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Ximenia americana, Vitex doniana and Lophira lanceolata are species prized by the populations of the Guinean savannah highlands of Cameroon. They are unfortunately still in the wild where they are subjected to various pressures. From the perspective of the conservation and enhancement of local biodiversity, their domestication appears necessary. The objective of the work is to study the vegetative propagation by air layering of these fruit trees. The experimental device used is a split-split-plot with three repetitions. Species represents the main treatment; the substrates constitute the secondary treatment while the covering of the layers wit h aluminum foil represents the tertiary treatment. The experimental unit was 30 layers. The rooting rate of layers varies significantly (0.000<0.001) from 48.88±1.89% in Ximenia americana to 81.38±2.08% in Lophira lanceolata. Sphagnum was the best substrate with 69.63±1.38% against 61.66±1.54% for the black soil-sawdust mixture. The analysis of variance reveals a significant difference for the substrates (0.0025<0.01). Covering the layers with aluminum foil presented a rate of 69.44±2.15% while the uncovered layers presented 61.85±1.54%, the analysis of variance shows a significant difference (0,0031<0.01). Lophira lanceolata exhibited the best air layering ability; the rooted layers were weaned and acclimatized for two months before being transferred to the field. During this process 19% and 52% respectively of the layers of Vitex doniana and Ximenia americana flowered. This inexpensive technique is an essential step in the process of their domestication. [ABSTRACT FROM AUTHOR]

Resistance of human malaria parasites to existing chemotherapeutic drugs remains a global challenge to malaria control. This study was an evaluation of the gametocyte dynamics and the potential roles of aqueous and ethanolic leaf extracts of Lophira lanceolata in the transmission of Plasmodium parasites using mice experimentally infected with P. berghei as a model. A total of 192 experimental mice divided into 15 groups in a randomized block design and replicated four times with four mice in each group were used for this study. Thirty-six (36) mice were used for acute toxicity test, 32 mice each for curative antiplasmodial assay, prophylactic assay and gametocyte evaluation, and analyses. Experimental mice were inoculated intraperitoneally with standard inoculum of 1 x 107P.berghei parasitized red blood cells on first day (DO). Body weights of mice were taken using sensitive digital weighing balance. Blood sample was collected by cardiac puncture using sterile needle and 5ml syringe and preserved in ethylene diaminetetraacetic acid (EDTA) bottle. Haematological components were determined using an autohaematology analyzer SYSMEX KX21. Data analysis was done using student's t-test and one way analysis of variance with multiple comparison tests. Phytochemical screening revealed the presence of phenols, terpenoids, tannins, saponins, alkaloids, flavonoids, steroids, oxalates and cardiac glycosides. The flavonoids had the largest concentrations of 388.24mg/ml, and 350.00mg/ml in ethanolic and aqueous extracts respectively. LD50 was found to be ≥ 5000mg/kg body weight in both extracts. At ≥ 100mg/kg body weight, infected treated mice experienced body weight increases while infected untreated mice experienced decreases in mean body weight from 23.33g to 20.08g (mean 10% weight loss). Aqueous and ethanolic leaf extracts produced variations in number of gametocyte from mice infected with P.berghei. On days 7, 14, 21, and 28, the mean gametocytes of the parasite in the control group were 18, 21, 22, and 20 respectively which were significantly (p < 0.05) higher compared with the mean gametocytes in the groups of mice treated with aqueous extract, ethanolic extract and chloroquine drugs. The dose level of 10mg/kg body weight of aqueous extract produced the mean gametocyte counts of 10, 10, 8 and 6 on days 7, 14, 21 and 28 respectively which were significantly (p < 0.05) lower than the mean gametocyte counts of the control. [ABSTRACT FROM AUTHOR]

