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Cardiac glycosides (CGs) are bioactive compounds originally used to treat heart diseases, but recent studies have demonstrated their anticancer activity. We previously demonstrated that Antiaris toxicaria 2 (AT2) possesses anticancer activity in KRAS mutated lung cancers via impinging on the DNA damage response (DDR) pathway. Toward developing this class of molecules for cancer therapy, herein we report a multistep synthetic route utilizing k-strophanthidin as the initial building block for determination of structure-activity relationships (SARs). A systematic structural design approach was applied that included modifications of the sugar moiety, the glycoside linker, stereochemistry, and lactone ring substitutions to generate a library of O-glycosides and MeON-neoglycosides derivatives. These molecules were screened for their anticancer activities and their impact on DDR signaling in KRAS mutant lung cancer cells. These results demonstrate the ability to chemically synthesize CG derivatives and define the SARs to optimize AT2 as a cancer therapeutic.

The study investigated the use of thermal modification to improve the hygroscopic properties of False Iroko [Antiaris toxicaria (Lesch)]. Samples of Antiaris toxicara Lesch wood were subjected to thermal modification in a furnace at temperatures of 160, 180 and 200°C for 30 and 60 minutes. Results showed that wood properties were improved with exposure to different temperatures. Subsequent to the thermal process, a colour change from pale yellow to darkish brown was observed progressively with increase in temperature, accompanied by a weight loss in the range of 12.08% to 23.67%. The outcome of these treatments resulted in a decrease in volumetric swelling and increase in dimensional stability of modified wood; this can be attributed to observed decrease in moisture intake. The thermal modification of Antiaris toxicara Lesch wood affected the dimensional stability properties. Thus, due to significant changes via modification carried out on the selected species which is classified as lesser utilized wood species, lesser utilized wood,Antiaristoxicara Lesch wood is recommended for use due to its efficient dimensional stability after modification . keywords:, Thermally modified wood ;False Iroko

Investigations were carried out on the effect of growth ring width, fiber morphometrics, and wood type on the compressive strength of three members of the Moraceae family namely; Milicia excelsa , Treculia africana , and Antiaris toxicaria . Fiber diameter ( D ), Fiber length ( L ), fiber lumen diameter ( l) , cell wall thickness ( c ), derived fiber values, and growth ring width were measured and correlated with compressive strength. Results obtained revealed significant relationships: negative between growth ring width and compressive strength and positive between wood type and compression strength at p = 0.05 and p < 0.01 levels. A. Toxicaria had the highest compression strength which differed significantly ( p = 0.05) when compared with T. africana and M. excelsa . On the other hand, T. africana was observed to have the smallest growth ring width and shorter fibers. It is evident from the results that species with narrower growth rings widths have higher compression strength, although some factors other than this, which may depend on the wood type, could equally influence the compression strength positively.

This study aims at appraising the capability of tannic powders of African locust been pod husks (Parkia Biglobosa) and of the India tamarind (Pithecellobium dulce) peel to bind Africa antiaris sawdust particles in order to manufacture environmental panels without formaldehyde emission. In the process, the granulometry has been studied. Thus, four granular groups (g) are obtained: 1.6

Recent publication attested that in the urban forest of Brazzaville, litter decomposition is faster with almost 45% of initial weight loss than in the dry season, where an average loss of 26% in initial litter weight is noted (Ifo et al., 2018). This study was carried out in the urban forest of Brazzaville to follow the decomposition of some organic compounds/secondary metabolites (reducing Sugars, total Flavonoid and Polyphenols) of the leaves litters of two tropical species Antiaris toxicaria Lesch and Millettia laurentii De Wild. Thin-layer chromatography and spectrophotometric assay of these metabolites were used on the samples of litters collected in the field on various dates of follow-up of the decomposition (0 d, 14 d, 28 d, 42 d, 56 d, 72 d and 84 d). The chromatographic profile of initial litters shows a series of spots on yellow florescence materializing presence of flavonoids, green fluorescence revealing the presence of the acids phenols derived from the cinnamic acid. But the chromatographic profile of the two litters in decomposition after two weeks remains without structural information, being able to characterize the decomposition of the chemical families highlighted in the initial litters. Also, the analysis of quantitative total reducing sugar in the initial litters, gives average concentrations of 64.4, 58.6, 57.5 g EG/kg Ms respectively for the litters of Millettia laurentii De Wild, Antiaris toxicaria Lesch and the mixed litters (Millettia laurentii and Antiaris toxicaria). Comparatively with the other types of litters, the initial average concentrations in phenolic compounds (polyphenols and flavonoids totals) were the highest for the litters of Antiaris toxicaria Lesch (27.3 g EAG/kg Ms and 13.07 g EC/kg Ms) (P = 0.001). The losses of organic chemical compounds are more significant during the first two weeks of experiment than after this period. Antiaris toxicaria Lesch loses on average 43.8 g EG/kg Ms of reducing Sugars, 12.21 g EC/kg Ms of totals flavonoids and 26.4 g EAG/kg Ms of total polyphenols, equivalent to 30% of loss of the initial weight. Average losses of 45.7 g EG/kg Ms were obtained for reducing sugars, 1.5 g EC/kg Ms for totals flavonoids and 8.72 g EAG/kg Ms for totally phenols in for the litters of Millettia laurentii, comparable to 24% in initial weight loss. This study showed on the one hand, the direct link between rainfall and litters decomposition and the losses in weight of the litters resulted in dissolution in the water of the studied compounds.

