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In regions facing water scarcity and soil salinity, mitigating these abiotic stresses is paramount for sustaining crop production. This study aimed to unravel the synergistic effects of organic matter and phosphorus management in reducing the adverse effect of saline water for irrigation on red pepper ( Capsicum annuum L.) production, fruit quality, plant physiology, and stress tolerance indicators. The study was carried out in the arid Tadla region of Morocco and involved two key experiments: (i) a field experiment during the 2019 growing season, where red pepper plants were subjected to varying phosphorus fertilizer rates (120, 140, and 170 kg of P 2 O 5 .ha -1 ) and saline water irrigation levels (0.7; 1.5; 3; and 5 dS.m -1 ); and (ii) a controlled pot experiment in 2021 for examining the interaction of saline water irrigation levels (EC values of 0.7, 2, 5, and 9 dS.m -1 ), phosphorus rates (30, 36, and 42 kg of P 2 O 5 .ha -1 ), and the amount of organic matter (4, 8, 12, and 16 t.ha -1 ). The field study highlighted that saline irrigation significantly affected red pepper yields and fruit size, although phosphorus fertilization helped enhance productivity. Additionally, biochemical markers of stress tolerance, such as proline and glycine betaine, along with stomatal conductance, were impacted by increasing salinity levels. The pot experiment showed that combining organic amendments and phosphorus improved soil properties and stimulated red pepper growth and root weight across all salinity levels. The integration of phosphorus fertilization and organic amendments proved instrumental for counteracting salinity-induced constraints on red pepper growth and yield. Nonetheless, caution is necessary as high salinity can still negatively impact red pepper productivity, necessitating the establishment of an irrigation water salinity threshold, set at 5 dS.m -1 .

Soil salinity adversely limits crop and soil health, and this can be reversed by cropping systems where species exclude salts and activate microbial nutrient cycling. A randomized complete block design experiment was established in Laayoune-Morocco to evaluate the influence of irrigated grass pea and barley monocrops or combined together in 50-50% and 70-30% mixtures against soil salinity and CO 2 -C flux in sites with varying salinity. Site by treatment interaction significantly influenced (p < 0.05) soil salinity and CO 2 -C flux. Salinity reduced by 37 to 68 dS m -1 in highly saline soils across season regardless of treatment and barley monocrop retained the least salinity (15 dS m -1 ). Same applied to sites with low (1 to 2 dS m -1 ) and medium (2 to 5 dS m -1 ) salinity although less pronounced. The 70-30% grass pea, barley mixture maintained the greatest CO 2 -C flux in soils with low salinity and marginally enhancing soil active carbon (130 to 229 mg kg -1 soil) in different sites. Increasingly saline water filled pore space devastated CO 2 -C flux, although this process recovered under barley at extreme salinity. Overall, barley in mixture with grass pea can alleviate salinity and accelerate microbial carbon sequestration if irrigation is modulated in shallow desertic soils., (© 2023. Springer Nature Limited.)

Salinity has become a major issue in various parts of the world negatively impacting agricultural activities and leading to diminished crop potential and lower yields. Such situation calls for urgent interventions such as adopting salt-tolerant crops to fill the gap in food and feed availability. Blue panicgrass ( Panicum antidotale Retz.) is a promising salt-tolerant forage crop that has shown an appropriate adaptation and performance in the saline, arid, and desertic environments of southern Morocco. However, for obtaining a highest forage productivity with nutritional quality, optimization of the cutting interval is required. Thus, the objective of this study was to determine the optimal cutting time interval allowing high forage production and quality under high salinity conditions. This experiment was conducted over one entire year covering the summer and winter seasons. The effect of five cutting time intervals on selected agro-morphological traits, crop productivity, mineral nutrient accumulation, and forage quality of blue panicgrass in the region of Laayoune, southern Morocco. The finding of this study recommend that cutting blue panicgrass every 40 days maximized the annual fresh and dry forage yield as well as the protein yield, which reached 74, 22, and 2.9 t/ha, respectively. This study also revealed a significant effect of the season on both productivity and quality. However, forage yield declined during the winter and increased during the summer, while protein content increased during winter compared to summer. The mineral nutrient partitioning between shoots and roots, especially the K + /Na + ratio, indicated that blue panicgrass has salt tolerance mechanism as it excluded sodium from the roots and compartmentalized it in the leaves. In conclusion, there is a potential of blue panicgrass on sustaining forage production under salt-affected drylands, as demonstrated by the response to two key questions: (a) a technical question to farmers for its adoption such as at which interval should blue panicgrass be harvested maximizing both forage yield and quality? And (b) a scientific question on how does blue panicgrass maintain high K + /Na + ratio to cope with salinity stress?, Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2023 El Mouttaqi, Mnaouer, Nilahyane, Ashilenje, Amombo, Belcaid, Ibourki, Lazaar, Soulaimani, Devkota, Kouisni and Hirich.)

In the Sahara Desert, due to drought and salinity and poor soil fertility, very limited crop choice is available for the farmers to grow crops. Quinoa ( Chenopodium quinoa Willd.) has shown promising under such conditions in the South of Morocco, a true representative site of Sahara Desert. Soil organic amendments have the potential to minimize negative effects of soil salinity and improve crop production. Thus, this study aimed to elucidate the impact of nine organic amendments on quinoa (var. ICBA-Q5) growth, productivity, and biochemical parameters under saline irrigation water application (4, 12, and 20 dS·m -1 ). Results of the experiment indicate a significant effect of organic amendments on major agro-morphological and productivity parameters. Biomass and seed yield tends to decrease with the rise of salinity level, and organic amendments have improved productivity compared to the non-treated control. However, salinity stress alleviation was assessed by determining pigments concentration, proline content, phenolic compounds, and antioxidant activity. Therefore, the action of organic amendments varies from one level of salinity to another. Furthermore, a remarkably significant decrease in total saponin content was reached due to the application of amendments even at high saline conditions (20 dS·m -1 ). The results demonstrate the possibility of enhancing the productivity of quinoa as an alternative food crop under salinity conditions by using organic amendments and improving the quality of grains (saponin reduction) during the pre-industrialization process., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2023 El Mouttaqi, Sabraoui, Belcaid, Ibourki, Mnaouer, Lazaar, Sehbaoui, Ait Elhaj, Khaldi, Rafik, Zim, Nilahyane, Ghoulam, Devkota, Kouisni and Hirich.)

