Current Issue : July - September Volume : 2010 Issue Number : 2 Articles : 18 Articles
Local and traditional knowledge has been the starting point for many successful drug development projects over the last decades. Here we discuss some examples of anti-cancer drugs which have had enormous impact as anti-cancer agents (camptothecan, taxol and derivatives) and a few examples of drugs currently under various stages of preclinical development. Ethnobotanists investigate the relationship between humans and plants in all its complexity, and such research is generally based on a detailed observation and study of the use a society makes of plants. The requirements of modern research on natural products as, for example, outlined in the Convention on Biological Diversity (Rio Convention) and the overall approach in ethnobotanical research are also discussed. Selected phytochemical-pharmacological studies based on traditional plant use are used to highlight the potential of ethnobotany driven anti-cancer research. The link between traditionally used plants and targets of the NF-kappaB pathway is discussed using on an EU-funded, multidisciplinary project as an example. Lastly the potential of chemopreventive agents derived from traditional food plants is briefly addressed....
The herbal preparations of the root bark of Annona senegalensis Pers (Annonaceae) is used in traditional medicine in South Eastern Nigeria for the treatment of epilepsy and febrile convulsions. A pilot study has confirmed the potency of the root bark of A. senegalensis in the control of seizure in mice. The current study was aimed to identify the active phytochemical responsible for the activity. Activity guided fractionation of the methanol: methylene chloride root bark extract (MME) afforded ethylacetate fraction (EF) as the most anticonvulsant potent fraction between hexane fraction (HF) and methanol fraction (MF) when studied for anticonvulsant activity in mice using pentylenetetrazole (PTZ) (60 mg/kg, s.c.) induced convulsions. Further fractionation of the ethyl acetate fraction (EF) yielded eight (8) fractions of which fraction F4 gave the most potent activity. Phenobarbitone induced sleep time test and motor coordination test on rota-rod performance were also used to assess the sedative and central depressant effects of MME, EF, and F4. Acute toxicity and lethality (LD50) test as well as phytochemical analysis were also performed on the extract and fractions. Results indicated that the MME, EF (200, 400, 800 mg/kg) and fraction F4 (50, 100 and 200 mg/kg) exhibited a dose dependent significant (P < 0.05) delay in the latency of myoclonic spasms and tonic - clonic phase of seizure induced by PTZ. At 200 mg/kg MME, EF and F4 respectively offered 60, 80 and 60 % protection against seizure induced death while HF and MF offered no percentage protection. Also MME, EF and F4 decreased the latency and increased the duration of phenobarbitone induced sleeping time as well as exhibited a significant (P < 0.05) inhibition of motor incoordination. The acute toxicity test revealed an oral LD50 of 1296 and 2154 mg/kg for MME and EF respectively, while the phytochemical studies showed the presence of alkaloids, resins, glycosides, carbohydrate, reducing sugar, fats and oils, flavonoids, and terpenoids. The phytochemical analysis revealed that flavonoids were present in MME, EF and F4 and absent in HF and MF. The results suggested that the extract and fractions of A. senegalensis possessed anticonvulsant activity and central depressant effects which may be attributable to the flavonoids....
The aqueous, methanol and chloroform extracts of Artemisia nilagirica (Clarke) leaves (AEAN, MEAN & CEAN respectively) was investigated for anti-inflammatory and analgesic activities. All the extracts (100mg/kg each) were found to significantly (P<0.05) inhibit paw edema induced by carrageenan in rats and the nociception induced by Tail immersion in hot water (50.0 ± 1.0ºC) and acetic acid. The methanol extract produced the highest paw edema inhibition while in thermally induced nociception both the MEAN and CEAN show high and comparable analgesic activity with acetylsalicylic acid (150mg/kg). However in chemically induced pain (acetic acid) MEAN produced the highest and comparable analgesic activity to acetylsalicylic acid (150mg/kg). We therefore conclude, that apart from the folklore uses of Artemisia nilagirica (Clarke) leaves as antimalarial agents, the various extracts of the plant also possess anti-inflammatory and analgesic activities. Phytochemical analysis showed that the methanolic extract of Artemisia nilagirica (Clarke) contain some secondary metabolites namely alkaloids, sesquiterpine lactones and some polyphenolic compounds. Also, this extract exhibits some antioxidative activities....
