Anticholinesterase constituents from the leaves of Spondias mombin L. (Anacardiaceae).

Spondias mombin has been used in traditional medicine for the management of several diseases, including memory loss. This study aimed to evaluate the cholinesterase inhibitory activity of the methanol extract of the leaves and its derived fractions, as well as carry out detailed phytochemical investigations leading to the isolation and characterization of bioactive compounds from the plant. The acetyl cholinesterase (AChE) and butyryl cholinesterase (BUChE) inhibitory activities were evaluated by colorimetric and thin-layer chromatography bioautographic assay techniques. The ethyl acetate fraction was most active against both enzymes, with percentage inhibition of 58.10 ± 1.08% and 52.66 ± 1.34% against AChE and BUChE, respectively. Three compounds, namely, botulin, campesterol and phytol, with IC50 of 0.88 µg/mL (AChE), 4.67 µg/mL (BuChE); 1.89 µg/mL (AChE), 4.08 µg/mL (BuChE) and 12.51 µg/mL (AChE), 23.89 µg/mL (BuChE), respectively, were isolated from the supernatant of the ethyl acetate fraction. The isolated cholinesterase inhibitory compounds correlate with the known memory-enhancing property of the plant and thus support one of its uses in ethnomedicine.

Spermicidal Constituents of Ethanolic Extract of Sacoglottis gabonensis Stem Bark.

AIM: To isolate the spermicidal constituents of Sacoglottis gabonensis. MATERIALS AND METHODS: The ethanolic extract with partitioned fractions of Sacoglottis gabonensis stem bark were subjected to sperm immobilization assay. The most active EtOAc fraction was further purifi ed by column and Semi-Preparative High Performance Liquid Chromatography to give compounds which were characterized by spectroscopic methods (UV, LC/MS, and NMR). The compound(s) was also tested for sperm immobilization activity. RESULTS: The ethanolic extract showed 100% signifi cant (p < 0.05) sperm immobilization activity at a concentration of 30 mg/mL at 20 s compared to both negative and positive controls. The most active ethyl acetate fraction yielded methyl 3,5-dihydroxy-4-methoxybenzoate, eriodictyol and bergenin. Bergenin had 100% sperm immobilization activity at 20 mg/mL in 60 s which was signifi cant (p < 0.05) also when compared to the positive and negative control while methyl 3,5-dihydroxy- 4-methoxybenzoate, eriodictyol were not active. CONCLUSION: The active spermicidal constituent in Sacoglottis gabonensis stem bark extract is bergenin. However, methyl 3,5-dihydroxy-4-methoxybenzoate and eriodictyol showed no activity. This plant is known for its aphrodisiac action; hence, caution may have to be exercised in its use because of its spermicidal eff ect.

Cholinesterase inhibitory activity and structure elucidation of a new phytol derivative and a new cinnamic acid ester from Pycnanthus angolensis

ABSTRACT The leaves of Pycnanthus angolensis (Welw.) Warb., Myristicaceae, are used as memory enhancer and anti-ageing in Nigerian ethnomedicine. This study aimed at evaluating the cholinesterase inhibitory property as well as isolates the bioactive compounds from the plant. The acetylcholinesterase and butyrylcholinesterase inhibitory potentials of extracts, fractions, and isolated compounds were evaluated by colorimetric and TLC bioautographic assay techniques. The extract inhibited both enzymes with activity increasing with purification, ethyl acetate fraction being most active fraction at 65.66 ± 1.06% and 49.38 ± 1.66% against acetylcholinesterase and butyrylcholinesterase, respectively while the supernatant had 77.44 ± 1.18 inhibition against acetylcholinesterase. Two new bioactive compounds, (2E, 18E)-3,7,11,15,18-pentamethylhenicosa-2,18-dien-1-ol (named eluptol) and [12-(4-hydroxy-3-methyl-oxo-cyclopenta-1,3-dien-1yl)-11-methyl-dodecyl](E)-3-(3,4-dimethylphenyl)prop-2-enoate (named omifoate A) were isolated from the plant with IC50 of 22.26 µg/ml (AChE), 34.61 µg/ml (BuChE) and 6.51 µg/ml (AChE), 9.07 µg/ml (BuChE) respectively. The results showed that the plant has cholinesterase inhibitory activity which might be responsible for its memory enhancing action, thus justifying its inclusion in traditional memory enhancing preparations.