Rapid and accurate soybean yield prediction at an on-farm scale is important for ensuring sustainable yield increases and contributing to food security maintenance in Nigeria. We used multiple approaches to assess the benefits of rhizobium (Rh) inoculation and phosphorus (P) fertilization on soybean yield increase and profitability from large-scale conducted trials in the savanna areas of Nigeria [i.e., the Sudan Savanna (SS), Northern Guinea Savanna (NGS), and Southern Guinea Savanna (SGS)]. Soybean yield results from the established trials managed by farmers with four treatments (i.e., the control without inoculation and P fertilizer, Rh inoculation, P fertilizer, and Rh + P combination treatments) were predicted using mapped soil properties and weather variables in ensemble machine-learning techniques, specifically the conditional inference regression random forest (RF) model. Using the IMPACT model, scenario analyses were employed to simulate long-term adoption impacts on national soybean trade and currency. Our study found that yields of the Rh + P combination were consistently higher than the control in the three agroecological zones. Average yield increases were 128%, 111%, and 162% higher in the Rh + P combination compared to the control treatment in the SS, NGS, and SGS agroecological zones, respectively. The NGS agroecological zone showed a higher yield than SS and SGS. The highest training coefficient of determination (R 2 = 0.75) for yield prediction was from the NGS dataset, and the lowest coefficient (R 2 = 0.46) was from the SS samples. The results from the IMPACT model showed a reduction of 10% and 22% for the low (35% adoption scenario) and high (75% adoption scenario) soybean imports from 2029 in Nigeria, respectively. A significant reduction in soybean imports is feasible if the Rh + P inputs are large-scaled implemented at the on-farm field and massively adopted by farmers in Nigeria., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2023 Jemo, Devkota, Epule, Chfadi, Moutiq, Hafidi, Silatsa and Jibrin.)

Cacti are one of the most significant and diversified groups of angiosperms, distributed and cultivated globally, mostly in semi-arid, arid, and the Mediterranean climate regions. Conventionally, they are propagated by seeds or through vegetative propagation via rooted offshoots or grafting. However, these multiplication procedures remain insufficient for mass propagation. In vitro culture techniques are utilized to mass propagate endangered and commercial cacti species. These include somatic embryogenesis and plant regeneration through indirect or direct organogenesis. The latter is a promising tool for commercial clonal propagation of high-value species and has been successfully implemented for several species, such as Mammillaria, Hylocereus, Cereus, Echinocereus , and Ariocarpus . However, its success depends on explant type, basal nutrient formulation of culture medium, and types and concentrations of plant growth regulators. This study aimed to assess the potential of in vitro propagation methods applied to cacti species and discuss the different factors affecting the success of these methods. This study has also highlighted the insufficient work on Opuntia species for mass propagation through axillary buds' proliferation. The development of an efficient micropropagation protocol is thus needed to meet the supply of increasing demand of Opuntia species for human consumption as fruit, animal feed, and ecological restoration in semi-arid and arid zones., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2022 Bouzroud, El Maaiden, Sobeh, Devkota, Boukcim, Kouisni and El Kharrassi.)

Soil salinity is a major problem in arid and semi-arid regions, causing land degradation, desertification, and subsequently, food insecurity. Salt-affected soils and phosphorus (P) deficiency are the common problems in the sub-Sahara, including the Southern region of Morocco. Soil salinity limits plant growth by limiting water availability, causing a nutritional imbalance, and imparting osmotic stress in the plants. The objective of this study was to determine the positive effects of P on growth and productivity and understand the major leaf mineral nutrient content of quinoa ( Chenopodium quinoa Willd.) cv. "ICBA Q5" irrigated with saline water. A field experiment applying three salinity (Electrical Conductivity, EC) levels of irrigation water (ECw = 5, 12, and 17 dS·m -1 ) and three P fertilizer rates (0, 60, and 70 kg of P 2 O 5 ha -1 ) were evaluated in a split-plot design with three replications. The experiment was conducted in Foum El Oued, South of Morocco on sandy loam soil during the period of March-July 2020. The results showed that irrigation with saline water significantly reduced the final dry biomass, seed yield, harvest index, and crop water productivity of quinoa; however, P application under saline conditions minimized the effect of salinity and improved the yield. The application of 60 and 70 kg of P 2 O 5 ha -1 increased ( p < 0.05) the seed yield by 29 and 51% at low salinity (5 dS·m -1 ), by 16 and 2% at medium salinity (12 dS·m -1 ), and by 13 and 8% at high salinity (17 dS·m -1 ), respectively. The leaf Na + and K + content and Na + /K + ratio increased with irrigation water salinity. However, the leaf content of Mg, Ca, Zn, and Fe decreased under high salinity. It was also found that increasing P fertilization improved the essential nutrient content and nutrient uptake. Our finding suggests that P application minimizes the adverse effects of high soil salinity and can be adopted as a coping strategy under saline conditions.