Achyranthes Aspera Linn., known as Chirchira (Hindi), Agadha (Marathi) is an indigenous herb found in India. Agadha is the basic composition of many traditional remedies. It is commonly used for the treatment of fever, dysentery, asthma, hypertension, diabetes, cough, bronchitis and rheumatism. Present study was designed to evaluate the analgesic (antinociceptive) activity of an ethanol extract of Achyranthes Aspera (Agadha). Findings of this study may help researchers to set their minds for studying the utility, efficacy and potency of herb as an analgesic.The ethanol extract of A. Aspera was examined for its central analgesic activity by using hot plate, tail flick method in albino mice. The doses administered were 200 mg/kg and 400 mg/kg p.o. (orally). The Pentazocine10mg/kg i.p. (intraperitoneal) was taken as standard drug.Data analyzed by ANOVA test followed by Dunnett’s test. All the results were expressed as Mean (±SEM). P <0.05 was considered significant. The animal that administered a dose of 400mg/kg leaf extract has shown the maximum analgesic activity comparable to Pentazocine (p<0.001). The analgesic activity was observed after 60min of drug administration and showed wearing off after 120mins. An ethanol extract of A. Aspera has central analgesic activity involving spinal as well as supraspinal mechanisms. This activity may be due to saponins found in the extract. Extrapolation of findings in clinical situation however needed to develop it as novel analgesic....
Rodent model of neuropathic pain is used to evaluate the efficacy of novel compounds. Since neuropathic pain occurs due to the neuronal injury, is a chronic condition thus it require the prolong treatment. In the present study the effect of pregabalin on chronic constriction injury (CCI) induced neuropathic pain model in SD rats (Sprague-dawley) during and after the treatment was first time examined. The majority of animals in CCI model exhibited characteristic neuropathic pain behaviors in all three nociceptive tests on postoperative day 5 and then maintained it during the whole study period. Pregabalin treatment was given from post operative day 7-13. Spontaneous pain and chemical allodynia were strongly attenuated by pregabalin (30 mg/kg, ip., bid.) during the whole treatment duration. Post treatment effect were maintained till post operative day 26 and 17 respectively, while mechanical hyperalgesia response was weakly attenuated only on post operative day 9. The effect of pregebalin on body weight, water intake and food intake insignificant was observed in all groups. All comparison was done using two tail unpaired t – test. Data were consider statistically significant at p value < 0.05, moderately significant at p value< 0.01 and highly significant at p value < 0.001. Overall, the results indicate that pregabalin was found to be effective in treatment of spontaneous pain and chemical allodynia conditions associated with neuropathic pain but the duration of therapy will be much longer....
The study was designed to investigate the cardioprotective and antioxidant effects of Tinospora cordifolia against isoproterenol induced myocardial damage in rats. Sixty, male wistar rats were randomly divided into five groups. Group 1 served as control and groups 2, 3, 4 and 5 were given isoproterenol @ 85 mg/kg b.wt. subcutaneously for four consecutive days. In addition, groups 3, 4 and 5 received vitamin E (60 mg/kg b.wt), T. cordifolia dose I (100 mg / kg b.wt) and dose II (200 mg / kg b.wt), respectively orally from day 1 till the end of experimental period. Whole blood and serum were collected on 5th, 8th and 12th days to estimate CPK, LDH, AST, ALT, serum troponins, whole blood GSH and erythrocyte antioxidant enzymes (GPx, GSH-R, and CAT). At the end of the experimental period, lipid peroxidation, gross and histopathology of heart was studied. Isoproterenol significantly (P < 0.05) elevated CPK, LDH, troponins and lipid peroxidation products of heart and reduced GSH, GPx, GSH-R and CAT activities, which were restored, to normal following treatment with Vitamin E and Tinospora cordifolia. Gross findings showed enlargement, pallor and ischemic changes of heart and histopathology revealed sarcolysis, vacuolation, hemorrhage, edema and infiltration of inflammatory cells in isoproterenol control, while mild lesions were noticed in treated groups. From the present study it is evident that T. cordifolia and Vitamin E could offer significant cardioprotective and antioxidant actions in isoproterenol induced cardiac damage. However, Vitamin E accomplished better action compared to T. cordifolia....
