Goniothalamus Species: A Source of Drugs for the Treatment of Cancers and Bacterial Infections?

Irrespective of the presence of cytotoxic acetogenins and styryl-lactones in the genus Goniothalamus, only 22 species in the genus Goniothalamus, out of 160 species (13.7%) have so far been investigated. In an effort to promote further research on the genus Goniothalamus which could represent a source of drugs for the treatment of cancers and bacterial infections, this work offers a broad analysis of current knowledge on Goniothalamus species. Therefore, it includes (i) taxonomy (ii) botanical description (iii) traditional medicinal uses and (iv) phytochemical and pharmacological studies. We discuss the molecular mechanisms of actions of acetogenins and styryl-lactones, with some emphasis on the possible involvement of protein kinase, Bax and TRAIL receptors in the cytotoxic effects of styryl-lactones. We also report (v) the growth inhibition of several nosocomial bacteria by Goniothalamus. scortechinii. The crude methanol extract of G. scortechinii showed a good and broad spectrum of antibacterial activity against both Gram-negative and Gram-positive bacteria

Antibicrobial and cytotoxic compounds of Scorodocarpus borneensis (Olacaceae) and Glycosmis calcicola (Rutaceae)

The extracts of plants collected from the forest of Northern Malay Peninsula were tested against bacteria, fungi and CEM-SS leukemia cel1 line. Gram-positive Bacillus cereus and Gram-negative Pseudomonas aeruginosa which are commonly involved in skin infections, have been used for screening antibacterial activity whereas Candida lipolytica, Saccharomyces cerevisae, Saccharomyces lipolytica, and Aspergillus ochraceous have been used for screening antifungal activity. The crude extract from the seeds of Scorodocarpus bomeensis showed a strong cytotoxic activity against CEM-SS leukemia cell-line and antimicrobial activities. A bioassay-guided separation had been carried out to separate the active constituents of the seeds. This resulted in the isolation and identification of an aliphatic sulfur compound, bis-(methylthiomethyl)disulfide, and a new indole alkalOld, 13-docosenoyl serotonme from the petroleum ether extract A new sesquiterpene, scopotin, has been isolated from the chloroform extract of the seeds Another sesquiterpene, cadalene-p-carboxyhc acid, has been isolated from the bark of this species bis-(Methyithiomethyl)-disulfide appeared as the most active compound and the major constttuent of the seeds extract of Scorodocarpus borneensis it acted significantly on a methicillin resistant strain of Staphylococcus aureus and showed a strong Cytotoxic activity against CEM-SS leukemia and KU812F chronic myelogenous leukemia cell lines 13-Docosenoyl serotonme showed a moderate Cytotoxic activity against CEM-SS leukemia cell line Scopotin showed a moderate antimicrobial activity and a strong Cytotixic effect against CEM-SS leukemia cell line The crude petroleum ether extract and bis-(methyithtomethyl)disulfide strongly inhibited the growth of pathogen fungi and was formulated m external preparation by usmg commercial paraffin as exipient. This preparation exhibited drastic antifungal activities in vitro and in VIVO The acute toxicity of the crude petroleum ether extract was found to be inferior to phenobarbital in mice with LD50 at 275 mg/kg The skin irritancy test was performed on rabbits and it showed that this preparatlOn had an irritancy level acceptable by the FDA. Antimicrobial and cytotoxic activities were also performed on methylgerambullin and desmethoxyzanthophylline which were previously isolated from Glycosmis calcicola (Rutaceae). Methylgerambullin showed a strong cytotoxic activity against CEM-SS leukemia, melanoma HACCl, and colon cancer HT29 cell lines whereas desmethoxyzanthophylline has moderate activity against Bacillus cereus, Pseudomonas aeruginosa and CEM-SS leukemia cell line

PHYTOCHEMICAL SCREENING OF ARTABOTRYS CRASSIFOLIUS HOOK.F. & THOMSON (ANNONACEAE JUSS.)

