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Antimalarial activity of lactucin and lactucopicrin: sesquiterpene lactones isolated from Cichorium intybus L.

Folklore reports from Afghanistan prior to the wars described the use of aqueous root extracts of Cichorium intybus (L.) as a light-sensitive plant remedy for malaria. Preparative isolation and bioassay against HB3 clone of strain Honduras-1 of Plasmodium falciparum identified the previously known light-sensitive sesquiterpene lactones Lactucin and Lactucopicrin to be antimalarial compounds.

Animals↗

Anti-diarrhoeal and ulcer-protective effects of the aqueous root extract of Guiera senegalensis in rodents.

The anti-diarrhoeal and ulcer-protective properties of the aqueous root extract of Guiera senegalensis, a popular herbal traditional medicine in Nigeria were investigated in rats and mice. Acute toxicity studies were also carried out. The intestinal transit in mice was significantly (P < 0.05) reduced and gastric emptying delayed. One hundred and Two hundred milligrams per kilogram (p.o.) of the extract elicited a greater anti-motility activity than 0.1 mg/kg of atropine. The extract exhibited ulcer-protective properties against ethanol-induced ulceration in rats with maximal anti-ulcer activity recorded at 100 mg/kg. Guiera senegalensis also exerted significant anti-enteropooling effects causing a dose-related inhibitory effect on castor oil-induced enteropooling in rats. A profound anti-diarrhoeal activity was observed when Guiera senegalensis was tested in diarrhoeic mice. The frequency of defaecation as well as the wetness of the faecal droppings was significantly reduced. Furthermore, the extract produced 100% inhibition of castor oil-induced diarrhoea in mice. The oral LD50 values obtained were > 5000 mg/kg in both mice and rats. The results support the folkloric applications of Guiera senegalensis for the treatment of diarrhoea and ulcer in Nigerian herbal traditional medicine.

Animals↗

Studies on the antihypertensive, antispasmodic, bronchodilator and hepatoprotective activities of the Carum copticum seed extract.

This study describes the antihypertensive, antispasmodic, bronchodilator and hepatoprotective activities of the aqueous-methanolic extract of Carum copticum Benth. seeds (CSE) to rationalize some of its traditional uses. CSE (3-100 mg/kg) caused a dose-dependent fall in arterial blood pressure in anaesthetized rats. In isolated rabbit aorta and jejunum preparations, CSE (0.1-3.0 mg/ml) caused an inhibitory effect on the K+-induced contractions. The calcium channel blocking (CCB) effect was confirmed when CSE shifted the Ca2+ dose-response curves (DRCs) to right similar to verapamil. In isolated guinea-pig tracheal preparations, it caused inhibition of carbachol and K+-induced bronchoconstriction at 0.1-1.0 mg/ml as well as shifted the dose-response curves (DRCs) of carbachol and histamine to the right with suppression of maximum response suggestive of non-specific bronchodilator effect mediated possibly through CCB. Pretreatment of rats with CSE (500 mg/kg orally for 2 days at 12 h intervals) prevented paracetamol (640 mg/kg) and CCl4 (150 ml/kg)-induced rise in serum alkaline phosphatase (ALP) and aminotransferases (AST and ALT). The same dose of CSE was able to prevent the CCl4-induced prolongation in pentobarbital-induced sleeping time in mice confirming its hepatoprotectivity. These results indicate the presence of calcium antagonist(s) in Carum copticum seeds and thus provides sound mechanistic basis for some of their folkloric uses.

Animals↗

Anti-inflammatory and analgesic properties of water-ethanolic extract from Pothomorphe umbellata (Piperaceae) aerial parts.

Anti-inflammatory and analgesic activities as well as the median lethal dose (LD50) of water-ethanolic extract (PHE) of the aerial parts of Pothomorphe umbellata were evaluated in animal models. The ED(50) (oral) for the inhibition of carrageenan-induced rat paw edema assay was determined to be 550 mg/kg, while the LD(50) was higher than 2.0 g/kg. At a dose of 550 mg/kg, PHE inhibited the inflammatory process by 48.7% (P < 0.05) on the third hour of the assay (edema peak) when compared to the untreated control. Indomethacin, the positive control used in this test, inhibited the edema by 58.6% at a dose of 10 mg/kg, when compared to the untreated control (P < 0.05). All three fractions--hexane, methylene chloride and ethyl acetate--obtained by partition of PHE with respective solvents also showed inhibition of the edema induced by carrageenan over a period of 4h but the methylene chloride fraction showed the best activity. The activity shown by the methylene chloride fraction at 200 mg/kg was comparable to that exhibited by indomethacin at a dose of 10mg/kg. The number of writhings induced by a 0.6% acetic acid solution intraperitoneal injection was decreased by 22% (P < 0.05) in the group treated orally with Pothomorphe umbellata crude extract. PHE also inhibited the granulomatous tissue formation in rats by 6.2% (P < 0.05). In the same assay, topically applied dexamethasone decreased the granuloma formation by 14.2%. The above results suggest that Pothomorphe umbellata crude extract has analgesic and anti-inflammatory properties supporting its folkloric use for the treatment of these conditions.