Limited scientific data are available to validate the use of a variety of indigenous Nigerian plants to treat diseases whose pathogenesis implicates oxidative stress. We have, therefore, investigated the antioxidant ability, phenolic contents and cytotoxic effect of seven widely used Nigerian medicinal plants. Standard antioxidant assays were used to assess the capability of the extracts to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl (.OH), superoxide anion (O2.-) radicals as well as to inhibit lipid peroxidation. Furthermore, the cytotoxic effect of the extracts on human peripheral blood mononuclear cells (PBMC) and A2.01 cell line was investigated ex vivo using 7-amino actinomycin and WST-1 cytotoxicity assay. The extracts possessed significant antioxidant activity compared to standard antioxidants, and had relatively low cytotoxicity. Landolphia owariensis and Irvingia gabonensis had the most potent antioxidant activity in the DPPH assay (IC50 = 8.8 ± 0.2 and 12.7 ± 0.4 μg/ml respectively) compared to ascorbic acid (4.9 ± 0.1 μg/ml) and also significantly inhibited the Fe2+/ascorbate-induced lipid peroxidation (IC50 = 31.9 ± 1.4 and 59.1 ± 1.6 μg/ml respectively). I. gabonensis and Nauclea latifolia were found to be powerful quenchers of .OH radical (IC50 = 25.5 ± 1.7 and 37.6 ± 4.7 μg/ml respectively) compared to α-tocopherol (IC50 =38.9 ± 2.8 μg/ml). The antioxidant activity and lipid peroxidation inhibitory potency of the plant extracts correlated significantly with their total phenolics and flavonoid contents. These results suggest that the inherent antioxidant activity of these extracts could be a substantial contributing factor to their traditional medicinal use....
Peptic ulcer is an illness which is considerably prevalent in a large number of people worldwide. It occurs primarily in that part of G.I.T which is exposed to gastric acid and pepsin i.e. the stomach and duodenum. The major etiological factors of this disorder include stress, smoking, nutritional deficiencies, infections, frequent and indiscriminate use of NSAID’S. The pathogenesis of gastrointestinal disorders is influenced by both aggressive factors (like increased acid-pepsin secretion, bile salts, H.pylori etc.) and defensive factors (such as mucus secretion, mucosal barrier, blood flow, cellular regeneration , endogenous protective agents, prostaglandins and epidermal growth factors). Many allopathic synthetic drugs like proton pump inhibitors , H¬2 receptor antagonists are available in the market but these fail to provide a complete & safe cure. Thus an urgent requirement for safe and efficacious anti-ulcer agent is the necessity of time. Indian medicinal plants, herbs offer a potential solution to combat such disorder. This present article reviews anti-secretory, ulcer-healing and anti-oxidant properties of not only some of the Indigenous herbs but also those available worldwide. To achieve this objective, published literature and reports were studied intensively to consolidate information on the herbs with potential anti-ulcer activity. Eruca sativa, Musa sapientum, Eugenia jambolana, Trigonella foenum along with many others have been summarized in this article....