Acetylcholinesterase and butyrylcholinesterase inhibitory activity of some selected Nigerian medicinal plants / Atividade inibitória da acetilcolinesterase e butirilcolinesterase de algumas plantas medicinais da Nigéria

Plants have been found to be useful as memory enhansers as well as antiaging. Twenty two of such plants from sixteen families were investigated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities using the in vitro Ellman's spectrophotometric and in situ bioautographic methods with physostigmine as standard. At least three morphological parts were examined for each of the plants investigated and the test concentration was 42.5 µg/ mL. Some plants were active on both enzymes though with some morphological parts being more active than others. The root bark of Spondias mombin showed the highest activity to the two enzymes; 64.77 percent and 83.94 percent on AChE and BuChE respectively. Other plant parts of the selected plants exhibited some remarkable selectivity in their actions. Those selectively active against AChE were Alchornia laxiflora stem bark (41.12 percent) and root bark, Callophyllum inophyllurn root bark (56.52 percent). The leaves of C. jagus (74.25 percent), Morinda lucida leaves (40.15 percent), Peltophorum pterocarpum leaves and stem bark (49.5 percent and 68.85 percent, respectively), physiostigmine gave 90.31 percent inhibition. Generally higher activities were found against BuChE. Bombax bromoposenze leaves, root bark and stem bark were particularly active. The inhibition was over 80 percent. Other selective plant parts are the leaves Antiaris africana, Cissampelos owarensis aerial parts (78.96 percent), Combretum molle leaves and stem bark (90.42 percent and 88.13 percent, respectively), Dioscorea dumentorum root bark and tuber (over 87 percent), G. kola leaves, Markhamia tomentosa root bark, Pycnanthus angolensis stem bark and Tetrapleura tetraptera leaves. Most of these plants are taken as food or are food ingredients in Nigeria and may account for the low incidence of Alzheimer's disease in the country and may play certain roles in the mediation of the disease.

As plantas podem ser úteis para estimular a memória, bem como serem usadas para combater o envelhecimento. Vinte e duas plantas, de dezesseis famílias, foram investigadas in vitro oara verificar sua atividade inibidora das enzimas acetilcolinesterase (AChE) e butirilcolinesterase (BuChE) pelo método espectrofotométrico de Ellman in situ e métodos de bioautografia utilizando fisostigmina como padrão. Pelo menos três partes morfológicas de cada planta foram analisadas e a concentração de ensaio foi de 42,5 µg/mL. Algumas plantas foram ativas em ambas as enzimas, embora com algumas partes mais ativas que outras. A casca da raiz de Spondias mombin apresentou a maior atividade as duas enzimas, 64,77 por cento para AChE e 83,94 por cento para BuChE. Outras partes das plantas selecionadas apresentaram boa seletividade em suas ações. As plantas seletivamente ativos contra AChE foram as casca do caule e casca da raiz de Alchornia laxiflora (41,12 por cento), e casca da raiz de Callophyllum inophyllurn (56,52 por cento). As folhas de C. jagus (74,25 por cento), folhas de Morinda lucida (40,15 por cento), folhas e casca do caule de Peltophorum pterocarpum (49,5 por cento e 68,85 por cento, respectivamente), physiostigmine inibiu 90,31 por cento. Em geral, atividades melhoras foram apresentadas contra BuChE. Folhas, casca da raiz e casca do caule Bombax bromoposenze foram particularmente ativos. A inibição foi acima de 80 por cento. Outras partes de algumas espécies também foram seletivas, como as partes aéreas de Antiaris africana, Cissampelos owarensis (78,96 por cento), folhas e casca do caule de Combretum molle (90,42 por cento e 88,13 por cento, respectivamente), casca da raiz e de tubérculos de Dioscorea dumentorum (mais de 87 por cento), folhas de G cola, cascas de raiz de Markhamia tomentosa, casca do caule de Pycnanthus angolensis e folhas de Tetrapleura tetraptera. A maioria destas plantas são utilizadas como alimentos ou ingredientes alimentares na Nigéria e podem ser responsáveis pela baixa incidência da doença de Alzheimer no país e desempenhar determinadas funções na mediação da doença.