Salinity is a major problem affecting crop production in many regions in the world including Morocco. Agricultural practices such as fertilization could be useful to overcome this problem and improve crop productivity. The objective of our study was to evaluate the combined effect of phosphorus fertilization and irrigation water salinity on growth, yield, and stomatal conductance of forage corn ( Zea mays L.) cv. "Sy sincerro". Field experiments were carried out for two years testing four levels of irrigation water salinity (ECw = 0.7; 2, 4, and 6 dS·m -1 ) and three rates of phosphorus (105, 126, and 150 kg P 2 O 5 ·ha -1 ) fertilization conducted in a split-plot design with three replications. The obtained results show that irrigation water salinity had a negative effect on all monitored parameters. For instance, the dry matter yield reduced by an average of 19.3 and 25.1% compared to the control under saline irrigation with an EC value equal to 4 and 6 dS·m -1 , respectively. The finding also showed that phosphorus applications tend to increase root weight, root length, stem length, leaf stomatal conductance, grain yield and dry matter yield under salinity conditions. For example, the addition of phosphorus with a rate of 126 and 150 kg P 2 O 5 ·ha -1 respectively improved dry matter yield by an average of 4 and 9% under low salinity level (ECw = 2 dS·m -1 ), by 4 and 15% under medium salinity (4 dS·m -1 ), and by 6 and 8% under a high salinity level (6 dS·m -1 ). Our finding suggests that supplementary P application could be one of the best practices to reduce the adverse effects of high salinity on growth and development of forage corn.

The benchmarking and monitoring of rice production performance indicators are essential for improving rice production self-sufficiency, increasing profitability, reducing labor requirements, optimizing fertilizer inputs, engaging youths in rice production, and increasing the overall sustainability of smallholder rice production systems in countries in sub-Saharan Africa (SSA). In this paper, we quantified five sustainability performance indicators (grain yield, net profit, labor productivity, and nitrogen (N) and phosphorus (P) use efficiencies) to benchmark rice production systems in SSA. Data were collected between 2013-2014 from 2907 farmers from two rice production systems (irrigated and rainfed lowlands) across five agroecological zones (arid, semiarid, humid, subhumid and highlands) in 12 countries (Benin, Cameroon, Cote d'Ivoire, Ghana, Madagascar, Mali, Niger, Nigeria, Senegal, Sierra Leone, Tanzania and Togo). The exploitable gap for each indicator (the difference between the mean of 10 % highest-yielding farms and the mean-yielding farms) was calculated across the countries, the two production systems and agroecological zones. The mean yield varied widely between 2.5 to 5.6 t ha -1 and 0.6 to 2.3 t ha -1 in irrigated and rainfed lowlands, respectively, with an average yield of 4.1 and 1.4 t ha -1 , respectively. Across the country-production system combinations, there were yield gaps of 29-69 %, profit gaps of 10-89 %, and labor productivity gaps reaching 71 %. Yield, profit, and labor productivity were positively correlated. They were also positively correlated with N and P fertilizer application rate, but not with N and P use efficiencies. Only between 34-44 % of farmers had desirable ranges in N- or P-use efficiencies in the two production systems. All sites for rainfed lowlands were characterized by low-yield and large gaps in yield, profit, and labor productivity, whereas irrigated lowlands in some countries (Madagascar, Mali, and Togo) have similar characteristics as rainfed ones. We conclude that there is an urgent need to disseminate precision nutrient management practices for optimizing nutrient use efficiency and enhancing rice performance indicators especially in rainfed lowlands as well as low-yielding irrigated lowlands. Furthermore, we propose recommendations for specific categories (i.e. farmer, rice production system, agroecological zone and country) to close performance indicator gaps and to allow the production at scale to achieve rice self-sufficiency in SSA., Competing Interests: The authors report no declarations of interest., (© 2021 The Author(s).)

Laser land levelling is expanding rapidly in the rice-wheat (RW) and maize-wheat (MW) systems of the Indo-Gangetic Plains of India and Pakistan. Current practice is to level to zero (0%) gradient, whereas a small gradient (e.g. 0.1%) is typically used in developed countries. Therefore, experiments were conducted in farmers' plots (~15 m x 40 m) in the Eastern Gangetic Plains to evaluate laser levelling with a 0.1% gradient in comparison with 0% and farmer levelling practice (FL). The study was conducted over two years in RW and MW systems. In the MW system, raised beds in plots lasered with 0% and 0.1% gradients were also evaluated. Laser levelling with 0% gradient significantly reduced irrigation amount and/or increased irrigation water productivity (WPi) in all crops/systems grown on the flat compared to FL except for wheat in the MW system. While there was a consistent trend for higher yield with a 0% gradient compared with FL, the differences were not significant in any crop/system. For the RW system, the results suggest no to marginal benefits in irrigation amount and WPi from levelling with a 0.1% gradient in comparison with 0% gradient. In that system, by far the bigger gains were from changing from FL to laser levelling with 0% gradient. This resulted in substantial reductions in irrigation amount, which greatly increased WPi in both crops (by ~40%), while yield was not affected. Rice grown with FL was not profitable, but lasering with 0% gradient significantly increased gross margin for rice, wheat and the total RW system. As for the RW system, levelling to 0% with a flat configuration significantly increased WPi of both crops in the MW system compared to FL, but by a lesser proportion. Raised beds significantly increased yield of maize by 8% (0.5 t ha -1 ), reduced irrigation amount by 20% (40 mm) and increased WPi by 34% (1.0 kg m -3 ) in comparison with the laser levelled flat plots. Gross margin of the MW system on beds was 17-20% higher than FL, and gross margin with beds on a 0.1% gradient was significantly higher than either gradient on the flat. The results suggest that the gains from levelling with a 0.1% gradient compared to 0% are marginal; however, this may change if the goal of consolidation of small farmer plots into larger fields becomes a reality provided there is a proportionate increase in irrigation flow rates, and ability to drain., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2021 The Authors.)

