ANTIMALARIAL activities and alkaloids from Crinum jagus (Thomps) DANDY.

ETHNOPHARMACOLOGICAL RELEVANCE: Locally, among the Yoruba speaking people of South Western, Nigeria, the bulb of Crinum jagus (CJ), known as "ogede odo" is used to treat malaria and as an anthelmintic among other uses. AIMS OF THIS STUDY: Study aimed at identifying the purified active fractions and constituents of this fraction in an antiplasmodial activity-guided process. MATERIALS AND METHODS: Antiplasmodial activity-guided fractionation of the bulb and leaf extracts of CJ was investigated against chloroquine-sensitive (NK 65) Plasmodium berghei using 4-day suppressive and prophylactic methods. Molluscicidal activity of the extracts was assayed on adult Biomphalaria glabrata molluscs following WHO test protocols. Fractionation and purification of the active bulb extract was achieved using various chromatographic and spectroscopic techniques to isolate its constituents. Isolated compounds were identified using different spectroscopic methods. RESULTS AND DISCUSSION: Both extracts had oral median lethal dose (LD50) greater than 5000 mg/kg body weight (b.wt.). The leaf extract had 40% lethality on molluscs while the bulb extract was inactive. The chemosuppressive and prophylactic antimalarial effects of the bulb extract were 76.55 ± 2.76% and 90.49 ± 2.70% (p<0.05) respectively at 1000 mg/kg b. wt. while the reference drugs; chloroquine and pyrimethamine, had 80.26 ± 3.09% and 50.39 ± 6.80% chemosuppressive effects, respectively. Lycorine (1) and crinamine (2) were isolated from the alkaloidal fraction with 71.36 ± 12.54% antiplasmodial activity. CONCLUSION: The leaf and bulb extracts of Crinum jagus displayed low molluscicidal and moderate antimalarial activities. Lycorine and crinamine were identified from the antiplasmodial alkaloidal active fraction of the bulb.

Bioactivity-directed evaluation of fruit of Kigelia africana (Lam.) benth. Used in treatment of malaria in Iwo, Nigeria.

ETHNOPHARMACOLOGICAL RELEVANCE: The ancient people of Iwo communities consisting of Ile-Ogbo, Olupona, Iwo and Ogbagba continue to engage in the traditional use of medicinal plants for the treatment and management of common diseases especially malaria. AIMS OF THIS STUDY: This study conducted an ethnomedicinal survey of plants used to treat malaria and feverish conditions by the people of Iwo, Nigeria. It also evaluated the antiplasmodial activity of the morphological parts of Kigelia africana (Lam.) Benth., and isolated, as well as characterised pure compounds from the semi-purified fractions of the fruit extract. MATERIALS AND METHODS: The ethnomedicinal survey was conducted using semi-structured questionnaires administered to only herb sellers in Iwo, Ile-Ogbo, Olupona, and Ogbagba areas of Osun State. Extracts of K. africana morphological parts; leaf, root, stem bark, and fruit were obtained by cold maceration in methanol, followed by assessment of acute toxicity (LD50) and antiplasmodial activity in Plasmodium berghei infected rats using the 4-day suppressive test model. The most active fruit extract was further subjected to activity-guided fractionation and purification using n-hexane, dichloromethane, ethyl acetate (EtOAc), n-butanol (n-BuOH), and methanol (MeOH) in gradients to obtain the semi-purified fractions and two pure isolated compounds using various chromatographic and spectroscopic techniques. RESULTS AND DISCUSSION: From the survey, thirty-one plant species were identified for treating malaria in Iwo area. Azadirachta indica leaf was the most frequently used (78.3% of the respondents) while Manihot esculenta leaf (3.33%) was the least. The identified plants are distributed among 24 families, with Anacardiaceae and Asteraceae (11.67% each) been the most occurring families. Kigelia africana (Bignoniaceae) ranked the 6th position with 60% frequency of occurrence. The LD50 values obtained for the extracts were greater than 5000 mg/kg (p.o). The chemo-suppression activity of the extracts at 125 mg/kg was in the order of stem bark (26.59%), leaf (41.75%), root (43.95%), and fruit (54.54%). The semi-purified methanol fraction of the fruit showed the most antiplasmodial activity with a percent chemo-suppression of 69.94 and yielded 4-(2,3-dihydroxypropoxy)-3,5-dihydroxy-5-methylfuran-2-one and sucrose. CONCLUSION: The use of herbs and medicinal plants either singly or in combination for the treatment of malaria among the people of Iwo community in Nigeria is still well practised. Lack of formal education among most of the respondents and use of same local name for different plants species or plant parts; which often lead to wrong plant collection were among the constrains encountered. Kigelia africana has antiplasmodial activity in the order of fruit > root > leaf > stem bark.