Objectives: The present study sought to establish quality control parameters of a locally and ubiquitously occurring medicinal plant, Lophira lanceolata which is utilized as folk medicine among the local communities in Northern Nigeria as well as other regions, due to its therapeutic indication mainly as an aphrodisiac, among other uses. Materials and Methods: Pharmacognostically, different types of evaluations were carried out that focuses on organoleptic, macroscopic, microscopic, chemical evaluations as well as heavy metal assessments using Atomic Absorption Spectroscopy (AAS). Results: Organoleptic and macroscopic studies revealed some features of the leaves as green and oblanceolate, pinnate venation, with an average leaf size length and width of 14-15 and 4-5 cm respectively. The root has a light pale-brown outer surface and a reddish-brown inner surface. The outer surface was soft and dry while the inner surface was moist and smooth. Leaf microscopy indicated the presence of anisocytic or cruciferous type of stomata while both the rootbark and leaves are not devoid of common ergastic cell contents of calcium oxalate, lignin, starch, protein and tannin. Phytochemical evaluations revealed abundance of phytoconstituent that are richly phenolic of the types of saponin, tannin, triterpenoid, flavonoid, glycosides, diterpenoids, alkaloid, steroid, anthraquinones and phenols etc. Physicochemical evaluations showed a good source of mineral content of carbohydrate (35.93 ± 1.9199 for leaves and 33.58 ± 1.6791 for rootbark), Ash (9.33 ± 0.4714 for leaves and 7.17 ± 0.2358 for rootbark) in the plant. Heavy metal analysis of the leaves and rootbark investigated for Cadmium, Copper, Lead and Mercury showed that their concentrations were within the WHO (2002) permissible limits. Conclusion: This study provides the scientific data for the proper identification and establishment of standards for the use of the plant, Lophira lanceolata (False shea). [ABSTRACT FROM AUTHOR]

Abstracts Background Chemotherapy is associated with male infertility. Cisplatin (CP), an antineoplastic agent has been successfully used for the treatment of diverse kinds of malignancies, however, the use of this effective agent could induce oxidative stress injury, nephrotoxicity, hepatotoxicity, and testicular damage. Combined CP chemotherapy with plant extracts can diminish the toxicity and enhance the antitumor efficacy of the drug. The objective of the study was to determine the protective effect Lophira lanceolata leaf extract (LLLE) on CP-induced toxicity on male reproductive organs. Methods The study was carried out with 30 (n = 30) male Wistar rats (Rattus norvegicus). The rats were randomly assigned into 6 groups of 5 rats each. Rats in group 1 (Control) were administered distilled water per os. Rats in group 2 were administered 5 mg/kg of CP intraperitoneally (i.p). Rats in groups 3 and 4 were administered per os LLLE at the doses of 200 and 400 mg/kg body weight and rats in groups 5 and 6 were administered 5 mg/kg body weight of CP + LLLE at the doses of 200 and 400 mg/kg body weight respectively. Results The results showed a significant decrease in the sperm parameters in the group treated with CP alone when compared with the control and there in the sperm parameters in the groups administered CP + LLLE. The body and organ weights of the rats were significantly (p

Background: This study was to determine the effects of Lophira lanceolata leaf extracts on haematological, biochemical, and histopathological parameters of the mice in the transmission of Plasmodium parasites using mice infected with P.berghei as a model. A total of 196 experimental mice divided into 15 groups in a randomized block design and replicated four times with four mice in each group were used for this study. Thirty six (36) mice were used for acute toxicity test, 50 each for haematological, biochemical, and histopathological analyses. Experimental mice were inoculated intraperitoneally with standard inoculum of 1 x 107 P.berghei parasitized red blood cells on first day (DO). Results: Data analysis was done using student's t-test and one way analysis of variance with multiple comparison tests. Aqueous leaf extract exerted significant (p < 0.05) non-dose dependent reduction in parasitaemia level with chemosuppression of 48.79%, 24.26%, 29.38% and 80.32% at 10, 100, 200 mg/kg body weight and 5mg/kg body weight chloroquine treated groups respectively. Dose level of 10, 100, 200 mg/kg body weight of both aqueous and ethanolic leaf extract produced significant increase in aspartate amino transferase, alanine amino transferase, total bilirubin, cholesterol, triglycerides and urea profiles of infected treated mice compared with the control. At 200mg/kg body weight of aqueous extract there was a significant decrease (p < 0.05) in weight of liver and kidney organs in the infected treated mice compared with the control. The results of histopathological examinations of the liver organs of the mice were characterized by tissue stromal proliferation, enlarged hepatocytes and disorganized sinusoids and lamina of hepatic cells. The results of histopathological examination of kidneys showed no histopathological changes. The aqueous and ethanolic leaf extracts of Lophira lanceolata plant showed significant antiplasmodium activities comparable to chloroquine drugs. Conclusions: The leaf extracts of Lophira lanceolata plant had gametocytocidal action on P. berghei. The results of the haematological, biochemical and histopathological examinations indicated that caution should be exercised while taking the plant extract as an antimalarial agent. [ABSTRACT FROM AUTHOR]