Objective: The aim of the present study was to determine the phytochemical constituents of Artabotrys crassifolius.   Methods: The leaves and barks of Artabotrys crassifolius were extracted sequentially with hexane, chloroform and ethanol. The corresponding crude extracts obtained were then subjected to phytochemical screening.   Results: The phytochemical analysis of crude extracts of Artabotrys crassifolius demonstrated the presence of alkaloids, cardiac glycosides, flavonoids, phenolic compounds, saponins and terpenoids.   Conclusion: The chemical profile of these crude extracts can serve as a useful reference for further investigations in pharmacological activities of Artabotrys crassifolius. Keywords Phytochemical analysis, Artabotrys crassifolius, Annonacea

Modeling and characterization of the uplink and downlink exposure in wireless networks

This paper deals with a new methodology to assess the exposure induced by both uplink and downlink of a cellular network using 3D electromagnetic simulations. It aims to analyze together the exposure induced by a personal device (uplink exposure) and that induced by a base station (downlink exposure). The study involved the major parameters contributing to variability and uncertainty in exposure assessment, such as the user's posture, the type of wireless device, and the propagation environment. Our approach is relying basically on the modeling of the power radiated by the personal device and the ambient electric field, while taking into account the effects of human body shadowing and the propagation channel fluctuations. The exposure assessment as well as the human-wave interactions has been simulated using the finite difference in time domain method (FDTD). In uplink scenarios, four FDTD simulations were performed with a child model, used in two postures (sitting and standing) and in two usage scenarios (voice and data), which aimed to examine the exposure induced by a mobile phone and a tablet emitting, respectively, at 900 MHz and 1940 MHz. In the downlink scenario, a series of FDTD simulations of an exposure to a single plane wave and multiplane waves have been conducted, and an efficient metamodeling of the exposure using the Polynomial Chaos approach has been developed

In vivo MRI assessment of permanent middle cerebral artery occlusion by electrocoagulation: pitfalls of procedure

Permanent middle cerebral artery (MCA) occlusion (pMCAO) by electrocoagulation is a commonly used model but with potential traumatic lesions. Early MRI monitoring may assess pMCAO for non-specific brain damage. The surgical steps of pMCAO were evaluated for traumatic cerebral injury in 22 Swiss mice using diffusion and T2-weighted MRI (7T) performed within 1 h and 24 h after surgery. Temporal muscle cauterization without MCA occlusion produced an early T2 hyperintensity mimicking an infarct. No lesion was visible after temporal muscle incision or craniotomy. Early MRI monitoring is useful to identify non-specific brain injury that could hamper neuroprotective drugs assessment

Acalypha wilkesiana extracts induce apoptosis by causing single strand and double strand DNA breaks

Ethnopharmacological relevance: The seeds of Acalypha wilkesiana have been used empirically by traditional healers in Southwest Nigeria together with other plants as a powder mixture to treat patients with breast tumours and inflammation. Aim of the study: There is an increasing interest among researchers in searching for new anticancer drugs from natural resources, particularly plants. This study aimed to investigate the anticancer properties of Acalypha wilkesiana extracts and the characteristics of DNA damage against brain and lung cancer cells. Materials and methods: The antiproliferative activity of Acalypha wilkesiana extracts (ethyl acetate, hexane, and ethanol) was examined on human glioma (U87MG), human lung carcinoma (A549), and human lung fibroblast (MRC5) cells. Results: Cell viability MTT assay revealed that ethyl acetate extract of the plant possessed significant antiproliferative effects against both U87MG (GI50 = 28.03 ± 6.44 μg/ml) and A549 (GI50 = 89.63 ± 2.12 μg/ml) cells (p value 300 μg/ml). The ethanol extract showed no antiproliferative effects on any cell line examined. Haematoxylin & Eosin (H & E) staining and single cell gel electrophoresis (SCGE) comet assay confirmed that plant extract-treated cells underwent apoptosis and not necrosis. SCGE comet assays confirmed that plant extracts caused both single strand (SSB) and double strand (DSB) DNA breaks that led to the execution of apoptosis. Conclusion: The extracts (especially ethyl acetate and hexane) of Acalypha wilkesiana possess valuable cytotoxic effects that trigger apoptosis in U87MG and A549 cancer cells through induction of DNA SSBs and DSBs

IN VITRO ANTICANCER EFFECT OF ARTABOTRYS CRASSIFOLIUS HOOK.F. & THOMSON AGAINST HUMAN CARCINOMA CELL LINES

The aim of the present study was to investigate the anticancer effects of crude extracts of Artabotrys crassifolius on the growth of human breast and colorectal carcinoma cell lines. The leaves and barks of Artabotrys crassifolius were extracted sequentially with hexane, chloroform and ethanol. The corresponding crude extracts obtained were then tested for their anticancer activity using MTT assay. Among the extracts studied, chloroform and hexane extracts of barks were found to possess the most potent anticancer activity which necessitates further isolation and characterisation of the bioactive compounds present in the respective extracts. Keywords: Anticancer, Artabotrys crassifolius, Human carcinoma cell line