Acetic Acid↗

In vitro immunomodulatory effect of Pouteria cambodiana (Pierre ex Dubard) Baehni extract.

The methanolic stem bark extract from Pouteria cambodiana (Pierre ex Dubard) Baehni was evaluated for immunomodulating activity on BALB/c mice. The antioxidant effect was also assessed. The extract presented a good dose-response effect in the peritoneal macrophage phagocytosis assay with higher activity at 1mg/ml and an EC50 of 0.02 mg/ml and also activated lysosomal enzyme activity with an EC50 of 0.16 mg/ml. In the splenocyte proliferation assay, the extract without mitogen was active (EC50, 0.01 mg/ml) while the EC50 of the extract with lipopolysaccharide (LPS) and pokeweed mitogen (PWM) were 0.02 and 0.41 mg/ml, respectively. The extract showed low free radical scavenging activity in the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical assay with an IC50 of 0.24 mg/ml, being less active than ascorbic acid, butylated hydroxytoluene (BHT) and alpha-tocopherol which showed IC50 of 0.08, 0.10 and 0.11 mg/ml, respectively. The extract at doses up to 0.073 mg/ml had no effect on lipid peroxidation. The potent immunological but no antioxidant activity of the extract presented in this study can explain, at least in part, the Thai folklore application of this plant in the treatment of fever and skin eruption.

Animals↗

In vivo immunomodulating activity of wood extracts from Clausena excavata Burm. f.

Immunomodulating effects in Balb/C mice of aqueous extract (CEHW) and the Thai folklore preparation (CEHF) of Clausena excavata Burm. f. were investigated. Haemagglutinating antibody (HA) titers at day 0, 7, 14, 21, 28 and 35 from the serum of animals fed or injected intraperitoneally with the extracts for 5 days were compared and evaluated for humoral mediated immunity (HMI). Footpad swelling test was used to determine delayed type hypersensitivity for cell mediated immunity (CMI). CEHW and CEHF injected intraperitoneally and administered orally exhibited the same maximum antibody production of 1/800. Both extracts given orally reached the maximum antibody titer at day 7, which was 2 weeks faster than by intraperitoneal administration. However, antibody titers from CEHW injected intraperitoneally diminished without retaining whereas the CEHF retained for 1 week. Moreover, CEHW gave CMI response more than the CEHF. This study suggested the potential in vivo immunomodulating activities of extracts from Clausena excavata supporting our previous in vitro studies.

Animals↗

Antispasmodic and blood pressure lowering effects of Valeriana wallichii are mediated through K+ channel activation.

Crude extract of Valeriana wallichii rhizome (Vw.Cr) and its fractions were studied for possible antispasmodic and blood pressure lowering activities to rationalize some of the folkloric uses. In rabbit jejunum preparations, Vw.Cr (0.1-3.0 mg/mL) caused relaxation of spontaneous contractions. When tested against high K(+) (80 mM)-induced contractions it produced weak inhibitory effect, while caused complete relaxation of the contractions induced by low K(+) (20 mM). In the presence of glibenclamide (3 microM), the inhibitory effect of low K(+) was shifted to the right, similar to that produced by cromakalim while, verapamil caused no differentiation in its inhibitory effect against low and high K(+)-induced contractions. In guinea pig ileum, the plant extract produced similar results as in rabbit jejunum. Intravenous administration of Vw.Cr, produced fall in arterial blood pressure in normotensive anaesthetized rats and this effect was partially blocked by glibenclamide. In rabbit aortic preparations, plant extract also caused a selective and glibenclamide-sensitive relaxation of low K(+) (20 mM)-induced contractions. Activity-directed fractionation studies revealed that the observed activity was distributed both in the chloroform and aqueous fractions. These results indicate that the antispasmodic and hypotensive effects of Valeriana wallichii are mediated possibly through K(ATP) channel activation, which justify its use in gastrointestinal and cardiovascular disorders.

