy. Haemoglobin (Hb) was measured using haematology analyser Sysmex (KX21). RESULTS: Of the screened women, 60% were found anaemic (Hb < 12 g/dl) 10% of which were severely anaemic (Hb < 6 g/dl). Anaemia was related to socio-demographic and obstetric history characteristics. The prevalence of anaemia was significantly lower in women who used iron supplements during their pregnancies. Lactating mothers not making up for the iron deficiencies during pregnancies usually carried their anaemia postpartum and beyond. Lower gaps between pregnancies also contributed significantly to the problem. CONCLUSION: Prevalence and severity of anaemia in reproductive age females reporting to surgical units were found to be exceptionally high. Frequency of anaemia in the parous females of relatively affluent city of Abbotabad indicates that anaemia may be on the rise in developing countries. Addressing pregnancy related anaemia and nutritional deficiencies through intake of supplements on regular basis in women before and between pregnancies is essential.