Ethnopharmacological relevance Different parts of Antiaris africana Englea (Moraceae) are used traditionally for the treatment of various diseases, including epilepsy and other nervous system disorders. Aims of this study The current study was designed to evaluate the neuroprotective activity of flavonoids isolated from A. africana against potassium cyanide (KCN)-induced oxidative damage in brain homogenate. Materials and methods Dried and ground leaves of A. africana were extracted with methanol and fractioned into n-hexane (HFA), dichloromethane (DFA), ethyl acetate (EFA) and methanol (MFA). Each fraction was assessed for neuroprotective potential by anticholinesterase activity test. The fraction with the best anticholinesterase activity was subjected to various chromatographic techniques through bioassay-guided fractionation to isolate the bioactive compounds. The protective ability of the extract, fractions and compounds against Potassium cyanide (KCN)-induced mitochondrial damage in rat brain homogenate was evaluated. Structures of the isolated compounds were determined using 1D and 2D NMR, mass spectrometry and by comparison with literature data. Results and discussion The ethyl acetate fraction showed the best anticholinesterase activity with an IC50 of 23.23 ± 1.12 μg/ml. Quercetin and a biflavonoid glucoside identified as 3′-4′-bisquercetin-3β-D-diglucoside from this fraction displayed a remarkable antioxidant activity in the DPPH assay and showed significant (P Conclusion Quercetin and the bisquercetin-diglucoside isolated from the leaves of A. Africana for the first time, are major contributors to the observed neuroprotective property of the plant which supports its folkloric usage in the management of seizures, epilepsy and other neurological disorders.

The immune system is one of the most complex biological systems in the body. During infection, the immune system is under attack by a large number of viruses, bacteria, fungi and parasites. Immune response firstly involves, recognition of the pathogen or foreign object and secondly, a reaction to eliminate it. Aqueous extract of Antiaris africana is used to study their immune modulator activity. This plant has its various parts used in folk medicines. The mechanism of action has not been fully elucidated. Therefore, this research work studies the effect of aqueous extract of Antiaris Africana stem bark on phagocytic activities of neutrophil isolated from apparently healthy individual using a non-subjective commercial colourimetric assay kit obtained from Cell-Biolab Inc., USA. The purity and viability of isolated neutrophils were >90% and >95% respectively. The extract enhances neutrophil phagocytosis at 1.0, 5.0, 10.0, 15.0, 20.0 and 25 μg/ml by 2.5%, 11.6%, 18.4%, 24.4%, 31.2% and 38.2% respectively, compared to the control (100%). Hence, it was observed that neutrophil phagocytosis increases with increased extract concentrations. It can be concluded from the study that enhancement of phagocytosis may be the possible mechanism of action of the plant as an immune modulator.

Natural plant compounds with potent proliferation inhibition and apoptosis induction properties have been screened as novel anticancer drugs. Toxicarioside N (Tox N) was isolated from the seeds of the tropical plant Antiaris toxicaria in Hainan province, China. To our knowledge, the effects that Tox N has on the apoptosis of SGC-7901 cells and its potential mechanism have never been investigated. In this study, we detected the anticancer activities of Tox N and explored the potential mechanism in the human gastrointestinal cancer cell line SGC-7901. Here, we found that Tox N inhibited SGC-7901 cell growth in a dose- and time-dependent manner and induced apoptosis in cells based on cell morphology and flow cytometry analyses. Additionally, the SGC-7901 cell treated with Tox N up-regulated the expression level of cleaved caspase-3/9 and PARP, increased the Bax/Bcl-2 ratio, and led to the release of cytochrome c into the cytoplasm. In addition, Tox N treatment led to the phosphorylation of p38MAPK. SB203580, a p38MAPK inhibitor, partially attenuated Tox N induced apoptosis by preventing the activation of caspase-3/9 and PARP. Our results indicated for the first time that Tox N can induce SGC-7901 cells apoptosis by activating the p38MAPK pathway.