Animals↗

Anti-ulcerogenic activity of some plants used in folk medicine of Pinarbasi (Kayseri, Turkey).

Several ethnomedicinal plant remedies used in Pinarbasi, Kayseri, in particular those which are used for the treatment of several peptic ulcer symptoms such as stomach ache, heartburn, etc. were selected for evaluation of their anti-ulcerogenic potential. In order to confirm the claimed activities, decoctions were prepared from aerial parts of Malva neglecta Wallr. (Malvaceae), leaves of Potentilla reptans L. (Rosaceae), fruits of Rumex patientia L. (Polygonaceae), aerial parts of Sanguisorba minor Scop. ssp. muricata (Spach) Briq. (Rosaceae), aerial parts of Sideritis caesarea Duman, Aytac&Baser (Lamiaceae), and flowers of Verbascum cheiranthifolium Boiss var. cheiranthifolium (Scrophulariaceae) according to their described folkloric applications. Pharmacological experiments clearly demonstrated that the extracts of all plants given orally showed significant gastric protection against the ethanol-induced gastric ulcer model in rats. Furthermore, healing effects were also confirmed through histopathological examination.

Animals↗

Anti-inflammatory activities of the methanol extracts and an isolated furanoditerpene constituent of Sphenocentrum jollyanum Pierre (Menispermaceae).

Sphenocentrum jollyanum crude extracts and an isolated constituent were evaluated for anti-inflammatory activity using the carrageenan-induced hind paw oedema of healthy adult albino rats and utilizing the oral route of administration. The fruit methanol extract (79.58% inhibition at 200 mg kg(-1)) gave a higher anti-inflammatory activity than the root extract (53.75% inhibition at 200 mg ml(-1)). Further purification of the most active fruit methanol extract (MFE) led to the isolation of three furanoditerpenes identified as columbin, isocolumbin, fibleucin (uv, ir, nmr and ms) as well as a flavonoid-rich fraction (FDE). Both columbin (67.08% inhibition at 20 mg kg(-1), p<0.05) and FDE (76.25% inhibition at 200 mg kg(-1); p<0.05) gave significant anti-inflammatory activities in comparable range with reference acetylsalicylic acid (72.5% inhibition at 100 mg kg(-1)). The results provide some justification for the folkloric uses of Sphenocentrum jollyanum in the treatment of inflammatory-based diseases across the West African sub-region.

Animals↗

Integrated approaches towards drug development from Ayurveda and other Indian system of medicines.

Biodiversity of natural resources has served not only for the primary human needs but also for health care, since time immemorial. The Indian subcontinent, with the history of one of the oldest civilization, harbors many traditional health care systems. Their development was supported by the diverse biodiversity in flora and fauna due to variations in geographical landscaping. Ayurveda, whose history goes back to 5000 b.c., is one of the ancient health care systems. The Ayurveda was developed through daily life experiences with the mutual relationship between mankind and nature. The ancient text of Ayurveda reports more than 2000 plant species for their therapeutic potentials. Besides Ayurveda, other traditional and folklore systems of health care were developed in the different time periods in Indian subcontinent, where more than 7500 plant species were used. According to a WHO estimate, about 80% of the world population relies on traditional systems of medicines for primary health care, where plants form the dominant component over other natural resources. Renewed interest of developing as well as developed countries in the natural resources has opened new horizons for the exploration of natural sources with the perspectives of safety and efficacy. The development of these traditional systems of medicines with the perspectives of safety, efficacy and quality will help not only to preserve this traditional heritage but also to rationalize the use of natural products in the health care. Until recent past, the nature was considered as a compendium for templates of new chemical entities (NCEs). The plant species mentioned in the ancient texts of these Ayurveda and other Indian systems of medicines may be explored with the modern scientific approaches for better leads in the health care.

Drug Design↗

Preliminary toxicity and phytochemical studies of the stem bark aqueous extract of Musanga cecropioides in rats.

