Immunomodulatory activity of a lupane triterpenoid ester isolated from the eastern Nigeria mistletoe, Loranthus micranthus (Linn)

OBJECTIVE@#To provide further evidence for the ethnomedicinal use of the Eastern Nigeria mistletoe, Loranthus micranthus (L. micranthus), as an immunostimulant.@*METHODS@#Solvent fractions from the crude extract of the mistletoe plant was obtained and screened by the cell mediated delayed type hypersensitivity reaction (DTHR) model in mice. Then the immunomodulatory potentials of a major lupane triterpenoid ester isolated from an active hexane fraction of the Eastern Nigeria mistletoe was investigated. Three lupeol-based triterpenoid esters: 7β 15α-dihydroxyl-lup-20(29)-ene-3β-palmitate (I), 7β, 15α-dihydroxyl-lup-20(29)-ene-3β-stearate (II) and 7β, 15α-dihydroxyl-lup-20(29)-ene-3β-decadecanoate (III) were isolated from the plant leaves epiphyting on a local kola nut tree and were characterized. Compound 1 was subjected to cell proliferation studies using C57Bl/6 splenocytes at three dose levels (5, 25 and 100 μg/mL) in presence of controls. Furthermore, the effect of this compound on IL-8 receptor expression was evaluated at three doses (1, 5 and 10 μg/mL) using the real time polymerase chain reaction assay.@*RESULTS@#This triterpenoid ester produced some enhancement of the splenocytes at the tested doses but at doses higher than 5 μg/mL caused inhibition of the IL-8 receptor expression.@*CONCLUSIONS@#The present findings support the ethnomedicinal use of the Eastern Nigeria Mistletoe in the management of diseases affecting the immune system. The triterpenoid(s) have some immunomodulatory abilities on splenocytes and IL-8 receptors and may partly account for the overall immunomodulatory activity of this plant.

Rapid response to lipids profile and leukocyte gene expression after rosuvastatin administration in Chinese healthy volunteers / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>Statins are potent lipid-lowering agents widely used in medical practice. There has been growing evidence suggesting the pleiotropic effects of statins in addition to the lipid-lowering effect. However, it is still unclear how rapidly the beneficial effects of statins occur. The transcriptome of peripheral blood cells can be used as a sensor to drug therapy. The purpose of the study was to investigate the acute effects of rosuvastatin both on lipids profile and gene expression of peripheral leukocytes following therapy with a single dose of rosuvastatin.</p><p><b>METHODS</b>Thirty healthy Chinese male volunteers were enrolled. The serum lipids, high-sensitivity C-reactive protein, and plasma fibrinogen were determined before and 72 hours after administration of 20 mg of rosuvastatin. The differentially expressed genes of peripheral leukocytes after administration of rosuvastatin were screened using human oligonucleotide microarray gene expression chips. Then four of the differentially expressed genes including ATM, CASP8, IL8RB and S100B were verified by real-time polymerase chain reaction (PCR).</p><p><b>RESULTS</b>Rosuvastatin decreased both serum total cholesterol and low-density lipoprotein cholesterol significantly 72 hours after administration of a single dose of 20 mg rosuvastatin. However, no significant changes occurred in blood high-density lipoprotein cholesterol, triglycerides, C-reactive protein and fibrinogen after the treatment. A total of 24 genes were differentially expressed after the treatment. They were involved in important cell biological processes such as cytokine-cytokine receptor interaction, apoptosis signaling, etc.</p><p><b>CONCLUSIONS</b>Rosuvastatin rapidly modulates the serum lipids and affects the gene expression of peripheral leukocytes in healthy volunteers. This finding provides some new clues for further studies on its potential pleiotropic effects.</p>