Background: Oxidative stress plays a significant role in stroke pathogenesis. Hence, plants rich in antioxidant phytochemicals have been suggested as effective remedies for prevention and treatment of stroke and other neurological diseases. Antiaris africana Engl. (Moraceae) is traditionally used for the management of brain-related problems but there is paucity of data on its anti-stroke potential. Materials and Methods: Ischemia/reperfusion injury was induced by a 30 min bilateral common carotid artery occlusion/ 2 h reperfusion (BCCAO/R) in the brain of male Wistar rats. A sham-operated group which was not subjected to BCCAO/R and a group subjected to BCCAO/R without treatment with MEA served as controls. The ameliorative effect of 14 days of pretreatment with 50 mg/kg or 100 mg/kg A. africana methanol leaf extract (MEA) on BCCAO/R-mediated alterations to key markers of oxidative stress (malondialdehyde, reduced glutathione, xanthine oxidase, superoxide dismutase, catalase and glutathione peroxidase) and neurochemical disturbances and excitotoxicity (myeloperoxidase, glutamine synthetase, Na+/K+ ATPase, acetylcholinesterase and tyrosine hydroxylase), was evaluated and compared with the effect produced by treatment with 20 mg/kg quercetin as a reference standard. Results: Results show that pretreatment with MEA significantly mitigated or reversed BCCAO/R-induced changes in the level or activity of the evaluated biochemical markers of oxidative stress, neurochemical dysfunction and excitotoxicity compared with the BCCAO/R untreated control group (p < 0.05). The effect produced by 100 mg/kg MEA was similar to that of the reference standard, quercetin. Conclusion: These results revealed the neuroprotective potential of A. africana in stroke and other ischemia-related pathologies. Key words: brain ischemia

// Yong-Hao Huang 1, * , Yan Sun 1, * , Feng-Ying Huang 1, * , Yue-Nan Li 1 , Cai-Chun Wang 1 , Wen-Li Mei 2 , Hao-Fu Dai 2 , Guang-Hong Tan 1 and Canhua Huang 1, 3 1 Key Laboratory of Tropical Diseases and Translational Medicine of the Ministry of Education & Hainan Provincial Key Laboratory of Tropical Medicine, Hainan Medical College, Haikou 571199, China 2 Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571199, China 3 State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China * These authors have contributed equally to the work Correspondence to: Canhua Huang, email: hcanhua@hotmail.com Guang-Hong Tan, email: tanhoho@163.com Hao-Fu Dai, email: daihaofu@itbb.org.cn Keywords: colorectal cancer, toxicarioside O (TCO), autophagy, apoptosis, sirtuin-1 (SIRT1) Received: February 15, 2017 Accepted: March 21, 2017 Published: April 18, 2017 ABSTRACT Colorectal cancer is the most common cancer. It has high morbidity and mortality worldwide, and more effective treatment strategies need to be developed. Toxicarioside O (TCO), a natural product derived from Antiaris toxicaria , has been shown to be a potential anticancer agent. However, the molecular mechanisms involved remain poorly understood. In this study, our results demonstrated that TCO can induce both apoptosis and autophagy in colorectal cancer cells. Moreover, TCO-induced autophagy was due to the increase of the expression and activity of the enzyme sirtuin-1 (SIRT1), and subsequent inhibition of the Akt/mTOR pathway. Inhibition of SIRT1 activity by its inhibitor, EX-527, attenuated TCO-induced autophagy. Of interest, inhibition of autophagy by chloroguine, an autophagy inhibitor, enhanced TCO-induced apoptotic cell death, suggesting that autophagy plays a protective role in TCO-induced apoptosis. Together, these findings suggest that combination of TCO and autophagy inhibitor may be a novel strategy suitable for potentiating the anticancer activity of TCO for treatment of colorectal cancer.

Background The physiopathologies of many neurologic diseases are characterized by related biochemical dysfunctions that could be explored as drug targets. This study evaluated the effect of a methanol leaf extract of Antiaris africana (MEA) on critical bioindices of Parkinsonism and related neurologic dysfunctions in rats with rotenone-induced neurotoxicity. Methods Animals were administered 50 or 100 mg/kg MEA for 14 consecutive days. Rotenone (1.5 mg/kg) was administered three times per day on days 13 and 14. Coenzyme Q10 (5 mg/kg) was the reference drug. Complex I activity, dopamine level, activities of acetylcholinesterase, myeloperoxidase, Na+/K+ ATPase and glutamine synthetase, as well as oxidative stress indices were evaluated at the end of the period of treatment. Results Rotenone-intoxicated group showed disruption of complex 1 activity, dopamine level, and glutamine synthetase activity with negative alterations to activities of acetylcholinesterase, myeloperoxidase, and Na+/K+ ATPase as well as heightened cerebral oxidative stress. MEA restored brain mitochondria functionality, mitigated altered neurochemical integrity, and ameliorated cerebral oxidative stress occasioned by rotenone neurotoxicity. The activity of A. Africana was comparable with that of 5 mg/kg coenzyme Q10. Conclusions These results indicated that A. africana displayed therapeutic potential against Parkinsonism and related neurologic dysfunctions and support its ethnobotanical use for the treatment of neurologic disorders.