These studies were designed to determine the preliminary oral toxicity profile of the crude aqueous stem bark extract of Musanga cecropioides (MCW) in adult Sprague-Dawley rats and its active chemical constituents by way of phytochemistry. The acute oral toxicity study was conducted using limit dose test of Up and Down Procedure according to the OECD/OCDE Test Guidelines on Acute Oral Toxicity (AOT425statPgm, version: 1.0) at a limit dose of 3,000 mg/kg body weight/oral route. Repeat dose oral toxicity studies were conducted by daily oral dosing of 750 mg/kg body weight of MCW dissolved in 1 ml of 0.9% saline and 1 ml of 0.9% saline to rats in the test and control groups, respectively, for 28 days. On day 29, blood samples for bioassays were collected by cardiac puncture under diethyl ether anesthesia. The phytochemical analysis was conducted using standard procedures. The LD(50) estimate of the extract was calculated to be greater than 3,000 mg/kg body weight/oral route. The extract caused a significant (P<0.05) decrease in weight gain, differential eosinophil count and increase in serum creatinine but did not affect the organ weights, other serum electrolytes (Na(+), K(+), HCO(3)(-)), liver enzymes and other hematological indices in test rats. Its phytochemical analysis showed it contains saponins, flavonoids, alkaloids, tannins, phlobatannins, glycosides, reducing sugars and anthraquinones. These results show that the aqueous extract of Musanga cecropioides is relatively safe toxicologically when administered orally. Thus, its use in folkloric medicine as an oral antihypertensive is relatively safe when used over the tested period.

Animals↗

Anti-diabetes and hypoglycaemic properties of Hemionitis arifolia (Burm.) Moore in rats.

Hemionitis arifolia, a folklore anti-diabetes fern, was evaluated for its hypoglycaemic and anti-diabetic properties using rats. Glucose lowering effect and anti-diabetes activity were studied using glucose tolerance test in normal rats and alloxan diabetic rats, respectively. When different extracts were tested, the ethanol and, to some extent, the water extracts were found to lower the levels of blood glucose in glucose fed rats. The ethanol extract showed optimum activity at 200 mg/kg. The extract exhibited only marginal hypoglycaemic activity in overnight fasted normal rats and it was devoid of conspicuous toxic symptoms in sub-acute toxicity evaluation in mice. When the alcohol extract was fractionated by sequential solvent extraction, the activity was found in ethyl acetate fraction (50 mg/kg). This fraction containing steroids and coumarins showed anti-diabetes activity in alloxan diabetic rats as judged from serum glucose levels, liver glycogen content and body weight. This fraction is an attractive material for further research vis-à-vis drug development.

Alloxan↗

Anti-inflammatory and anti-nociceptive activities of Pluchea quitoc (DC.) ethanolic extract.

Pluchea quitoc DC. (Asteraceae), a plant widely distributed throughout Brazil and popularly known as "quitoco", "madre-cravo" or "tabacarana", is used in traditional medicine for the treatment of inflammation, as well as of digestive and respiratory diseases. The anti-inflammatory and anti-nociceptive activities of the ethanolic extract (EE) from aerial parts of this plant were evaluated in mice and rats. Oral treatment with the EE (1-2g/kg, p.o.) decreased the paw oedema induced by carrageenan in rats, showed anti-nociceptive effects on the tail-flick test and on acid-induced writhing in mice, and inhibited both phases of pain (neurogenic and inflammatory) of the formalin test in rats. Topical application (EE 1.25, 2.5 and 5.0mg) inhibited the ear oedema induced by croton oil in mice. The results support the folkloric use of the plant in inflammatory processes.

Acetic Acid↗

Search for antibacterial and antifungal agents from selected Indian medicinal plants.

A series of 61 Indian medicinal plants belonging to 33 different families used in various infectious disorders, were screened for their antimicrobial properties. Screening was carried out at 1000 and 500 microg/ml concentrations by agar dilution method against Bacillus cereus var mycoides, Bacillus pumilus, Bacillus subtilis, Bordetella bronchiseptica, Micrococcus luteus, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Streptococcus faecalis, Candida albicans, Aspergillus niger and Saccharomyces cerevisiae. Twenty-eight plant extracts showed activity against at least one of the test organisms used in the screening. On the basis of the results obtained, we conclude that the crude extracts of Dorema ammoniacum, Sphaeranthus indicus, Dracaena cinnabari, Mallotus philippinensis, Jatropha gossypifolia, Aristolochia indica, Lantana camara, Nardostachys jatamansi, Randia dumetorum and Cassia fistula exhibited significant antimicrobial activity and properties that support folkloric use in the treatment of some diseases as broad-spectrum antimicrobial agents. This probably explains the use of these plants by the indigenous people against a number of infections.

Anti-Bacterial Agents↗

Studies on the reproductive, cytological and biochemical toxicity of Ginkgo Biloba in Swiss albino mice.