Sustainability of rice production systems is a prime concern for Asia to maintain food security and to support economic growth. This gain in productivity not only depends on agricultural inputs but also depends on social and environmental factors. To address these emerging issues, new resource- and capital-efficient and profitable technologies have been introduced. The conventional method of rice production (puddling and manual transplanting, PTR) is considered as highly input intensive. As an alternative, dry direct seeded rice (DSR) using seed drill has been promoted to save labor and production costs compared with PTR. Similarly, machine transplanted rice (MTR) has been also considered and promoted in many rice growing countries of South and East Asia. Economic, environmental, and social performances of DSR and MTR (alternative rice establishment technologies) were compared to the PTR using Sustainable Rice Platform (SRP) defined 12 Performance Indicators (PIs) (version 1.0) as a gauge to measure their sustainability. For that, a household survey was conducted on 652 households in Odisha India during 2016. The gaps, i.e., the target to achieve better sustainability, were computed for most of the indicators from the difference between top 10th percentile and the population mean value of the indicator. The results indicated a yield gap of 1.35 t ha -1 , a profit gap of $273 ha -1 , labor productivity gap of 21 kg day -1 , nitrogen (N) use efficiency gap of 22 kg grain kg -1 N, phosphorus (P) use efficiency gap of 105 kg grain kg -1 P, and water productivity gap of 0.00010 kg grain L -1 water in rice production systems in Odisha. Among the compared technologies, MTR results in the highest yield, profit, labor productivity, nitrogen-, phosphorus-use efficiency, and water productivity (at par), and is positive for children's welfare and the overall energy productivity, indicating better sustainability and has the potential to replace PTR. Direct seeded rice has the highest yield gap (1.57 t ha -1 ; 38%) but has the lowest production cost (can reduce the cost of production by $130 ha -1 ), and the highest greenhouse gas (GHG) reduction potential. SRP PIs are capable for assessing the sustainability of rice establishment technologies except for a few indicators, for example food safety and workers health and safety, which are more applicable to watershed and household level indicators, respectively. The SRP PIs provide scientific evidence and practical impetus for the selection and promotion of sustainable rice production technologies., (© 2019 The Authors.)

Following our interest in new diterpene glycosides with better taste profiles than that of Rebaudioside M, we have recently isolated and characterized Rebaudioside IX-a novel steviol glycoside-from a commercially-supplied extract of Stevia rebaudiana Bertoni. This molecule contains a hexasaccharide group attached at C-13 of the central diterpene core, and contains three additional glucose units when compared with Rebaudioside M. Here we report the complete structure elucidation-based on extensive Nuclear Magnetic Resonance (NMR) analysis (1H, 13C, Correlation Spectroscopy (COSY), Heteronuclear Single Quantum Coherence-Distortionless Enhancement Polarization Transfer (HSQC-DEPT), Heteronuclear Multiple Bond Correlation (HMBC), 1D Total Correlation Spectroscopy (TOCSY), Nuclear Overhauser Effect Spectroscopy (NOESY)) and mass spectral data-of this novel diterpene glycoside with nine sugar moieties and containing a relatively rare 16 α-linked glycoside. A steviol glycoside bearing nine glucose units is unprecedented in the literature, and could have an impact on the natural sweetener catalog.

In a continued search for novel diterpenoid glycosides, we recently isolated and characterized a Rebaudioside M derivative with a hydroxyl group at position 15 in the central diterpene core from an extract of Stevia rebaudiana Bertoni. Here we report the complete structure elucidation of 15α-hydroxy-Rebaudioside M (2) on the basis of NMR (1H, 13C, COSY, HSQC-DEPT, HMBC, 1D TOCSY, NOESY) and mass spectral data. Steviol glycoside with a hydroxyl group at C-15 in the central diterpene core has not been previously reported.

A natural sweetener, Rubusoside (1), subjected to extreme pH and temperature conditions, resulted in the isolation and structural elucidation of one novel rubusoside degradant (7), together with seven known degradants (2-6 and 8-9). ID and 2D NMR spectroscopy (1H, 13C, COSY, HSQC-DEPT, HMBC, and NOESY) and mass spectral data were used to fully characterize the degradant 7.

To supply the increasing demand of natural high potency sweeteners to reduce the calories in food and beverages, we have looked to steviol glycosides. In this work we report the bioconversion of rebaudioside A to rebaudioside I using a glucosyltransferase enzyme. This bioconversion reaction adds one sugar unit with a 1→3 linkage. We utilized 1D and 2D NMR spectroscopy (1H, 13C, COSY, HSQC-DEPT, HMBC, 1D TOCSY and NOESY) and mass spectral data to fully characterize rebaudioside I.

We report the isolation and complete structure of an isomer of rebaudioside D, known as rebaudioside D2. This novel steviol glycoside was isolated from a bioconversion reaction of rebaudioside A to rebaudioside D. Rebaudioside D2 possesses a relatively rare 1 --> 6 sugar linkage, which was discovered by extensive analysis of NMR (1H, 13C, COSY, HSQC-DEPT, HMBC, 1D TOCSY and NOESY) and mass spectral data.