Mist Antiaris is a herbal decoction for treatment of nervous disorders. Safety and efficacy were evaluated in Sprague-Dawley rats and human patients, respectively. Acute toxicity was assessed by administration of a single 5000 mg/kg oral dose of decoction to a group of six rats. For subchronic toxicity, four groups of six rats each received water (control) or 10, 100, or 200 mg/kg oral doses of decoction daily for eight weeks. Body weight, serum, urine, and hematological profile of the animals in each group were monitored over the period. Effects of treatment on pentobarbital-induced sleeping time and histology of liver, lung, heart, and kidney tissue were assessed at the end of the study. There was no evidence of acute toxicity within 48 hours of the oral dose. Over the 8-week period, body weight increases in Mist Antiaris treatment groups were reduced relative to the control group. There were no significant differences in urine profile, serum biochemistry, hematological parameters, and pentobarbital-induced sleeping time. Tissue histology revealed no differences relative to controls. Assessment of efficacy was by retrospective review of data on patients who presented with peripheral neuropathy. Treatment resulted in 53.7 % of patients reporting complete resolution and 15.7 % showing reduction in neuropathic symptoms. The data demonstrate that there is no toxicity due to subchronic administration of Mist Antiaris in Sprague-Dawley rats. The reduction or resolution of neuropathic symptoms indicated by patents’ file data provides evidence to suggest that Mist Antiaris has antineuropathic effects.

Antiaris toxicaria (Pers.) Lesch. is one of the species of ecological importance distributed in Western Ghats and other parts. This species is considered as one of the threatened species and it needs conservation. The information on fruit and seed trait variation and germination attributes are scanty. Such database is useful for afforestation programme as well as for augmentation of rare plant species in their natural habitat. For the present study, 10 open pollinated trees distributed in Devade forest of Sakharpa were marked. April month was the peak fruiting period and healthy fruits were collected from the ground. Fruit and seed traits were found to be varied significantly among trees, where fruit length ranged from 21.50 to 24.71 mm and fruit weight ranged from 3.64 to 4.07 g. Similarly, seeds length (14.01 -15.09 mm), seed thickness (12.15 -13.04 mm) and seed weight (1.20 – 1.57g) also showed significant variation among 10 trees. Field observation showed that there was a poor regeneration in this species at studied site. Therefore, germination study was conducted at nursery condition by imposing several pretreatments. Among eight treatments including control, soaking seeds in water for 24 hrs (T2) resulted in better germination of 38.0% as compared to others. In T2 seed germination started at 16 days after sowing and completed within 42 days. Potting mixture of red soil with saw dust in 30:70 ratio improved seed germination about 20 % as compared to red soil media.

The study was aimed at evaluating the toxicological and antioxidant activities of Antiaris africana Engl. (family Moraceae), that is used in Nigeria and other West Africa countries as a panacea for the treatment of several ailments. The methanolic extract of A. africana (MEA) obtained was analysed for antioxidant activities in vitro and screened for various phytochemicals present. Phenolic and flavonoid contents were determined followed with high performance liquid chromatography -diode-array detection (HPLC-DAD) fingerprinting of phenolic content. Furthermore, the sub-acute toxicity of MEA was determined via oral administration of varying doses for 14 consecutive days (0, 50, 100, 200 and 400 mg/kg) in rats. After oral administration for 14 consecutive days in male rats, the toxicity effect was assayed by determining aspartate aminotransferase (AST) and alanine aminotransferase (ALT) for hepatic function; urea and creatinine for renal function; creatinine kinase (CK) for cardiac function; and lipid profile. HPLC results showed that the major phenolics present are quercetin, rutin, caffeic acid, garlic acid and quercetin. MEA was able to scavenge diphenyl picryl hydrazyl, hydroxyl and nitric oxide radicals and prevent lipid peroxidation induced by ferrous sulphate at all concentration tested. The toxicology investigation showed that at low doses, A. africana is non-toxic, while at high doses; it is moderately toxic to the animals. In conclusion, A. Africana is generally non-toxic; however, care must be taken in administration at higher doses. Key words: Toxicology, HPLC, phytochemicals, Antiaris africana.

Three new compounds, namely (+)-pranferol (1), antiarone M (2), and anticerol A (3), together with 9 known compounds, were obtained from the bark of Antiaris toxicaria. Their chemical structures were elucidated on the basis of spectroscopic methods including UV, IR, (HR) ESI-MS, H-1, C-13 NMR, HSQC, H-1-H-1 COSY, HMBC and X-ray crystallographic technique. The absolute configurations of compounds 1 and 2 were determined by modified mosher method and CD spectrum. (C) 2015 Phytochemical Society of Europe. Published by Elsevier B.V. All rights reserved.