Ginkgo biloba (an herbal product), used as a folkloric medicine in the treatment of dementia, was evaluated for its effects on reproductive, cytological and biochemical toxicity in male Swiss albino mice. The mice were treated with different doses (25, 50 and 100mg/kg/day) of the aqueous suspension of Ginkgo biloba for 90 days by oral gavage. The following parameters were evaluated: (1) reproductive organ weight; (2) motility and content of sperms; (3) spermatozoa morphology; (4) cytology of the testes chromosomes; (5) study on reproduction; (6) biochemical study on proteins, nucleic acids, malondialdehyde (MDA) and nonprotein sulfhydryl (NP-SH). The treatment caused significant changes in the weight of caudae epididymis, prostate, chromosomal aberrations, rate of pregnancy and pre-implantation loss. However, the percent motility, sperm count and morphology of spermatozoa were not affected. Our study on biochemical parameters showed depletion of nucleic acids, NP-SH and increase of MDA, which elucidated the role of free radical species in the induced changes in testis chromosomes and the reproductive function. The exact mechanism is not known, however, the activation of GABA, glycine and glutamate under the influence of Ginkgo biloba and its constituents might have generated free radicals and depleted cellular glutathione by calcium influx and membrane depolarization. The observed toxicity is attributed to the toxic constituents (ginkgolic acids, biflavones, cardanols, cardols, bilobalides and quercetin) of Ginkgo biloba. Our results warrant careful use of Ginkgo biloba as a remedy for impotence and/or erectile dysfunction.

Animals↗

Analgesic activity of some Indian medicinal plants.

In the present study of some of the Indian medicinal plants Sida acuta whole plant (Malvaeae), Stylosanthes fruticosa (whole plant) (Papilionaceae), Toona ciliata (heart wood) (Meliaceao), Bougainvilla spectabilis (leaves) (Nyctaginaceae), Ficus glomerata (bark, leaves) (Moraceae) and Polyalthia longifolia (leaves) (Annonaceae). The different plants were used in folklore medicine in the treatment of toothache and strengthening of gums, anthelmintic, kidney diseases, analgesic, anti-inflammatory, hepatoprotective, antihyperglycaemic, antihyperglycaemic and anticancer. The extract was prepared using powdered material with ethanol, concentrated under vacuo and were evaluated for analgesic activity by analgesiometer at three dose level (100, 300 and 500mg/kg). Analgesic activity was significant with Toona ciliata (heart wood) ethanolic extract when compared with other extracts and its activity was confirmed by tail immersion method.

Analgesics↗

Medicinal plants used to induce labour during childbirth in western Uganda.

Traditional medicine usage in rural Ugandan population for day-to-day health care needs is close to 90%. Women and children form the bulk of the people reliant on herbal medicine. This study was undertaken to document how ethnomedical folklore aids childbirth in rural western Uganda by conducting field surveys, discussions and interviews with the resource users (mothers) and health providers (traditional birth attendants). Health surveys revealed that over 80% of childbirths are conducted at home by using herbal remedies in Bushenyi district. Seventy-five plants have been recorded for usage in inducing labour and some of these plants may be oxytocic. The dilemma lies in the toxicity levels and the unspecified dosages that may threaten the life of the unborn baby and the mother. The high population growth rate, high total fertility rate coupled with high maternal mortality and morbidity in Uganda calls for rethinking in gendered health provision policies and programmes for which herbal medicine integration in health care systems seems viable.

Adult↗

In vivo antidiabetic and antioxidant potential of Helichrysum plicatum ssp. plicatum capitulums in streptozotocin-induced-diabetic rats.

Helichrysum species (Asteraceae) are widely found in Anatolia. Decoction prepared from the capitulums of Helichrysum plicatum ssp. plicatum is used to alleviate the symptoms of diabetes mellitus in folk medicine. In the present study, the hypoglycaemic and antioxidant potential of Helichrysum plicatum ssp. plicatum was evaluated by using in vivo methods in normal and streptozotocin-induced-diabetic rats. After the oral administration of water and ethanolic extracts at doses of 500mg/kg body weight prepared from the capitulums of plant, blood glucose levels were monitored at specific intervals. Tolbutamide was used as a reference drug at a dose of 100mg/kg. The experimental data indicated that water and ethanol extracts of capitulums demonstrate significant antihyperglycaemic and antioxidant activity in streptozotocin-induced rats which confirmed the folkloric utilization. In order to assess the role of polyphenolic components in the relevant activity, phenolic and flavonoid contents of each extract were also determined in terms of total phenols: 113.5+/-8.6mg (gallic acid equivalent/1g extract) and total flavanoids 50.5+/-1.9mg (quercetin equivalent/1g extract) for ethanol extract, total phenols: 75.9+/-3.7, flavonoids: 31.5+/-2.3 for water extract using Folin-Ciocalteu reagent.

Animals↗