Despite the existence of an extended armamentarium of effective synthetic drugs to treat HIV, there is a continuing need for new potent and affordable drugs. Given the successful history of natural product based drug discovery, a library of close to one thousand plant and fungal extracts was screened for antiretroviral activity. A dichloromethane extract of the aerial parts of Daphne gnidium exhibited strong antiretroviral activity and absence of cytotoxicity. With the aid of HPLC-based activity profiling, the antiviral activity could be tracked to four daphnane derivatives, namely, daphnetoxin (1), gnidicin (2), gniditrin (3), and excoecariatoxin (4). Detailed anti-HIV profiling revealed that the pure compounds were active against multidrug-resistant viruses irrespective of their cellular tropism. Mode of action studies that narrowed the site of activity to viral entry events suggested a direct interference with the expression of the two main HIV co-receptors, CCR5 and CXCR4, at the cell surface by daphnetoxin (1).

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Seven free-radical-scavenging phenolic compounds including five flavonoids, rutin (1), chrysoeriol 7-O-rutinoside (2), kaempferol 3-O-glucoside (3), chrysoeriol 7-O-glucoside (4) and naringenin (5), and two phenylethanoid glycosides, forsythoside B (6) and acteoside (7) were isolated from the methanol extract of the aerial parts of the Iranian medicinal plant Phlomis caucasica by reversed-phase preparative high-performance liquid chromatography (HPLC), and the structures of these compounds were elucidated by spectroscopic means. The free-radical-scavenging properties of 1-7 were assessed by 2,2-diphenyl-1-picryl hydrazyl (DPPH) assay. Among these compounds, forsythoside B (6) and acteoside (7) were found to be the most potent antioxidants with the RC(50) values of 4.97 and 4.27 microg/ml, respectively.

Ten extracts with different polarity from two Iranian Artemisia species, A. armeniaca Lam. and A. aucheri Boiss, were screened for their antimalarial properties by in vitro   β-hematin formation assay. Dichloromethane (DCM) extracts of both plants showed significant antimalarial activities with IC50 values of 1.36 ± 0.01 and 1.83 ± 0.03 mg/mL and IC90 values of 2.12 ± 0.04 and 2.62 ± 0.09 mg/mL for A. armeniaca and A. aucheri, respectively. Bioactivity-guided fractionation of DCM extracts of both plants by vacuum liquid chromatography (VLC) over silica gel with solvent mixtures of increasing polarities afforded seven fractions. Two fractions from DCM extract of A. armeniaca and four fractions from DCM extract of A. aucheri showed potent antimalarial activity with reducing IC50 and IC90 values compared to extracts. The most potent fraction belonged to DCM extract of A. armeniaca with IC50 and IC90 values of 0.47 ± 0.006 and 0.71 ± 0.006 mg/mL, respectively.

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Isofraxidin (7-hydroxy-6, 8-dimethoxy coumarin) (IF) is a hydroxy coumarin with several biological and pharmacological activities. The plant kingdom is of the most prominent sources of IF, which, among them, Eleutherococcus and Fraxinus are the well-known genera in which IF could be isolated/extracted from their species. Considering the complex pathophysiological mechanisms behind some diseases (e.g., cancer, neurodegenerative diseases, and heart diseases), introducing IF as a potent multi-target agent, which possesses several herbal sources and the multiple methods for isolation/purification/synthesis, along with the unique pharmacokinetic profile and low levels of side effects, could be of great importance. Accordingly, a comprehensive review was done without time limitations until February 2020. IF extraction methods include microwave, mechanochemical, and ultrasound, along with other conventional methods in the presence of semi-polar solvents such as ethyl acetate (EtOAc). In addition to the isolation methods, related synthesis protocols of IF is also of great importance. From the synthesis point of view, benzaldehyde derivatives are widely used as precursors for IF synthesis. Along with the methods of isolation and biosynthesis, IF pharmacokinetic studies showed hopeful in vivo results of its rapid absorption after oral uses, leading to different pharmacological effects. In this regard, IF targets varieties of inflammatory mediators including nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), tumor necrosis factor-α (TNF-α), and matrix metalloproteinases (MMPs). thereby indicating anticancer, cardioprotective, and neuroprotective effects. This is the first review on the synthesis, biosynthesis, isolation, and pharmacokinetic and pharmacological properties of IF in combating different diseases.

Asian Pac J Cancer Prev, 15 (17), [7055][7056][7057][7058][7059] IntroductionIncrease in prevalence of cancer cases has been associated with the expansion of industrial, chemical and radioactive pollutants, also the gap between human being and nature (Colditz and Wei, 2012; Fasinu and Orisakwe, 2013). Despite the progress in the field of medicinal chemistry and development in the synthesis of several new therapeutic compounds, the role of plants and phytochemicals can not be ignored in pharmaceutical sciences (Cerella et al., 2014). Due to the presence of compounds with cytotoxic and anti-tumor activity in some plants and significant efficacy of plant derived compounds in inhibition and treatment of cancer, as well as the amazing diversity of natural compounds in plants, researches to find new phytochemicals and to evaluate their biological effects is essential and a research priority (Tayarani-Najaran et al., 2011;Wegiera et al., 2012;Sehitoglu et al., 2014).Artemisia is a genus belonging to the family Asteraceae Compositae with commonly fragrant species. Some species such as A. dracunculus L. are kitchen plants and used for

Phytochemical analysis of the Iranian plant Achillea wilhelmsii led to the isolation of 17 pure secondary metabolites belonging to the classes of sesquiterpenoids and phenolics. Two of these compounds, named wilhemsin (7) and wilhelmsolide (9), are new sesquiterpenoids, and the first shows undescribed structural features. Their structures were elucidated through extensive spectroscopic analysis, mainly based on 1D and 2D NMR, and chemical derivatization. Starting from plant traditional use and previous reports on the activity of the plant extracts, all the pure compounds were evaluated on endpoints related to the treatment of metabolic syndrome. The sesquiterpene hanphyllin (8) showed a selective cholesterol-lowering activity (−12.7% at 30 µM), santoflavone (13) stimulated glucose uptake via the GLUT transporter (+16.2% at 30 µM), while the trimethoxylated flavone salvigenin (14) showed a dual activity in decreasing lipid levels (−22.5% palmitic acid biosynthesis at 30 µM) and stimulating mitochondrial functionality (+15.4% at 30 µM). This study further confirms that, in addition to the antioxidants vitexin, isovitexin, and isoschaftoside, A. wilhelmsii extracts contain molecules that can act at different levels on the metabolic syndrome symptoms.