Background: Oxidative stress plays a significant role in stroke pathogenesis. Hence, plants rich in antioxidant phytochemicals have been suggested as effective remedies for prevention and treatment of stroke and other neurological diseases. Antiaris africana Engl. (Moraceae) is traditionally used for the management of brain-related problems but there is paucity of data on its anti-stroke potential. Materials and Methods: Ischemia/reperfusion injury was induced by a 30 min bilateral common carotid artery occlusion/ 2 h reperfusion (BCCAO/R) in the brain of male Wistar rats. A sham-operated group which was not subjected to BCCAO/R and a group subjected to BCCAO/R without treatment with MEA served as controls. The ameliorative effect of 14 days of pretreatment with 50 mg/kg or 100 mg/kg A. africana methanol leaf extract (MEA) on BCCAO/R-mediated alterations to key markers of oxidative stress (malondialdehyde, reduced glutathione, xanthine oxidase, superoxide dismutase, catalase and glutathione peroxidase) and neurochemical disturbances and excitotoxicity (myeloperoxidase, glutamine synthetase, Na+/K+ ATPase, acetylcholinesterase and tyrosine hydroxylase), was evaluated and compared with the effect produced by treatment with 20 mg/kg quercetin as a reference standard. Results: Results show that pretreatment with MEA significantly mitigated or reversed BCCAO/R-induced changes in the level or activity of the evaluated biochemical markers of oxidative stress, neurochemical dysfunction and excitotoxicity compared with the BCCAO/R untreated control group (p < 0.05). The effect produced by 100 mg/kg MEA was similar to that of the reference standard, quercetin. Conclusion: These results revealed the neuroprotective potential of A. africana in stroke and other ischemia-related pathologies.

Background Antiaris toxicaria has previously shown anticonvulsant activity in acute animal models of epilepsy. The aqueous extract (AAE) was further investigated for activity in kindling with pentylenetetrazole and administration of pilocarpine and kainic acid which mimic temporal lobe epilepsy in various animal species. Results ICR mice and Sprague–Dawley rats were pre-treated with AAE (200–800 mg kg−1) and convulsive episodes induced using pentylenetetrazole, pilocarpine and kainic acid. The potential of AAE to prevent or delay onset and alter duration of seizures were measured. In addition, damage to hippocampal cells was assessed in kainic acid-induced status epilepticus test. 800 mg kg−1 of the extract suppressed the kindled seizure significantly (P

Cocoa agroforestry is perceived as potential adaptation strategy to sub-optimal or adverse environmental conditions such as drought. We tested this strategy over wet, dry and extremely dry periods comparing cocoa in full sun with agroforestry systems: shaded by (i) a leguminous tree species, Albizia ferruginea and (ii) Antiaris toxicaria, the most common shade tree species in the region. We monitored micro-climate, sap flux density, throughfall and soil water content from November 2014 to March 2016 at the forest-savannah transition zone of Ghana with climate and drought events during the study period serving as proxy for projected future climatic conditions in marginal cocoa cultivation areas of West Africa. Combined transpiration of cocoa and shade trees was significantly higher than cocoa in full sun during wet and dry periods. During wet period, transpiration rate of cocoa plants shaded by A. ferruginea was significantly lower than cocoa under A. toxicaria and full sun. During the extreme drought of 2015/16, all cocoa plants under A. ferruginea died. Cocoa plants under A. toxicaria suffered 77% mortality and massive stress with significantly reduced sap flux density of 115 gcm−2d−1 whereas cocoa in full sun maintained higher sap flux density of 170 gcm−2d−1. Moreover, cocoa sap flux recovery after the extreme drought was significantly higher in full sun (163 gcm−2d−1) than under A. toxicaria (37 g cm−2 d−1). Soil water content in full sun was higher than in shaded systems suggesting that cocoa mortality in the shaded systems was linked to strong competition for soil water. The present results have major implications for cocoa cultivation under climate change. Promoting shade cocoa agroforestry as drought resilient system especially under climate change needs to be carefully reconsidered as shade tree species such as the recommended leguminous A. ferruginea constitute major risk to cocoa functioning under extended severe drought. This article is protected by copyright. All rights reserved.

The cholinesterase inhibitory activity and the memory-enhancing effects of 22 Nigerian medicinal plants belonging to 16 different families were investigated. The acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory potentials of extracts, fractions, and isolated compounds were evaluated by Ellman colorimetric and thin-layer chromatography (TLC) bioautographic assay techniques. Bioactivity-directed phytochemistry, as well as spectroscopic analysis, was carried out. Morris water maze test was used to assess the cognitive enhancing potential of some of the most active plants. Some plants such as Morinda lucida, Spondias mombin, Pycnanthus angolensis, and Peltophorum pterocarpum showed inhibitory activity on both enzymes, while others exhibited some remarkable selectivity in their actions. Alchornea laxiflora stem bark and root bark, Calophyllum inophyllum root bark, and Crinum jagus leaves were selectively active against AChE, while Antiaris africana, Bombax bromoposenze, Combretum molle, and Garcinia kola were selectively active against BuChE. Activity-directed phytochemistry led to the isolation of bioactive compounds which may lead to drug development. The in vivo effect of four most active plants, S. mombin, P. angolensis, P. pterocarpum, and M. lucida, on scopolamine-induced memory loss was also confirmed.