Psychoneuropharmacological activities and chemical composition of essential oil of fresh fruits of Piper guineense (Piperaceae) in mice.

ETHNOPHARMACOLOGICAL RELEVANCE: Piper guineense Schum & Thonn (Piperaceae) is a medicinal plant used in the Southern States of Nigeria to treat fever, mental disorders and febrile convulsions. AIMS OF THE STUDY: This study aims at determining the chemical composition and the central nervous system (CNS) activities of the essential oil obtained from the plant׳s fresh fruits in order to rationalize its folkloric use. MATERIALS AND METHODS: Essential oil of P. guineense (EOPG) obtained by hydrodistillation was analysed by GC/MS. EOPG (50-200mg/kg, i.p.) was evaluated for behavioural, hypothermic, sedative, muscle relaxant, anti-psychotic and anticonvulsant activities using standard procedures. RESULTS AND DISCUSSION: Analysis of the oil reveals 44 compounds of which 30 compounds constituting 84.7% were identified. The oil was characterized by sesquiterpenoids (64.4%) while only four monoterpeneoids (21.3%) were found present in the oil. Major compounds identified were ß-sesquiphellandrene (20.9%), linalool (6.1%), limonene (5.8%), Z-ß-bisabolene (5.4%) and α-pinene (5.3%). The EOPG (50-200mg/kg, i.p.) caused significant (p<0.01) inhibition on rearing {F(4,20)=43}, locomotor {F(4,20)=22} activity and decreased head dips in hole board {F(4,20)=7} indicating CNS depressant effect; decreased rectal temperature {F(4,20)=7-16}, signifying hypothermic activity; decreased ketamine-induced sleep latency {F(4,20)=7.8} and prolonged total sleeping time {F(4,20)=8.8}, indicating sedative effect; reduced muscular tone on the hind-limb grip test {F(4,20)=22}, inclined board {F(4,20)=4-49} and rota rod {F(4,20)=13-106}, implying muscle relaxant activity; induced catalepsy {F(4,20)=47-136}, inhibited apomorphine-induced climbing behaviour {F(4,20)=9} and inhibited apomorphine-induced locomotor {F(4,20)=16}, suggesting anti-psychotic effect; and protected mice against pentylenetetrazole-induced convulsions, indicating anticonvulsant potential. CONCLUSION: The most abundant component of the fresh fruits essential oil of P. guineense was ß-sesquiphellandrene (20.9%); and the oil possesses CNS depressant, hypothermic, sedative, muscle relaxant, antipsychotic and anticonvulsant activities, thus providing scientific basis for its ethnomedicinal applications.

Hypnotic, anticonvulsant and anxiolytic effects of 1-nitro-2-phenylethane isolated from the essential oil of Dennettia tripetala in mice.

This study investigated the hypnotic, anti-convulsant and anxiolytic effects of 1-nitro-2-phenylethane (BPNE) obtained from the oil of Dennettia tripetala G. Baker (Annonaceae) and established its mechanism of action. The essential oil (EO) from the leaf, fruit and seed was obtained by hydrodistillation, followed by isolation of BPNE purified to 99.2% by accelerated gradient chromatography on silica, and identified by NMR and GC-MS. The pure BPNE and EO of the dried seed (93.6%) were comparatively evaluated for hypnotic, anticonvulsant and anxiolytic effects in mice. The acute toxicity of BPNE was determined and the LD50 was 490 mg/kg, intrapritonealy. The hypnotic activities of the EO and BPNE (50-400 mg/kg, i.p.) were assessed by loss of righting reflex, while sodium pentobarbitone (PBS) and diazepam (DZM) were used as positive controls. The anticonvulsant and anxiolytic effects of the EO and BPNE were evaluated in mice. Both BPNE and EO at doses ≥100 mg/kg induced spontaneous hypnosis with loss of righting reflex, significantly decreased sleep latency (SL) and also increased total sleeping time (TST) dose-dependently. They had comparable activity with NAP in TST. The BPNE exhibited higher hypnotic potency than EO at the same dose levels. The EO and BPNE offered comparable dose-related protections against PTZ- and strychnine-induced convulsions. Flumazenil (2 mg/kg) blocked the hypnotic and anticonvulsant (PTZ-convulsions) effects of both EO and BPNE. The essential oil at 5-20 mg/kg dose levels significantly (p<0.05) increased the percentage time spent and number of entries into the open arms. While at the same dose range BPNE significantly (p<0.05) increased the percentage time spent and the number of entries into the open arms respectively. The study concluded that 1-nitro-2-phenylethane exhibited dose dependent significant hypnotic, anticonvulsant and anxiolytic effects and it is the compound largely responsible for the neuropharmacological effects of the oil.