Tetra-acetylajugasterone C (TAAC) was found to be one of the naturally occurring compounds of the Cameroonian medicinal plant Vitex cienkowskii which is responsible for a vasorelaxant activity of an extract of this plant. The evaluation of the underlying mechanisms for the relaxing effect of TAAC was determined using aortic rings of rats and mice. TAAC produced a concentration-dependent relaxation in rat artery rings pre-contracted with 1μM noradrenaline (IC50: 8.40μM) or 60mM KCl (IC50: 36.30μM). The nitric oxide synthase inhibitor l-NAME (100μM) and the soluble guanylate cyclase inhibitor ODQ (10μM) significantly attenuated the vasodilatory effect of TAAC. TAAC also exerted a relaxing effect in aorta of wild-type mice (cGKI(+/+); IC50=13.04μM) but a weaker effect in aorta of mice lacking cGMP-dependent protein kinase I (cGKI(-/-); IC50=36.12μM). The involvement of calcium channels was studied in rings pre-incubated in calcium-free buffer and primed with 1μM noradrenaline prior to addition of calcium to elicit contraction. TAAC (100μM) completely inhibited the resulting calcium-induced vasoconstriction. The same concentration of TAAC showed a stronger effect on the tonic than on the phasic component of noradrenaline-induced contraction. This study shows that TAAC, a newly detected constituent of Vitex cienkowskii contributes to the relaxing effect of an extract of the plant. The effect is partially mediated by the involvement of the NO/cGMP pathway of the smooth muscle but additionally inhibition of calcium influx into the cell may play a role., (Copyright © 2014 Elsevier GmbH. All rights reserved.)

A minor product, rebaudioside M2 (2), from the bioconversion reaction of rebaudioside A (4) to rebaudioside D (3), was isolated and the complete structure of the novel steviol glycoside was determined. Rebaudioside M2 (2) is considered an isomer of rebaudioside M (1) and contains a relatively rare 1→6 sugar linkage. It was isolated and characterized with NMR (1H, 13C, COSY, HSQC-DEPT, HMBC, 1D-TOCSY, and NOESY) and mass spectral data. Additionally, we emphasize the importance of 1D and 2D NMR techniques when identifying complex steviol glycosides. Numerous NMR spectroscopy studies of rebaudioside M (1), rebaudioside D (3), and mixture of 1 and 3 led to the discovery that SG17 which was previously reported in literature, is a mixture of rebaudioside D (3), rebaudioside M (1), and possibly other related steviol glycosides.

A neurofibromatosis type 1 ( NF1 ) based bioassay-guided phytochemical investigation on Simarouba berteroana led to the isolation of one new canthin-6-one-9-methoxy-5- O - β - D -glucopyranoside ( 1 ), seven known canthine alkaloids ( 2 - 8 ), two known quassinoids ( 9 - 10 ) and a known neo-lignan ( 11 ). The structures of all compounds were established by HRMS, 1D- and 2D-NMR analysis and comparison with previously reported data. Most of the compounds inhibited the proliferation of an Nf1 - and p53 -deficient mouse glioma cell line at non-cytotoxic concentrations.

In order to study cannabinoid receptor ligands, a novel plate-based assay was developed previously to measure internalization of CB1/CB2 receptors by determining the change in the intracellular levels of the radiolabeled agonists. This plate-based assay was also used for screening against complex matrices, specifically, in the present study screening for CB1/CB2 receptor activity of extracts for several species of the plant genus Zanthoxylum. The objective of this screen was to identify novel antagonists of the CB1 receptor, which simultaneously displayed agonist activity against the CB2 receptor, since compounds matching this criterion could be potential candidates for the treatment of type-1 diabetes. As a result, two Z. bungeanum extracts were deemed active, leading to the identification of eight compounds, of which compound 7 [(2E,4E,8E,10E,12E)-N-isobutyl-2,4,8,10,12-tetradecapentaenamide, γ-sanshool] was obtained as a promising lead compound.

Cannabinoid (CB) receptors are being targeted therapeutically for the treatment of anxiety, obesity, movement disorders, glaucoma, and pain. More recently, cannabinoid agonists have displayed antiproliferative activity against breast cancer and prostate cancer in animal models. To study cannabinoid receptor ligands, we have developed a novel plate-based assay that measures internalization of CB1/CB2 receptors by determining the change in the intracellular levels of the radiolabeled agonists: [(3)H]Win55-212-2 for CB1 and [(3)H]CP55-940 for CB2. The developed plate-based assay was validated by determining IC50 values for known antagonists: AM251, AM281, AM630, and AM6545. The data obtained were consistent with previously reported values, thereby confirming that the assay can be used to determine the functional binding activities (IC50) of antagonists for the CB1 and CB2 receptors. In addition, we demonstrated that the plate-based assay may be used for screening against complex matrices. Specifically, we demonstrated that the plate-based assay was able to identify which extracts of several species of the genus Zanthoxylum had activity at the CB1/CB2 receptors., (Published by Elsevier Inc.)

Bioassay-guided phytochemical investigation of Zygogynum calothyrsum using the human colon carcinoma cell lines COLO205 and KM12 led to the isolation of three new drimane-type sesquiterpenoids, 1β-p-hydroxy-E-cinnamoyldrimeninol (1), 1β-p-hydroxy-E-cinnamoyl-5α-hydroxydrimeninol (2), and methyl ether of 1β-p-hydroxy-E-cinnamoyl-12α-methoxydrimeninol (3). Also isolated was the known 1β-p-coumaroyloxypolygodial (4) together with two new tetralones, 3'-deoxyisozygolone A (5) and calothyrlone A (9), three known tetralones, isozygolone A (6), zygolone A (7), and 4'-O-methylzygolone A (8), and a known cinnamolide (10). Compounds 1, 7, and 8 demonstrated higher cytotoxicity against COLO205 (GI50 18, 17, and 11 μM, respectively) and KM12 (GI50 14, 14, and 17 μM, respectively) than the other compounds.