This study focused on wood extractives by a slow pyrolysis thermal extraction technique and screening of potentially valuable compounds from three African trees: Lophira lanceolata Tiegh. ex Keay., Dialium guineense Willd. and Afzelia africana Sm. The primary objective of the thermal treatment was biochar production but also liquids were collected and analyzed. Raw materials were cut into sizes of about 25 cm in length and then processed with slow pyrolysis from 20 °C up to 400 °C; the slow pyrolysis process included two stages, drying and pyrolysis. Five end-point temperatures were used in the range of 250 °C–400 °C. Raw distillates were collected at three temperatures (120 °C, 60 °C and 25 °C) and their composition screened by either cost-effective FTIR or benchtop 80 MHz 1H NMR methods. HR-NMR and 2D GC–MS were used to confirm some findings. Results from the drying stage indicated that all distillates contained mostly water >90%, acetic acid, methanol and some other compounds at very low levels. The percentages of acetic acid were 3.5% for L. lanceolate, 2.8% for D. guineensis and 3.8% for A. africana (% with respect to the identified peaks). Results from the pyrolysis stage revealed the presence of bioactive compounds such as ketones, methanol, hydrocarbons, acetic acid, esters, alkenes and phenolic compounds at higher quantities than in the drying stage. The quantity of phenols in certain runs and distillate fractions using NMR was 1%–20% for L. lanceolata, 7–17% for D. guineensis and 10%–17% for A. africana (% with respect to the composition of the identified peaks). The percentage of hydrocarbons was 1%–48% for L. lanceolata, 1%–34% for D. guineensis and 2%–33% for A. africana. The percentage of ketones was 7%–19% for L. lanceolate, 4%–27% for D. guineensis and 19%–22% for A. africana. In general, the results indicated the presence of potential valuable compounds at relatively high concentrations. By optimizing the slow pyrolysis process parameters, it is possible to collect distillates with high concentrations of valuable biomolecules.

Background: Chemotherapy is associated with male infertility. Cisplatin (CP), an antineoplastic agent has been successfully used for the treatment of diverse kinds of malignancies, however, the use of this effective agent could induce oxidative stress injury, nephrotoxicity, hepatotoxicity, and testicular damage. Combined CP chemotherapy with plant extracts can diminish the toxicity and enhance the antitumor efficacy of the drug. The objective of the study was to determine the protective effect Lophira lanceolata leaf extract (LLLE) on CP-induced toxicity on male reproductive organs. Methods: The study was carried out with 30 (n = 30) male Wistar rats (Rattus norvegicus). The rats were randomly assigned into 6 groups of 5 rats each. Rats in group 1 (Control) were administered distilled water per os. Rats in group 2 were administered 5 mg/kg of CP intraperitoneally (i.p). Rats in groups 3 and 4 were administered per os LLLE at the doses of 200 and 400 mg/kg body weight and rats in groups 5 and 6 were administered 5 mg/kg body weight of CP + LLLE at the doses of 200 and 400 mg/kg body weight respectively. Results: The results showed a significant decrease in the sperm parameters in the group treated with CP alone when compared with the control and there in the sperm parameters in the groups administered CP + LLLE. The body and organ weights of the rats were significantly (p < 0.05) decreased in the CP treated group relative to the control. However, there was an increase in the weight of the organs in the LLLE pretreated groups. The photomicrographs showed degenerative changes in the testicular tissues of the rats administered CP alone whereas the group pretreated with the LLLE showed amelioration induced by the CP. Our study revealed that CP treatment has deleterious effects on sperm parameters and testicular tissues and the accessory sex organs (Epididymis, prostate, seminal vesicles) of the rats. Oral administration of LLLE at 200 and 400 mg/kg bodyweight for 26 days conferred protective effects against testicular damage induced by CP. Conclusion: This study revealed that pretreatment with LLLE protected against CP-induced testicular toxicity. [ABSTRACT FROM AUTHOR]