Five new cardiac glycosides (1-5, namely antiaroside Y-ZC) together with 19 known compounds were obtained from the bark of Antiaris toxicaria. Their chemical structures were determined by IR, HR-ESI-MS, 1D and 2D NMR (HSQC, H-1-H-1 COSY, HMBC, ROESY). The absolute configuration of sugar unit was defined by acid hydrolysis and appropriate derivatization. Compound 1 was rare 5 beta-H-10 beta-H-19-nor-cardenolide, which might derive from decarboxylative derivative of 19-COOH cardenolide. The inhibitory effects of cardiac glycosides 1-11 on the viability of NIH-H460 lung cancer cells and their induction of Nur77 expression were evaluated and preliminary structure-activity relationship (SAR) was also discussed. (c) 2014 Elsevier B.V. All rights reserved.

Conventional wood preservatives are not only toxic to target bio-deterioration organisms but also to humans, other organisms and the environment. In an effort to find preservatives that are less toxic or non-toxic to man, other organisms and the environment, efficacy of branch bark and heartwood water extracts (0.65 g/ml) of Erythropleum suaveolens (potrodom) and Distemonanthus benthamianus (bonsamdua) were tested on five less used species (LUS) namely, Sterculia oblonga (ohaa), Antiaris toxicaria (kyenkyen), Canarium ediwonua), Celtis zenkeri (esa-kokoo) and Cola gigantea (watapuo) of varying perviousness and retentiveness from varying contents of hydrophobic and water-repellent extractives and/or extraneous substances in wood and/or vessels. Bonsandua extracts were more resistant to leaching, but potrodom extractives improved durability of Canarium schweinfurthii more than bonsamdua extractives. Potrodom bark extracts could be readily employed to preserve non-recalcitrant low durability timber species such as C. schweinfurthii, and possibly recalcitrant low durability ones such as S. oblonga after some form of pre-treatment and/or under pressure conditions. Improved durability of immersed and brushed LUS was ranked as follows: C. gigantea > C. zenkeri > S. oblonga > A. toxicaria > C. schweinfurthii proving that the natural durability of timber is somewhat dependent on their level of recalcitrance from intrinsic hydrophobic and/or water-repellent extractives and/or extraneous substances. Though extracts showed reduced efficacy with time, the use of potrodom extractives for the preservation (control of pests) of non-recalcitrant low durability wood is promising.

Eight new cardiac glycosides/aglycones (antiaritoxiosides A-G, 1-7, and antiarotoxinin B, 8), two new coumarins (anticarins A-B, 41-42), and two new flavanones (antiarones L-K, 43-44) were isolated from trunk bark of Antiaris toxicaria together with 53 known compounds. The new structures were established by extensive analysis of spectroscopic data. Compound 1 (10-carboxy and 3 alpha-hydroxy) and compounds 3-6 (10-hydroxy) contain unique substituents that are rarely found in cardiac glycosides. The cytotoxic effects of isolated compounds against ten human cancer cell lines, KB, KB-VIN, A549, MCF-7, U-87-MG, PC-3, 1A9, CAKI-1, HCT-9 and S-KMEL-2, were tested using the sulforhodamine B assay. Five compounds (12, 16, 20, 22, and 31) showed significant cytotoxicity against all ten cancer cell lines, with notable potency at the ng/mL level against some cell lines, which merits further development as clinical trial candidates. (C) 2014 Published by Elsevier Ltd.

Antiaris toxicaria (Antiaris, Moraceae) is a medicinal and extremely toxic species. To facilitate species identification and provide genetic information, we determined the complete chloroplast genome of A. toxicaria using the Illumina platform. The genome was 161,412 bp in length, comprising a large single-copy region (LSC) of 89,883 bp, a small single-copy region (SSC) of 20,375 bp, and a pair of inverted repeats (IRs) of 25,577 bp each. The genome contained 130 encoded genes in total, including 85 protein-coding genes, 8 ribosomal RNA genes, and 37 transfer RNA genes. The overall GC content of the A. toxicaria chloroplast genome is 35.87%. The phylogenetic analysis revealed A. toxicaria was closely related to the genus Ficus within the family Moraceae.

The ant-plant Sarang Semut is one of the medicinal antimicrobial plants that is very beneficial to human health. As such the plant has widely been exploited in their natural habitat. The silviculture of this plant is not available due to limited knowledge about the existence in nature. Therefore, it is imperative to undertake the ecological study on the growth site of this plant in nature to collect the basic information for the culture and cultivation of this plant. The method used in this research was the descriptive method with the survey technique in Gunung Meja Nature Tourism Park, Manokwari. The research showed that one species of ant-plant was found namely Myrmecodia cf. schlechteri Valeton. The plant is epifit to selective host plants such as Garcinia picrorrhiza, Sterculia macrophylla, Intsia bijuga, Pometia coreacea, and Antiaris toxicaria. The ideal growth zone of this plant is in Zone 2 and 3.