To evaluate the hepatoprotective activity of Pterospermum acerifolium leafextract against carbon tetrachloride induced hepatotoxicity in vivo and also evaluate free radical scavenging activity in-vitro. The present study was undertaken to evaluate the protective effect of Pterospermum acerifolium leaf extract on carbon tetrachloride induced hepatotoxicity and to elucidate the possible mechanism that underlines above effect in rat. Analyzed parameters included serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), alkaline phosphatase (ALP) and total bilirubin. The active oxygen scavenging activity or free radical scavenging activity, hydroxyl radical scavenging activity and super oxide scavenging activity were also investigated. Pterospermum acerifolium leaf extract exhibited significant hepatoprotective activity as well as free radical scavenging activity by inhibiting DPPH (1,1-diphenyl-2picryl hydrazyl ) , Nitric oxide and Hydroxyl radical Pterospermum acerifolium leaves extract showed hepatoprotective as well as dose dependent free radical scavenging activity in all model....
Although several biological activities have been investigated in different lichen species, their antidiabetic potential has not been investigated yet. This study examined the hypoglycemic activity of methanol and methylene chloride extracts of the lichen Parmotrema grayana (Family: Parmeliaceae). This was tested in healthy adult Wistar male fasting rats using two oral doses (600, 1200 mg/kg, N=six/ group) of methanol and methylene chloride extracts of P. grayana in one percent (1%) methyl cellulose (vehicle). The results showed that, the two doses of methanol and methylene chloride extracts of P. grayana possess marked and significant (p<0.05, Mann - Whitney U - test) blood glucose level lowering activity. This blood glucose impairing activity had a rapid onset (two hours) and lasted up to four hours. Moreover, the two extracts did not induce acute toxicity (in terms of overt signs). It is concluded that, the methanol and methylene chloride extracts of P. grayana have profound oral blood glucose lowering activity (with a swift onset and short duration of action) in rats and it may lead to the development of a potent oral hypoglycemic agent from this lichen for the effective treatment of diabetes mellitus....
Hypoglycemic effect of acacia tortilis (100 mg/kg orally) gum extracted from seeds was evaluated in normal as well as alloxan (150 mg/kg body weight intraperitoneally) induced diabetic rats. Blood sugar levels (fasting & after oral glucose tolerance test) in normal rats were reduced after acacia torticollis gum (100 mg/kg orally) administration. Similar results were obtained when gum was administered to alloxon diabetic rats at different time intervals (0, 1 & 2 hr). Piogliotazone (4 mg/kg oral) was more potent than acacia tortilis gum in reducing blood sugar levels in alloxan diabetic rats....
In vitro, growth inhibitory and cytotoxic effects of hydro-alcoholic extract of Hippophae rhamnoides Linn (HEHR 50-500 µg.ml-1) seeds were investigated on human leukemia (HL-60) cells by Trypan blue exclusion assay while mutagenic effect of HEHR (10-500 µg.ml-1) was evaluated by ames assay using salmonella typhimurium strain (TA-98 and TA-100). All the concentrations of HEHR (50-500µg/ml) produced extremely significant cytotoxic and anti-proliferative effect after 24, 48 and 72 h of exposure. The IC50 value of HEHR on cytotoxicity was found to be 328.67 ± 23.3 and 156.0 ± 12.1 µg/ml at 48 and 72 h respectively on HL-60 cells. Only HEHR (500 µg/plate) produced extremely significant (p<0.001) mutagenic effect on TA98 and TA100 strains, with and without S9 liver mix but all other concentrations were non-significant. Mutagenic effect was more on TA98 strain (frame-shift mutations) compared to TA100 strain (base-pair substitutions). Our results indicate that anti-proliferative and cytotoxic effect of HEHR is not completely due to its mutagenic effect which occurred only with 500µg/ml concentration but all other concentrations used also showed anti-proliferative and cytotoxic effects. Effect of HEHR may also due to the presence of very rich phytoconstituents such as vitamin-E and K, sterol, carotenoides (β-carotene and lycopene etc.), flavonoides etc....