Abstract Background Onchocerciasis is one of the tropical neglected diseases (NTDs) caused by the nematode Onchocerca volvulus. Control strategies currently in use rely on mass administration of ivermectin, which has marked activity against microfilariae. Furthermore, the development of resistance to ivermectin was observed. Since vaccine and safe macrofilaricidal treatment against onchocerciasis are still lacking, there is an urgent need to discover novel drugs. This study was undertaken to investigate the anthelmintic activity of Lophira lanceolata on the cattle parasite Onchocerca ochengi and the anthelmintic drug resistant strains of the free living nematode Caenorhabditis elegans and to determine the phytochemical profiles of the extracts and fractions of the plants. Methods Plant was extracted in ethanol or methanol-methylene chloride. O. ochengi, C. elegans wild-type and C. elegans drug resistant strains were cultured in RPMI-1640 and NGM-agar respectively. Drugs diluted in dimethylsulphoxide/RPMI or M9-Buffer were added in assays and monitored at 48 h and 72 h. Worm viability was determined by using the MTT/formazan colorimetric method. Polyphenol, tannin and flavonoid contents were determined by dosage of gallic acid and rutin. Acute oral toxicity was evaluated using Swiss albino mice. Results Ethanolic and methanolic-methylene chloride extracts killed O. ochengi with LC50 values of 9.76, 8.05, 6.39 μg/mL and 9.45, 7.95, 6.39 μg/mL respectively for leaves, trunk bark and root bark after 72 h. The lowest concentrations required to kill 50% of the wild-type of C. elegans were 1200 and 1890 μg/mL with ethanolic crude extract, 1000 and 2030 μg/mL with MeOH-CH2Cl2 for root bark and trunk bark of L. lanceolata, respectively after 72 h. Leave extracts of L. lanceolata are lethal to albendazole and ivermectin resistant strains of C. elegans after 72 h. Methanol/methylene chloride extracted more metabolites. Additionally, extracts could be considered relatively safe. Conclusion Ethanolic and methanolic-methylene chloride crude extracts and fractions of L. lanceolata showed in vitro anthelmintic activity. The extracts and fractions contained polyphenols, tannins, flavonoids and saponins. The mechanism of action of this plant could be different from that of albendazole and ivermectin. These results confirm the use of L. lanceolata by traditional healers for the treatment of worm infections.

Background: Onchocerciasis is one of the tropical neglected diseases (NTDs) caused by the nematode Onchocerca volvulus. Control strategies currently in use rely on mass administration of ivermectin, which has marked activity against microfilariae. Furthermore, the development of resistance to ivermectin was observed. Since vaccine and safe macrofilaricidal treatment against onchocerciasis are still lacking, there is an urgent need to discover novel drugs. This study was undertaken to investigate the anthelmintic activity of Lophira lanceolata on the cattle parasite Onchocerca ochengi and the anthelmintic drug resistant strains of the free living nematode Caenorhabditis elegans and to determine the phytochemical profiles of the extracts and fractions of the plants. Methods: Plant was extracted in ethanol or methanol-methylene chloride. O. ochengi, C. elegans wild-type and C. elegans drug resistant strains were cultured in RPMI-1640 and NGM-agar respectively. Drugs diluted in dimethylsulphoxide/RPMI or M9-Buffer were added in assays and monitored at 48 h and 72 h. Worm viability was determined by using the MTT/formazan colorimetric method. Polyphenol, tannin and flavonoid contents were determined by dosage of gallic acid and rutin. Acute oral toxicity was evaluated using Swiss albino mice. Results: Ethanolic and methanolic-methylene chloride extracts killed O. ochengi with LC50 values of 9.76, 8.05, 6. 39 µ g/mL and 9.45, 7.95, 6.39 µ g/mL respectively for leaves, trunk bark and root bark after 72 h. The lowest concentrations required to kill 50% of the wild-type of C. elegans were 1200 and 1890 µg/mL with ethanolic crude extract, 1000 and 2030 µg/mL with MeOH-CH2Cl2 for root bark and trunk bark of L. lanceolata, respectively after 72 h. Leave extracts of L. lanceolata are lethal to albendazole and ivermectin resistant strains of C. elegans after 72 h. Methanol/methylene chloride extracted more metabolites. Additionally, extracts could be considered relatively safe. Conclusion: Ethanolic and methanolic-methylene chloride crude extracts and fractions of L. lanceolata showed in vitro anthelmintic activity. The extracts and fractions contained polyphenols, tannins, flavonoids and saponins. The mechanism of action of this plant could be different from that of albendazole and ivermectin. These results confirm the use of L. lanceolata by traditional healers for the treatment of worm infections. [ABSTRACT FROM AUTHOR]