Crude Ethanol Extract of Pithecellobium ellipticum

If left untreated, hypercholesterolaemia can lead to atherosclerosis, given time. Plants from the Fabaceae family have shown the ability to significantly suppress atherosclerosis progression. We selected four extracts from Pithecellobium ellipticum, from the Fabaceae family, to be screened in a 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) assay. The ethanol extract, at a concentration of 500 μg/mL, exhibited superior inhibition properties over the other extracts by demonstrating 80.9% inhibition, while 0.223 μg/mL of pravastatin (control) showed 78.1% inhibition towards enzymatic activity. These findings led to the fractionation of the ethanol extract using ethyl acetate : methanol (95 : 5), gradually increasing polarity and produced seven fractions (1A to 7A). Fraction 7A at 150 μg/mL emerged as being the most promising bioactive fraction with 78.7% inhibition. FRAP, beta carotene, and DPPH assays supported the findings from the ethanol extract as it exhibited good overall antioxidant activity. The antioxidant properties have been said to reduce free radicals that are able to oxidize lipoproteins which are the cause of atherosclerosis. Phytochemical screenings revealed the presence of terpenoid, steroid, flavonoid, and phenolic compounds as the responsible group of compound(s), working individually or synergistically, within the extract to prevent binding of HMG-CoA to HMG-CoA reductase

Evaluation of phytochemicals and antioxidant potential of a new polyherbal formulation TC-16: additive, synergistic or antagonistic?

Background Scientific literature has demonstrated the association of free radicals in the etiology of various chronic diseases. Hence, the identification of potent antioxidants remains a useful task. The combination of multiple herbs in polyherbal formulations (PHF) is often associated with greater therapeutic efficacy due to synergistic interactions. However, antagonism can occur in natural product mixtures and the resultant antioxidant potential might not always be the additive value of the antioxidant properties of each component. In this study, we aimed to evaluate the phytochemicals, antioxidative potential and interaction among the herbs in TC-16, a new PHF comprising Curcuma longa L., Zingiber officinal var. Bentong, Piper nigrum L., Citrofortunella microcarpa (Bunge) Wijnands and Apis dorsata honey. Methods TC-16 was screened for phytochemicals. Phenolic and flavonoid contents of TC-16 and its individual ingredients were determined, followed by assessment of antioxidant properties using in vitro assays including 2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonate) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC) and β-carotene bleaching (BCB) assays. Interactions among the herbs were also investigated by calculating the difference in antioxidant activity and combination index. Results Alkaloids, flavonoids, terpenoids, saponins and glycosides were present in TC-16. TC-16 possessed the highest phenolic (46.14±1.40 mg GAE/g) and flavonoid (132.69±1.43 mg CE/g) contents following C. longa. Synergistic antioxidant activity among the herbs was evident in ORAC and BCB assays which uses mainly hydrogen atom transfer-based antioxidant mechanisms. Conclusions TC-16 demonstrated roles in combating free radicals. In a PHF, synergistic interaction among the herbs is observed in some but not all mechanisms. Mechanisms showing synergistic interactions should be highlighted to maximize the beneficial property of the PHF

Characterization of far-field and near-field exposure of the population for RF-EMF in realistic configurations of ICT usages

International audienceThe study presented in this paper is part of a larger study within the European FP7 project LEXNET framework. The project LEXNET aims at considering new technologies and architectures for minimizing the global exposure of a population to radiofrequency electromagnetic fields. In the framework of the project a new exposure metric named Exposure Index (EI) is proposed. The EI quantifies the global exposure of a population induced by both mobile devices and base station antennas or wireless access points. The EI requires a set of SAR values (whole-body and local-body) for typical postures and usages of mobile devices in a population. In our study, we assessed these SAR values by 3D electromagnetic simulations. We used an adult and a child numerical model in two postures (sitting and standing) and in three usages (voice, data and laptop).The whole-body SAR for each exposure configuration was evaluated at four different frequencies (400, 900, 1940 and 2600MHz).</p