Natural Products Journal, The - Volume 6, Issue 4, 2016

Phosphatidylcholine (PC) is an essential part of human cell membranes and an important dietary source of choline, an important biochemical. Its common name is lecithin. It can be made from phosphatidylethanolamine (PE) by methylation of the ethanolamine moiety in a reaction catalyzed by phosphatidylethanolamine N-methyltransferase. There is a decrease in phosphatidylethanolamine (PE) and ether-linked PC concentrations, as well as an increase in lysophosphatidylethanolamine during chronic stress. PC and choline are important for healthy brains, hearts, skeletal muscles, livers and metabolism. For example, Alzheimer’s disease patients have lower concentrations of three different PCs in their blood serum than healthy control subjects. Choline is important in maintaining cell structure and synthesizing the neurotransmitter acetylcholine. Choline supplementation during critical periods of neonatal development can have long-term beneficial effects on memory. A lack of sufficient dietary choline can cause signs of subclinical organ dysfunction (fatty liver or muscle damage). The need for choline is especially high during pregnancy and lactation. If there is insufficient choline stored in the body, the ability to methylate homocysteine to make methionine decreases, and plasma concentrations of homocysteine increase. This can increase the risk for cardiovascular disease, cancer, cognitive decline and bone fractures. On the other hand, over-consumption of red meat and other dietary sources of PC can lead to the production of trimethylamine oxide (TMAO) by gut bacteria. TMAO is both a kidney toxin and a biomarker for kidney diseases. So, PC and choline must be present in sufficient concentrations to support life, but not be too high to be toxic. Moreover, not everybody is equally susceptible to TMAO toxicity. People who have a kidney disease or are highly susceptible to cardiovascular disease may want to restrict their consumption of red meat and egg yolks, as well as avoid lecithin dietary supplements. Still, vegetarians who don’t eat egg yolks may want to take such supplements. On the other hand, another supplement called citicoline (cytidine diphosphocholine, CDP-choline) may be a better option since it is not metabolized into TMAO and may help brain function. Citicoline supplementation may improve memory, including verbal memory in patients with age related cognitive impairment, as well as improving cognitive function in elderly patients with vascular related mild cognitive impairment.

Brain ischemia-reperfusion injury is a complex pathological condition that involves a cascade of events like excitotoxicity, peri-infarct depolarization, oxidative/nitrosative stress, inflammation, apoptosis, necrosis and autophagic degeneration. Since the past decades, researchers have provided significant information about the therapeutic potential and possible mechanism of action of plant extracts and derived chemicals to target multiple pathways of the ischemic cascade. Here, we summarized experimental, clinical and epidemiological therapeutic interventions of plants extracts and phytochemicals against brain ischemia-reperfusion injury. Whether oxidative stress is the cause or consequence of brain ischemia is open for debate but details about oxidative burden and inflammation following brain ischemia are also described. Furthermore, the antioxidant mechanism of these extracts/ phytochemicals was reviewed. Although these plant extracts and phytochemicals showed the ability to act on the multiple steps of the ischemic cascade in in vitro and in vivo models of brain ischemia, further investigations are needed for their validation and for the development of new drugs.

Background: Echium amoenum Fisch. (Boraginaceae) and C.A. Mey. (Iranian Borage or Gol-gavzaban) is traditionally applied as a general tonic, cardiotonic, diaphoretic, diuretic, tranquillizer, and anti-cough in Iran. Despite numerous investigations and continual administrations of E. amoenum by traditional healers, no specific review of this plant has previously been done. Objective: The current study aimed to present a critical overview of the phytochemistry and pharmacology of this plant to outline a possible scope for further investigations. Methods: An extensive search was performed through various databases such as PubMed, Scopus, ScienceDirect, and Google Scholar. The exact term “Echium amoenum” was searched, and papers related to the phytochemical and pharmacological properties of this plant were gathered. Papers focusing on agriculture and genetics were excluded. Data gathering was completed by May 1, 2015. Results: The derived papers dealt mostly with the pharmacological activities of the plant, such as its analgesic, antiviral, antimicrobial, anticonvulsant, anxiolytic, antioxidant, immunomodulatory, antidepressant, and anti-obsessive-compulsive effects. Some papers focused on phytochemicals, determining its fatty acid profile, phenolic compounds, volatile constituents, phytosterols, and total alkaloids. There is some controversy over certain of its antibacterial effects. From all pharmacological evaluations, only antidepressant, antioxidant, and anxiolytic properties have been studied both experimentally and clinically. Conclusion: Many clinical properties originating from traditional knowledge remain to be evaluated by current knowledge. Although the herb in question in this paper did not demonstrate mutagenic activities in usual doses, the presence of pyrrolizidine alkaloids may be a factor in hepatotoxicity. Therefore, E. amoenum must be administered conservatively.