Nontimber forest products are a source of income for women in rural African communities. However, these products are frequently damaged by insect pests. The present study investigates the diversity and damage rates of insect pests that attack Carapa procera seeds and Lophira lanceolata fruits. The experiment was set up in western Burkina Faso and, for C. carapa, consisted of pests collected from seeds that had fallen to the ground and from stockpiled seeds. For L. lanceolata, pests were collected from fruits on the trees, and on the ground. The collected samples were sent to the laboratory to estimate the proportion of damaged seeds/fruits and rear the insects. The results showed that Ephestia spp., Tribolium castaneum, Oryzeaphilus spp., and Tenebroides mauritanicus were the pests of Carapa procera seeds and Lophira lanceolata fruits. Ephestia spp. was recorded as the main pest of both C. procera and L. lanceolata, whereas T. castaneum was only detected from seeds of L. lanceolata. For C. procera, the stocks were the most infested (29 %) by Ephestia spp. The infestation rate of fruits of L. lanceolata by Ephestia spp. on trees (31.42 ± 3.75 %) was less than the rate of fruits by T. castaneum on the ground (44.00 ± 3.5 %). The different body sizes of Ephestia spp. may indicate the occurrence of two putative species, one from C. procera and another one from L. lanceolata. This work provides important information that could contribute to the setting up of a local-scale sustainable management framework for oil tree pests in Burkina Faso and surrounding countries. [ABSTRACT FROM AUTHOR]

Non Timber Forest Products play an important role as source of food and income generation in developing countries. In Burkina Faso, many wild tree species provide various useful products, among them the local oil tree, Lophira lanceolata which occurs in the western part of the country. This study aimed at assessing the habitat diversity and population structure of L. lanceolata's natural stands according to land cover types. Two sites were considered: Banfora, where the use value of fruits is unknown and Orodara, where fruits are exploited for oil production. A stratified and oriented sampling scheme based on the occurrence of L. lanceolata and land cover was applied using rectangular plots of 50 m × 20 m. Phytosociological and quantitative inventories were carried out to assess the woody species diversity of stands and L. lanceolata population structure, respectively. Species diversity indices, structural parameters were computed and analyses of variance, Chi square test were performed to compare sites according to land cover types. The results showed high woody species diversity associated with L. lanceolata stands (H = 3.2-3.6). The densities of L. lanceolata ranged between 94 and 280 trees per hectare, with significant differences between land cover types and sites. The population pattern showed a good regeneration potential and high resource availability. L. lanceolata was fairly resilient to human pressure and tended to recolonize disturbed lands. With a high potential for sustainable management, L. lanceolata is a promising NTFP species which can contribute to improve the local and national economy. [ABSTRACT FROM AUTHOR]

Lophira lanceolata seeds are used by Waama ethnic people in Benin to extract oils. We aimed to evaluate the chemical profiles (fatty acids, tocols and sterols) of the oil obtained following the ancestral process. Two extraction methods (enzymes-assisted aqueous extraction) and organic solvent method, were used to compare the oil properties. The impact of the roasting of seeds in ancestral process was also evaluated. The oil obtained following the ancestral process has shown good chemical parameters with brilliant colors. Results also revealed that all oils are rich in polyunsaturated fatted acids with α-linoleic (>30% w/w) and arachidonic (>14% w/w) acids as majors. Enzymes and roasting of the seeds induced lauric, eicosapentaenoic and adrenic acids formations in oils. The presence of tocols and phytosterols, determined by LC–MS/APCI+, may explain the therapeutic use of these oils in rural area. [ABSTRACT FROM AUTHOR]