A neurofibromatosis type 1 (NF1)-based bioassay-guided phytochemical investigation on Zanthoxylum armatum collected in Nepal led to the isolation of new timuramides A-D (1-4) and six known sanshools (5-10). The structures of all compounds were established by using modern spectroscopic techniques, including 1D and 2D NMR analysis and comparison with previously reported data. Most of the compounds inhibited growth of an Nf1- and p53-deficient mouse glioma cell line at noncytotoxic concentrations.

The methanol extract of dried fruits of Odyendyea gabonensis afforded one new quassinoid [(-)-odyendanol (1)], one new canthin-6-one alkaloid [9-hydroxy-5-methoxycanthin-6-one (4)], and two new steroids [22E, 24R-stigmasta-5,22-diene-3,7-dione (7) and 22E,24R-stigmast-22-ene-3,7-dione (8)] along with fourteen known compounds. The structures of all compounds were established by analyzing the spectroscopic data. The ¹³C-NMR values of (-)-odyendene (2) and (-)-odyendane (3), as well as the single-crystal X-ray structure of 5-methoxycanthin-6-one (6) are also reported.The oxidative burst inhibitory activity of pure compounds 1-12 was determined by the chemoluminescence assay, and cytotoxic activities of compounds 2-6 against the human prostate cancer cell PC-3 line were evaluated. Compounds 1-6 exhibited a clear suppressive effect on the phagocytosis response upon activation with serum-opsonized zymosan in the range of IC₅₀ = 0.9-2.0 µM versus ibuprofen with IC₅₀ = 12.1 µM, while all canthin-6-one alkaloids (4-6) displayed moderate cytotoxic activity against the human prostate cancer cell PC-3 line, with IC₅₀ values ranging from 13.5-15.4 µM versus doxorubicine with IC₅₀ = 1.5 µM., (Georg Thieme Verlag KG Stuttgart · New York.)

Three new β-indoloquinazoline alkaloids, orirenierine A (1), B (2) and C (4), together with eleven known compounds were isolated from the methanol extract of the stems of Oricia renieri. The structures of all compounds were determined by comprehensive analyses of their spectroscopic data and comparison with literature information. The alkaloids 9-11 were isolated for the first time from this genus. All compounds were tested for their activity against bacteria, fungi, and plant pathogen oomycetes using the paper disk agar diffusion assay. The agar diffusion test gave only low antimicrobial activities, corresponding to MICs > 1 mg/mL. However, compounds 1-4 and 11 exhibited a strong suppressive effect on phagocytosis response upon activation with serum opsonized zymosan in the range of IC(50) = 2.6-6.5 µM, while low cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3 was observed with IC(50) values ranging from 22.9 to 39.4 µM., (© Georg Thieme Verlag KG Stuttgart · New York.)

An activator protein-1 (AP-1) based bioassay-guided phytochemical investigation on Podocarpus latifolius led to the isolation of three new sempervirol-type diterpenes, cycloinumakiol (1), inumakal (2), and inumakoic acid (3), along with three known norditerpenes (4-6). Compounds 4 and 6 were responsible for the observed bioactivity.

Bioassay-guided fractionation of the fruit pericarp of Pentadesma butyracea, using the antiplasmodial test, led to the isolation of a new xanthone, named pentadexanthone (1), together with six known compounds: cratoxylone (2), α-mangostin (3), 1,3,5-trihydroxy-2-methoxyxanthone (4), garcinone E (5), (-)-epicathechin (6), and lupeol (7). The structure of 1 was elucidated by spectroscopic data analysis. An antiplasmodial assay was performed with the isolates, in which compounds 1- 3 and 5 exhibited potent activity in vitro against Plasmodium falciparum chloroquine-resistant strain W2, with IC₅₀ values below 3 µM., (© Georg Thieme Verlag KG Stuttgart · New York.)

Ethnopharmacological Relevance: Vitex cienkowskii Kotschy & Peyritsch is a deciduous tree, prescribed by Cameroonian traditional healers as one of the most popular plant widely used in many disorders including cardiovascular diseases. The preliminary pharmacological studies carried out on Vitex cienkowskii showed its vasorelaxant activities on guinea-pig aortic rings., Aim of the Study: The present work evaluated the vasorelaxant activity of extract and isolated compounds from Vitex cienkowskii., Materials and Methods: Rat aortic rings were used to evaluate the in vitro vascular effect of the extract. The antioxidant activity was determined by measuring the reduction of the free radical 1,1-diphenyl-1-picryl-hydrazyl (DPPH)., Results: Vitex cienkowskii induced significant relaxation in a concentration- and endothelium-dependent manner (EC(50)=12.12 μg/ml, CH(2)Cl(2)-MeOH, 1:1) and did not produce a vasorelaxant effect on contraction evoked by KCl (60 mM). In order to determine its mode of action, Vitex cienkowskii-induced relaxant effect was evaluated in the presence of indomethacin (10 μM), L-NAME (100 μM), ODQ (1 μM) and SQ22356 (100 μM). Relaxation was significantly blocked by L-NAME and ODQ. These results indicate that Vitex cienkowskii-mediated relaxation is endothelium dependent, probably due to NO release, and the consequent activation of vascular smooth muscle soluble guanylate cyclase (sGC), a signal transduction enzyme that forms the second messenger cGMP. Bio-guided study of Vitex cienkowskii allowed the isolation of the known pentacyclic triterpenoids and a ceramide. It is the first report of salvin A, maslinic acid and a ceramide from Vitex cienkowskii. The activity induced by these compounds indicated that they may be partly responsible for the vasorelaxant effect of the plant extract. A dose of 40 mg/kg of CH(2)Cl(2)-MeOH (1:1) extract administered intravenously induced a decrease of mean arterial pressure but did not affect the heart rate. Moreover the plant extracts were found to be highly active in the DPPH radical scavenging assay., Conclusion: Vitex cienkowskii extract possesses antioxidant property, vasorelaxing, and hypotensive effect linked to the endothelium related factors, where nitric oxide is involved., (Copyright © 2010 Elsevier Ireland Ltd. All rights reserved.)