Background: Hepatitis B virus claims approximately 780000 human lives each year. Inadequate effectiveness and drug resistance has led to the search for more potent antivirals with minimal risk of resistance. Plant extract from Phyllanthus genus have long been used in traditional medicine as effective antiviral and hepatoprotective agents. Objective: The present study aims to find the active principle of Phyllanthus and their mode of action against Hepatitis B Virus Reverse Transcriptase (HBV RT), a potential drug target of HBV infection. Methods: The 3D structure of HBV RT was modeled and its stability was assessed with a 50ns molecular dynamics simulation. Ninety-three phytochemicals were screened from Phyllanthus and used for docking study taking lamivudine as control drug. Results: Comparison of binding energy suggests that, lupeol acetate, a triterpene of P. niruri, P. reticulatus and P. urinaria showed highest binding energy for both native and M204V mutated HBV RT (-7.95 kcal/mol & -6.16 kcal/mol respectively) than the control drug lamivudine (-4.57 kcal/mol & -3.50 kcal/mol respectively). Subsequently, lupeol acetate was screened for in silico ADME/Tox property and result indicates good bioavailability without toxicity and can be treated as a candidate drug molecule. Conclusion: Further clinical testing may lead to the discovery of a novel HBV RT inhibitor.

Background: Boswellia serrata Roxb. is used in folklore medicine for the treatment of inflammation, arthritis and ulcerative colitis. Objective: The aim of this study was to evaluate the anti-ulcerogenic properties of ethanol extract of gum resin of Boswellia serrata extract and it’s microcapsule formulation. Methods: Microcapsules of Boswellia serrata extract were prepared by ionic gelation technique and evaluated. The Fourier Transform Infrared Spectroscopy (FT-IR) and Differential Scanning Colorimeter (DSC) study was performed for compatibility study. M1, M2 and M3 formulations were tested for anti-ulcerative colitis activity by inducing acetic acid in mice. Anti-ulcerative colitis property was evaluated by weight of colon tissue, lesion score, myeloperoxidase level, malondialdehyde level and histopathology. Results: The average particle sizes of microcapsules were 303.2±0.901, 330.13±1.235 and 368.80μm±6.048 for formulation M1, M2 and M3, respectively. Entrapment efficiency of microcapsules was 51.37, 60.45 and 76.60% for formulation M1, M2 and M3, respectively. Scanning Electron Microscopy (SEM) study revealed that the microcapsules were almost spherical, discrete and covered with sodium alginate coat material. Microcapsules formulations showed better reduction of ulceration in acetic acid induced mice. Histopathalogically, M3 formulation and standard drug prednisolone showed very small pathological score that was evident by less ulceration, hemorrhages, necrosis and leukocyte infiltration. Conclusion: Boswellia serrata extract and microcapsule formulations were shown to decrease the ulcerative colitis induced by acetic acid. The microcapsule formulation may be used to treat the ulcerative colitis.

Background: Quantitative and qualitative changes in the plant chemical profiles due to stress-induced response may alter the biological activity of plant tissues. In the current study, we tested the hypothesis that biologic potential against microorganisms of essential oils obtained from Piper marginatum leaves may be affected by herbivore or mechanical injury. Methods: The chemical compositions of the essential oils were determined by GC/MS while antimicrobial activity was determined by disc diffusion method and minimum inhibitory concentration assay. Results: The chemical profile of leaf essential oil of P. marginatum underwent alterations when infested with the grasshopper Xyleus discoideus. The antimicrobial activity of leaf essential oil infested by grasshopper decreased against the microorganisms Bacillus subtilis and Mycobacterium smegmatis, and oil was inactive against the fungus Malassezia furfur. Additionally, the essential oil obtained of P. marginatum leaves subjected to the mechanical damage showed chemical change compared to the oil from the intact leaves but did not cause alterations in the antimicrobial activity of oil. Conclusion: The overall results of this study reveal that P. marginatum leaves respond very clearly to the damages caused by attack by the grasshopper X. discoideus and mechanical damage.