Decoction of Lophira lanceolata known in Hausa as Namijin Kadanya has been used by many communities in northern Nigeria for the treatment of various ailments, commonest of which is epilepsy. The current study is aimed at evaluating the claim of this medicinal plant part by herbalist for the treatment of epilepsy. A preliminary phytochemical screening was performed on the stem bark extract after which intraperitoneal LD50 was determined in mice. Anticonvulsant screening was carried out using Maximal electroshock Test (MEST) and pentylenetetrazole (PTZ) in one day old chicks and mice respectively. Flavonoids, saponins, tannins and glycosides were found to be present. The intraperitoneal LD50 in mice was found to be 1131.31 mg/kg. There was no significant prolongation in the latency of seizures or protection in both the MEST and PTZ model. Conversely, a significant (p≤0.05) delay in the mean onset of seizures was recorded with standard drugs, sodium valproate (200 mg/kg) and phenytoin (40 mg/kg) in PTZ and MEST respectively. The findings of this study revealed that the stem bark extract of Lophira lanceolata at the doses tested do not contain any bioactive constituents that is useful in the management of epilepsy. [ABSTRACT FROM AUTHOR]

Background: This study investigated the acute toxicity effect of aqueous stem bark extract of Lophira lanceolata and the activities of liver enzymes and other markers of organ damage in rats pretreated with aqueous stem bark extract of L. lanceolata extract and subsequently intoxicated with paracetamol (PCM). Methods: A total of 30 rats were used to determine the acute toxicity of aqueous extract of L. lanceolata stem. They were divided into six groups consisting of five rats each. The groups (A-F) were administered the increasing doses of the extract (500 mg/kg, 1,000 mg/kg, 2,000 mg/kg, 3,200 mg/kg, 4,000 mg/kg and 5,000 mg/kg) orally. The rats were observed over a period of 24 h for acute toxicity signs such as dullness, anorexia, morbidity and death. Thirty rats of mixed sexes randomly assigned to six groups (A-F) of five rats each were used for the study on the effects of L. lanceolata extract on the haematology, liver enzymes and markers of organ damage of extract-pretreated PCM-intoxicated rats. The rats in groups A-D were pretreated with 100 mg/kg, 200 mg/kg, 300 mg/kg of L. lanceolata extract and 100 mg/kg Silymarin, respectively, twice a day for 7 days. On the seventh day, all the rats in groups A-E received 1,000 mg/kg PCM ( per os). Group E rats served as negative control while group F rats were neither intoxicated nor treated with the extract and served as positive control. Eighteen hours after PCM intoxication, blood samples were collected for biochemical analyses. The serum activities of these enzymes (aspartate aminotransferase [AST], alanine aminotransferase [ALT], alkaline phosphatase [ALP]) and other markers of organ damages (bilirubin and total protein) were investigated. Haematologic parameters such as packed cell volume, red blood cell count, white blood cell count and haemoglobin concentration were also determined. Results: The extract did not cause any death in all the groups even at the highest dose (5,000 mg/kg body weight). The results also showed varying degrees in the activity of the enzymes in the serum in comparison with the negative control. The mean serum ALP, ALT and AST activity of group C (rats pretreated with 300 mg/kg of the extract and 1,000 mg/kg PCM) were significantly (p<0.05) lower than that of the group E (rats intoxicated with 1,000 mg/kg PCM only). The AST and ALP activities of groups C-E rats) were statistically comparable. The serum ALT activities of group C rats were significantly (p<0.05) lower than that of group E rats but were statistically comparable (p>0.05) with the group F counterpart. The bilirubin levels were significantly (p<0.05) lower in the groups pretreated with the extract and Silymarin in comparison with the D group. The total protein and the haematologic indices were not significantly different (p>0.05) across the groups. Conclusions: This study therefore showed that the aqueous stem bark extract of L. lanceolata possesses some active constituents that have antihepatotoxic potentials. [ABSTRACT FROM AUTHOR]