Bioassay-guided fractionation of the methanol extract of the stem bark of Klainedoxa gabonensis Pierre ex Engl. (Irvingiaceae) afforded 12 compounds, namely, ellagic acid (1), ellagic acid 3,3'-dimethylether (2), gallic acid (3), methyl gallate (4), lupeol (5), β-amyrin (7), erythrodiol (8), oleanolic acid (9), betulinic acid (6), hederagenin (10), bayogenin acid (11), and stigmasterol-3-O-β-d-glucopyranoside (12). Compounds 1-3 and 7-12 were isolated for the first time from this genus. The structures were established on the basis of 1D/2D NMR experiments and mass spectrometric data. Crude extract, fractions (A, B, C and D) and pure compounds were tested for their antimicrobial activity using paper disk agar diffusion assay. The test delivered a range of low to high activities for phenolic compounds 1-4, low or missing activities for terpenoid compounds 5-11, and impressive very high antibacterial/antifungal values for two fractions C and D probably due to synergistic effects of compounds. The broth microdilution assay revealed MICs of 15.4-115.1 μg/mL for phenolic compounds, MICs higher than 1 mg/mL for terpenoids and MICs of 4.5-30.3 μg/mL for fractions C and D. The determination of the radical scavenging activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay gave high antioxidant values for the methanol extract and fraction D (IC(50) 10.45 and 5.50 μg/mL) as well as for the phenolic compounds 1-4 (IC(50) 45.50-48.25 mM) compared to the standard 3-t-butyl-4-hydroxyanisole (BHA) (IC(50) 44.20 mM).

Phytochemical investigation of the stem bark of Beilschmiedia zenkeri led to the isolation of four new methoxylated flavonoid derivatives, (2S,4R)-5,6,7-trimethoxyflavan-4-ol (1), (2S,4R)-4,5,6,7-tetramethoxyflavan (2), beilschmieflavonoid A (3), and beilschmieflavonoid B (4), together with seven known compounds. The structures of 1-4 were established by spectroscopic methods, and their relative configurations confirmed by X-ray crystallographic and CD analysis. The isolated compounds were evaluated in vitro for their antibacterial activity against three strains of bacteria, Pseudomonas agarici, Bacillus subtilis, and Streptococcus minor, and for their antiplasmodial activity against Plasmodium falciparum, chloroquine-resistant strain W2.

One new tricyclic clerodane type diterpene aldehyde nepetanal (1) and one new benzene derivative nepetanoate (2) have been isolated from a plant Nepeta juncea together with two known compounds oleanolic acid (3) and ursolic acid (4). The structures of the isolated compounds were elucidated by means of modern spectroscopic techniques and comparison with literature data., (2009 John Wiley & Sons, Ltd.)

Five new amide alkaloids, N-(4-hydroxyphenethyl)octacosanamide (1), N-(4-hydroxyphenethyl)hexacosanamide (2), N-(4-hydroxyphenethyl)decanamide (3), N-vanilloyltyramine (4), and N-[O-docosanoylvanilloyl]tyramine (5), were isolated from Fagara macrophylla, together with 15 known compounds. Their structures were established by using spectroscopic techniques, chemical reactions, and comparison with previously known analogues. A cytotoxicity assay was performed with the isolates, in which compounds 4, 8, and 9 were found to possess moderate to weak activity, with IC(50) values of 30.5, 11.5, and 13.5 microg/mL, respectively.

Three endiandric acid derivatives, beilschmiedic acids A, B and C were isolated from the stem bark of Beilschmiedia anacardioides together with the known beta-sitosterol. Their structures were established by means of modern spectroscopic techniques. The relative configuration of compound 1 was determined by single crystal X-ray analysis. The antibacterial activities of compounds A,B,C were evaluated in vitro against five strains of microbes. Compound C showed strong activity against Bacillus subtilis, Micrococcus luteus and Streptococcus faecalis (MICs below 23 microM). This Compound was more active than the reference antibiotic ampicillin against B. subtilis and M. luteus.

Two new β-indoloquinazoline alkaloids, orisuaveoline A (1) and orisuaveoline B (2), two new furoquinoline alkaloids, quinosuaveoline A (5) and quinosuaveoline B (6), and 12 known compounds were isolated from Oricia suaveolens. The structures of the new compounds were deduced by spectroscopic studies. The absolute configuration of nkolbisine (4) was also determined. Compounds 2, 3, 6-8, 10, and 14 were evaluated for oxidative burst inhibitory activity in a chemoluminescence assay and for cytotoxicity against A549 lung carcinoma cells.

The bioassay-guided phytochemical investigation of Sarcococca hookeriana with respect to cholinesterase inhibitory properties has yielded two new 5alpha-pregnane-type steroidal alkaloids, hookerianamides J (1) and K (2), along with eight known compounds (3-10). The structures of 1 and 2 were elucidated by spectroscopic methods. These compounds displayed good to moderate activities in vitro against the enzymes acetylcholinesterase (IC 50 8.1-48.5 microM) and butyrylcholinesterase (IC 50 0.4-4.0 microM). Compounds 1-10 were also tested in vitro for their leishmanicidal activity against Leishmania major and for their antibacterial activities against Bacillus subtilis, Micrococcus luteus, Streptococcus faecalis, and Pseudomonas pallida.