Antiaris toxicaria (Moraceae) was evaluated for anticonvulsant activity in rodents. Animal models used include maximal electroshock test (MEST); pentylenetetrazole-induced (PTZ) convulsions; picrotoxin-induced (PCT) convulsions; strychnine- (STR-) and 4-aminopyridine-induced convulsions. Increase in latency to seizures as well as reduction in duration and frequency of seizures indicated anticonvulsant activity. The extract was more effective in all models used except the maximal electroshock test and strychnine-induced convulsions. Antiaris toxicaria aqueous extract (200, 400, and 800 mg kg−1) significantly () shortened the duration of convulsions in PTZ- and PCT-induced seizures. Delay in the onset of convulsions in the two tests was significant (). Reduction in the frequency of seizures was also significant () in both tests. Antiaris further delayed the onset of seizures in 4-aminopyridine model while producing 75% protection against death in mice. Diazepam (0.1, 0.3, and 1 mg kg−1), carbamazepine (3, 10, and 30 mg kg−1), and sodium valproate (100–400 mg kg−1) were used as reference anticonvulsant drugs for various models. Flumazenil blocked the effect of the extract in the PTZ test significantly suggesting that Antiaris toxicaria may be acting by enhancing the effects of the GABAergic system. Antiaris toxicaria aqueous extract therefore possesses anticonvulsant activity.

Phytochemical investigation of the latex of Antiaris toxicaria resulted in the isolation of 15 new [antiarosides J-X (1-15)] and 17 known cardiac glycosides. The effects of the cardiac glycosides on apoptosis and the expression of orphan nuclear receptor Nur77 were examined in human NIH-H460 lung cancer cells. Several of the cardiac glycosides induced apoptosis in lung cancer cells, which was accompanied by induction of Nur77 protein expression. Treatment of cancer cells with the cardiac glycosides resulted in translocation of the Nur77 protein from the nucleus to the cytoplasm and subsequent targeting to mitochondria. The results show that the cardiac glycosides exert their apoptotic effect through the Nur77-dependent apoptotic pathway.

Two new strophanthidol cardenolides, toxicarioside N ( 1 ) and toxicarioside O ( 2 ), together with three known ones, were isolated from the seeds of Antiaris toxicaria . The structures of the new compounds were identified as strophanthidol-3- O - β - d -glucopyranosyl-(1 → 4)-6-deoxy- β - d -allopyranoside ( 1 ) and strophanthidol-3- O - β - d -glucopyranoside ( 2 ), respectively. The cytotoxic test showed that compounds 1 and 2 exhibited significant cytotoxicity against SMMC-7721 and K562.

Antiaris toxicaria is a plant traditionally used in Ghana for the treatment of various neurological conditions such as epilepsy and pain. This present study therefore seeks to screen for the neuropharmacological activities of the aqueous extract of Antiaris toxicaria (AAE) stem bark. The effect of Antiaris extract on pentobarbital-induced sleeping time, tail immersion test, spontaneous locomotor activity, motor coordination, PTZ-induced convulsions as well as the Irwin test was investigated. The extract produced analgesia and Straub tail at (300-3000 mg kg-1) in the Irwin test suggestive of a morphine-like action. These effects were absent after 24 h. No deaths were recorded in the test estimating the LD50 to be above 3000 mg kg-1. Spontaneous locomotor activity of the mice in the activity meter test was decreased significantly (p

Objective To investigate possible mechanism of toxicarioside A in HS-5 bone stromal cells. Methods HS-5 bone stromal cells were cultured in media supplemented with various concentrations of toxicarioside A or control DMSO (not treatment). Endoglin and TGF-β were detected by Northern and Western blot analysis and quantified in a standard method. Downstream molecules of endoglin and TGF-β (Smad1, Smad2 and their active phosphorylated counterparts, pSmad1 and pSmad2) were also detected and quantified by Western blot analysis. In addition, cell proliferation assay and small interfering RNA (siRNA) against endoglin were used to certificate the function of endolgin in the HS-5 cells. Results Compared with the not treated (0 μg/mL) or DMSO treated control HS-5 cells, HS-5 cells treated with toxicarioside A were found significant attenuation of endolgin and TGF-β expression. Significant inhibition of cell proliferation was also found in the HS-5 cells treated with toxicarioside A. ALK1-related Smad1 and ALK5-related Smad2 were decreased in HS-5 cells treated with toxicarioside A. In addition, phosphorylated Smad1 (pSmad1) and Smad2 (pSmad2) were also found attenuation in toxicarioside A-treated HS-5 cells. RNA interference showed that blockage of endoglin by siRNA also decreased Smad1 and Smad2 expression in HS-5 cells. Conclusions Our results indicate that toxicarioside A can influence bone marrow stromal HS-5's function and inhibit HS-5 cell proliferation by alteration of endoglin-related ALK1 (Smad1) and ALK5 (Smad2) signaling.