• Different methods and solvent extracts from Lophira lanceolata were investigated. • Antioxidant, cytotoxic and enzyme inhibitory effects were evaluated. • Lanceolatins and lophirones were identified in the extracts. • Stem bark extracts exhibited stronger biological propensities than leaf extracts. • The results might be valuable for designing novel bioproducts. Lophira lanceolata Tiegh. ex Keay, a native tropical plant to west and central Africa, is a multifunctional plant used as timber and also exploited in traditional medicine in Africa. The present study present the pharmacological properties of Lophira lanceolata leaf and stem bark extracts prepared from different extraction procedures (infusion, homogenizer‐assisted extraction, maceration, soxhlet). The detailed phytochemical composition, in vitro antioxidant and antiproliferative assays, as well as the key enzyme (cholinesterases, tyrosinase, α‐amylase and α‐glucosidase) inhibitory potentials of the extracts were evaluated. Chemical profiling confirmed the presence of lanceolatins and lophirones in all analyzed plant parts. Higher levels of total phenolics (156.42 mg gallic acid equivalent (GAE)/g for maceration-water), phenolic acids (165.84 mg caffeic acid equivalent (CE)/g for maceration-water) and flavanols (101.51 mg catechin equivalent (CAE)/g for soxhlet-methanol (MeOH)) were observed in the stem bark extracts. Antioxidant assays showed remarkable free radical scavenging and reducing power activities for all extracts, among which stem bark showed the highest potential. Stem bark extracts (IC 50 values: 57.55–93.10 μg/ml for colorectal adenocarcinoma (HT29) and 78.18–89.58 μg/ml for metastatic breast cancer cell line (MCF7)) also showed better antiproliferative effect than leaf (424.14–790.27 μg/ml for HT29 and 374.46–943.09 μg/ml for MCF7) on carcinoma cells while they induced proliferation in normal human cell lines (normal skin fibroblasts (HFF)). In the enzyme inhibitory assays, the methanol extracts of both plant parts were confirmed as effective against AChE, BChE (only stem barks extracts) and α-glucosidase enzymes. Regarding anti-tyrosinase effects, the methanol leaf extracts (122.21–131.17 mg kojic acid equivalent (KAE)/g) and all stem bark extracts (94.58–153.21 mg KAE/g) exhibited inhibitory effects. Findings amassed herein tend to validate the traditional uses of L. lanceolata and advocate for the development of phyto-medicaments based on its extracts. [ABSTRACT FROM AUTHOR]

Targeting the transmissible stages of the Plasmodium parasite that develop in the human and mosquito host is a crucial strategy for malaria control and elimination. Medicinal plants offer a prolific source for the discovery of new antimalarial compounds. The recent identification of the gametocytocidal activity of lophirone E, obtained from the African plant Lophira lanceolata (Ochnaceae), inspired the evaluation of the plant also against early sporogonic stages of the parasite development. The bioassay-guided phytochemical study led to the isolation of two known lanceolins and of a new glycosylated bichalcone, named glucolophirone C. Its stereostructure, including absolute configuration of the bichalcone moiety, was elucidated by means of NMR, HRMS, ECD and computational calculations. Lanceolin B proved to be a potent inhibitor of the development of Plasmodium early sporogonic stages indicating that the plant produces two different stage-specific antimalarial agents acting on transmissible stages in the human and mosquito host. Phytochemical study of Lophira lanceolata afforded lanceolin B, an inhibitor of Plasmodium early sporogonic stages, and the new bichalcone glucolophirone C. Image 1 • The glycosylated bichalcone glucolophirone C has been isolated from Lophira lanceolata. • The absolute configuration of the bichalcone Lophirone C has been determined. • Lanceolin B is a potent inhibitor of the development of Plasmodium early sporogonic stages. • Lophira lanceolata produces two different stage-specific antimalarial agents acting on transmissible stages. [ABSTRACT FROM AUTHOR]

Bioassay-guided fractionation of the organic extract obtained from stem barks of the African plant Lophira lanceolata has led to the isolation of seven biflavonoids, including the new α′-chlorolophirone E (5) and 5′-chlorolophirone D (6). Among the isolated compounds, the bichalcone lophirone E was identified as a potent gametocytocidal agent with an IC 50 value in the nanomolar range and negligible cytotoxicity (selectivity index = 570). Lophirone E proved to be about 100 times more active against P. falciparum stage V gametocytes than on asexual blood stages, thus exhibiting a unique stage-specific activity profile. The isolation of structural analogues allowed to draw preliminary structure-activity relationships, identifying the critical positions on the chemical scaffold of lophirone E. [ABSTRACT FROM AUTHOR]