The plants of the family Buxaceae are widely used in traditional medicine and constitute rich sources of terpenoidal alkaloids. Compounds of this family have been the subject of numerous chemical and pharmacological studies over past decades because of their interesting biological activities such as cholinesterase inhibition, as well as antibacterial and antileishmanial activities. The chemical and biological properties of these alkaloids, including data relevant to straightforward structure determination and information on biosynthesis, are highlighted in this review, with 144 references being cited.

Glaberianthrone (1), a new bianthrone was isolated from the hexane extract of the stem bark of Psorospermum glaberrimum together with thirteen known compounds: 3-geranyloxyemodin anthrone (2), friedelan-3-one (3), 3-prenyloxyemodin anthrone (4), 3-geranyloxyemodin (5), 3-prenyloxyemodin (6), friedelan-3-ol (7), acetylvismione D (8), betulinic acid (9), 2-geranylemodin (10), bianthrone A2b (11), bianthrone 1a (12), emodin (13) and 2-prenylemodin (14). The structures of the isolated compounds were established by means of spectroscopic methods. The extracts and the isolated compounds were tested in vitro for their anti-plasmodial activity against Plasmodium falciparum (chloroquine resistant strain W2) and for their acetyl- and butyrylcholinesterase inhibitory properties. The n-hexane extract showed good anti-plasmodial activity against P. falciparum W2 strain, with IC(50) of 0.87 microg/ml. It also exhibited 65.5% and 98.2% of acetyl- and butyrylcholinesterase inhibition at 0.2 mg/ml, respectively. Compounds 2 and 8 showed the best potencies against P. falciparum W2 strain with IC(50) of 1.68 microM and 0.12 microM, (0.66 microg/ml and 0.054 microg/ml) respectively. All tested compounds showed good butyrylcholinesterase inhibition activities with compound 12 displaying the best potency (IC(50) 9.25+/-0.25 microM). All the tested compounds showed weak inhibitory activity against acetylcholinesterase.

Bioguided phytochemical investigation of Sarcococca hookeriana with respect to the cholinesterase enzyme inhibitory assay yielded two new pregnane-type steriodal alkaloids hookerianamide H (1) and hookerianamide I (2), along with three known alkaloids N(a)-methylepipachysamine D (3), sarcovagine C (4) and dictyophlebine (5). Their structures were determined with the aid of extensive spectroscopic analysis. All compounds showed good inhibitory activities against the enzymes acetylcholinesterase (IC(50) 2.9-34.1 microM) and butyrylcholinesterase (IC(50) 0.3-3.6 microM). These compounds also showed moderate antiplasmodial activity (IC(50) 2.4-10.3 microM) against the Plasmodium falciparum chloroquine resistant W2 strain.

In a preliminary antiprotozoal screening of several Clusiaceae species, the methanolic extracts of Allanblackia monticola and Symphonia globulifera showed high in vitro leishmanicidal activity. Further bioguided phytochemical investigation led to the isolation of four benzophenones: guttiferone A (1), garcinol (2), cambogin (3) and guttiferone F (4), along with three xanthones: allanxanthone A (5), xanthone V1 (6) and globulixanthone C (7) as active constituents. Compounds 1 and 6 were isolated from S. globulifera leaves, while compounds 2-5 were obtained from A. monticola fruits. Guttiferone A (1) and F (4) showed particulary strong leishmanicidal activity in vitro, with IC50 values (0.2 microM and 0.16 microM, respectively) comparable to that of the reference compound, miltefosine (0.46 microM). Although the leishmanicidal activity is promising, the cytotoxicity profile of these compounds prevent at this state further in vivo biological evaluation. In addition, all the isolated compounds were tested in vitro for their anticholinesterase properties. The four benzophenones showed potent anticholinesterase properties towards acetylcholinesterase (AChE) and butylcholinesterase (AChE). For AChE, the IC50 value (0.66 microM) of garcinol (2) was almost equal to that of the reference compound galanthamine (0.50 microM). Furthermore, guttiferone A (1) and guttiferone F (4) (IC50 = 2.77 and 3.50 microM, respectively) were more active than galanthamine (IC50 = 8.5) against BChE.

Two anthraquinones, zenkequinones A and B were isolated from the stem bark of Stereospermum zenkeri together with known sterequinone-F, p-coumaric acid, sitosterol-3-O-beta-D-glucopyranoside and 3beta-hydroxyolean-12-en-28-O-beta-D-glucopyranoside. Their structures were established by spectroscopic methods. The antimicrobial activity of the isolated compounds was evaluated against six multiresistant strains of pathogens. Zenkequinone B showed the best antibacterial activity (MIC 9.50 microg/ml) against gram-negative Pseudomonas aeruginosa.

The search for antileishmanial constituents from the medicinal plant Sarcococca hookeriana (Buxaceae) of Nepalese origin has resulted in the isolation of 17 (1-17) active steroidal alkaloids. Compounds 1, 2, and 10 were subjected to derivatization and five chemically derived derivatives (1a, 2a, 10a, 10b, 10c) were also obtained. All these natural compounds and derivatives were found to have potent to mild antileishmanial properties. The IC(50) values were found to be in the range of 0.20-61.44 microg mL(-1) (IC(50) value of standard drug amphotericin B = 0.12 microg mL(-1)). The structure activity relationship indicated that the varieties of functionalities present in ring A of the steroidal alkaloids were found to play a characteristic role to increase the antileishmanial activity.

The microbial transformation of a steroidal alkaloid, dictyophlebine (1) with Rhizopus stolonifer (ATCC 10404) afforded three oxidized metabolites 2-4. Compound 2 was found to be a new product. These metabolites were structurally characterized on the basis of modern spectroscopic techniques. Their inhibitory activity towards acetyl- and butyrylcholinesterase has been evaluated and the new product 2 has been found to be more potent than the parent compound and other metabolites.