The study was aimed at investigating the pharmacognostic, phytochemical, antimicrobial screening and wound healing activity of different extracts with a view to justifying the use of the plant. This work suggested that results of organoleptic, microscopical and physical evaluation were satisfied the earlier report, none of extracts has shown the presence of emodin and quarcetin in HPLC analysis and maximum amount of sennosides has present in ethanolic extract among the other. The present investigation may be concluded that the plant C. occidentalis is endowed with significant antimicrobial and wound healing activity due to the presence active constituents like sennosides and others, there by justifying its use in the indigenous system of medicine....
Thespesia populnea (Linn.) Soland. belonging to family Malvaceae contains a wide range of chemical compounds such as terpenoids, lipids, glycoside, flavanoids which are responsible for its various pharmacological properties. The various parts of the plant like roots, bark, leaves, flowers and fruits are known to possess different pharmacological properties. The information published about chemical composition and biological activity of Thespesia populnea (Linn.) Soland. is reviewed here. The perspectives of research and therapeutic use of Thespesia populnea (Linn.) Soland. as potent hepatoprotective and antioxidant drug in ayurvedic formulations are discussed here in terms of phytopharmaceutics. The main aim of the present review has to focus on phytochemical, pharmacological and phytopharmaceutics aspects as a medicinal plant, Thespesia populnea (Linn.) Soland....
In the present study Methanol extract of dried leaves of Psidium guajava L. (Guava) were evaluated for their cytotoxic potentiality on Human Cervical Cancer cell lines (HeLa) by Direct cell Contact Assay. Phytochemical screening of the crude leaf extract revealed the presence of some bioactive compounds that may associated with cytotoxic effect on HeLa cell lines. This Methanol leaf extract exhibited pronounced cytotoxic effect (1.6x105 cells/ ml). Plants that showed pronounced cytotoxic activity will be further evaluated for the possible isolation of active antitumour compounds....
The ethanol seed extract of Achras zapota Linn. was evaluated for hepatoprotective activity in rats with experimental liver injury induced by carbon tetrachloride (CCl4) (1ml/kg body weight). The seed extract at the doses of 200 and 400mg/kg was administered for 5 days and the hepatoprotective activity was assessed by estimating the levels of serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), bilirubin, glutathione (GSH), superoxide dismutase (SOD) and total proteins in the rats. Silymarin was used as the standard hepatoprotective drug. The extract showed significant (P<0.05) dose-dependent hepatoprotective activity by decrease in the serum level of SGOT, SGPT, bilirubin and lipid peroxidation while the total protein, glutathione (GSH) and superoxide dismutase (SOD) levels were significantly increased in the animals received the extract at the higher dose level. The results suggest that the ethanol seed extract of Achras zapota possesses excellent hepatoprotective effect against CCl4 induced hepatocellular damage in rats....
Ayurveda is a goldmine for researchers. Unfortunately very few researches are planned with a comprehensive approach. The present situation does not permit mere in-vitro tests to ensure the safety of the drug. Hence, it is very important to give thorough attention before starting the research on ayurvedic drugs. Apart from opinion of ayurveda practitioner detailed discussion with pharmacologist, chemist, biologist statistician and pathologist will help in deciding appropriate model and sample size. it is always better to be precisely knowledgeable in modern terms instead of believing merely because it is stated in literature. It is necessary to treat Ayurveda drug research as New Drug Discovery....
The antioxidant, anti-inflammatory and analgesic activity of Atalantia Monophylla bark extract was evaluated with various in-vitro and in-vivo assay. The anti-oxidant potential of the bark extract were evaluated by DPPH radical scavenging and reducing power assay. Two experimental models of nociception employed were: acetic acid-induced abdominal constriction and formalin-induced pain and carrageenan induced oedema in rats used as inflammatory model. Results showed that bark extract of atalantia monophylla significant antioxidant activity. The results obtained in the current study indicate that the Atalantia Monophylla has potential analgesics and anti-inflammatory activity compared with diclofenac and morphine as standard....
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