Clinical effects of Garcinia kola in knee osteoarthritis.

OBJECTIVES: Over the past years, there has been a growing number of knee osteoarthritis (KOA) patients who are not willing to comply with long-term non-steroidal anti-inflammatory drugs (NSAID) treatment and wish to use herbal anti- rheumatic medicine. This study assessed the clinical effects of Garcinia kola (GK) in KOA patients. PATIENTS AND METHODS: Prospective randomized, placebo controlled, double blind, clinical trial approved by the institutional medical ethics review board and written informed consent obtained from each patient. All KOA patients presenting at the Obafemi Awolowo University Teaching Hospital complex were recruited into the study. The patients were grouped into four (A = Placebo, B = Naproxen, C = Garcinia kola, D = Celebrex). The drugs and placebo were given twice a day per oral route. Each dose consisted of 200 mg of G. kola, Naproxen (500 mg), Celebrex (200 mg) and Ascorbic acid (100 mg). The primary outcome measure over six weeks study period was the change in mean WOMAC pain visual analogue scales (VAS). Secondary outcome measures included the mean change in joint stiffness and physical function (mobility/walking). RESULTS: 143 patients were recruited, 84 (58.7%, males--24, females--60) satisfied the selection criteria and completed the study. The effect of knee osteoarthritis bilateralism among the subjects was not significant on their outcome (p > 0.05). The change in the mean WOMAC pain VAS after six weeks of G. kola was significantly reduced compared to the placebo (p < 0.001). Multiple comparisons of the mean VAS pain change of G. kola group was not lowered significantly against the naproxen and celebrex groups (p > 0.05). The onset of G. kola symptomatic pain relief was faster than the placebo (p < 0.001). However, it was slower than the active comparators (p > 0.05). The duration of therapeutic effect of Garcinia kola was longer than the placebo (p > 0.001). G. kola period of effect was less than naproxen and celebrex (p < 0.001). G. kola subjects had improved mean change mobility/walking after six weeks better than the control group(p < 0.001). The mean change in mobility of the G. kola group when compared to the active comparators was not significantly better (p < 0.05). The mean change of knee joint stiffness (p < 0.001) and the change of mean WOMAC score (p < 0.001) were improved on Garcinia kola as compared to the placebo. The mid term outcome of eleven Garcinia kola subjects after cessation of use had a mean pain relief period of 17.27 +/- 5.15 days (range: 9-26 days). There was no significant cardiovascular, renal or drug induced adverse reaction to Garcinia kola. CONCLUSION: Garcinia kola appeared to have clinically significant analgesic/anti-inflammatory effects in knee osteoarthritis patients. Garcinia kola is a potential osteoarthritis disease activity modifier with good mid term outcome. Further studies are required for standardization of dosages and to determine long-term effects.

Ethnobotanical survey of Akwa Ibom State of Nigeria.

ETHNOPHARMACOLOGICAL RELEVANCE: The medicinal plants employed in the ethnomedicine of Akwa Ibom State of Nigeria are studied. AIM OF THE STUDY: The survey aims at identifying and documenting the plants used amongst the indigenes of Akwa Ibom State. MATERIALS AND METHODS: Using ethnobotanical survey list, information is gathered through personal interviews with traditional medical practitioners, community elders and patients. RESULTS: A total of 114 medicinal plant species representing 102 genera and 54 families employed in the traditional medical practice of the people of Akwa Ibom State, Nigeria are recorded from 930 homes. Ailments such as skin diseases, malaria, gonorrhoea and haemorrhoids are mostly treated with the medicinal plants. Details pertaining to the preparation and administration of plant drugs are provided. CONCLUSIONS: The survey provides a veritable source of information for traditional medical practitioners and medicinal plant researchers. These medicinal plants may be incorporated into the healthcare delivery system of the country.