Wood extractives play a major role in the protection of wood against termite and fungal attack. Wood extractives from three hard wood species of Milicia excelsa, Albizia coriaria and Markhamia lutea that are known to be very resistant against termite attack and fungal decay were studied to assess their role as wood preservatives in Uganda. Acetone, hexane and distilled water were used in the extraction of these compounds from the outer heartwood of the selected durable species. Extraction was done using a soxhlet extractor. e extractives obtained were used to treat Pinus caribaea and Antiaris toxicaria species known to be susceptible to termites and fungal attack. Treated blocks were then exposed to Macrotermes bellicosus termites in the eld. It was observed that wood extracts used as preservatives improved the resistance of less durable samples to termite attack by 50% compared to the controls. It was also observed that removal of extractives decreased resistance of the durable samples. It can be concluded that wood extractives contribute greatly to the protection of less durable wood species against termite attack.

Antiaris africana seeds yielded 29.6% starch which showed appreciable high contents of ash, protein, and fat. The average diameter of A. africana starch granules was 3.98 µm compared to 8.93 µm for maize starch. A. africana starch had a C-type XRD pattern and crystallinity of 41.5%. A. africana starch had higher AM content (24.1%) than maize starch (20.9%). The gelatinization onset temperature of A. africana starch (66.7°C) was higher than maize starch (63.1°C), but its gelatinization temperature range (8.57°C) and enthalpy (13.97 J/g) were lower than the values for maize starch (14.02°C, 14.65 J/g). The pasting temperature (Pt) and setback (Vs) were lower and breakdown (Vb) higher for A. africana starch (Pt = 82.5°C, Vs = 173.8 RVU, and Vb = 121.42 RVU) than for maize starch (Pt = 84.9°C, Vs = 183.73 RVU, and Vb = 78.58 RVU). The GPC analysis gave Mw of 2.18 × 107 g/mol and radius of gyration of 95.1 nm for Antiaris starch. Antiaris starch paste exhibited poor freeze-thaw stability but its small granule size indicates potential for application as dusting starch.

The quality of seed treatment by frugivores has an effect on seed removal after dispersal, seed germination and tree recruitment. We provide information on postdispersal seed removal, germination and subsequent recruitment in tropical forest tree species Antiaris toxicaria in Ghana. We tested whether postdispersal seed removal and germination rates were differentially affected by the following seed treatments: seeds that were spat out by monkeys with all fruit pulp removed and spitting seeds with fruit pulp partially removed as observed in some birds and bats. We used seeds of intact ripened fruits as control. Frugivore seed treatment and distance from bole affected seed removal patterns, whereas intact seeds were significantly removed from all seed stations. The germination success was greater for seeds that were spat out by monkeys and poor for seeds with fruit pulp partially removed and intact fruits. More recruits were recorded at the edge of the adult A. toxicaria canopy radius. There was weak relationship (r2 = 0.042) between the number of recruits and distance away from the adult tree. Results suggest that the subsequent recruitment in tropical forest tree species may be enhanced by some frugivore fruit-handling behaviour where fruit pulp is removed from the seeds without destroying the seeds. Resume La qualite du traitement des graines par les frugivores a un effet sur la disparition des graines apres dispersion, sur leur germination et sur le recrutement des arbres. Nous donnons des informations sur le deplacement et la germination des graines apres leur dispersion et sur le recrutement subsequent des arbres de l’espece tropicale Antiaris toxicaria, au Ghana. Nous avons verifie si les taux d’enlevement et de germination des graines apres dispersion etait affecte differemment par les traitements suivants : des graines recrachees par des singes apres enlevement complet de la pulpe et des graines rejetees avec la pulpe partiellement enlevee, comme c’est le cas avec certains oiseaux et chauves-souris. Nous avons utilise des graines de fruits murs intacts comme controles. Le traitement des graines par les frugivores et la distance par rapport a l’arbre affectaient le schema de disparition des graines alors que les semences intactes etaient significativement enlevees de toutes les stations de production. Le succes de la germination etait plus grand pour les graines qui avaient ete recrachees par des singes et mediocre pour les graines desquelles la pulpe etait partiellement retiree et celles des fruits intacts. On a enregistre plus de recrus a la limite du rayon couvert par la canopee des A. toxicaria adultes. Il existait une faible relation (r2 = 0.042) entre le nombre de recrus et la distance par rapport a l’arbre adulte. Les resultats suggerent que le recrutement d’arbres d’especes tropicales peut etre ameliore par le traitement apporte par certains frugivores, qui enlevent la pulpe des fruits sans detruire les graines qui s’y trouvent.

A new drimane sesquiterpenoid glycoside, named 7-drimen-3β,11-diol 3-O-β-d-glucopyranoside, was isolated from the 95% EtOH extract of the seeds of Antiaris toxicaria (Pers.) Lesch. The chemical structure was completely elucidated using a combination of 1D and 2D NMR techniques (COSY, HMQC, HMBC, and ROESY) and HR-ESI-MS analysis. The compound showed inhibitory activities toward methicillin-resistant Staphylococcus aureus (MRSA), chronic myelogenous leukemia (K562), and human hepatoma (SMMC-7721) cell lines.