Showing papers in "Oriental Pharmacy and Experimental Medicine in 2012"

Saussurea lappa (Kuth root): review of its traditional uses, phytochemistry and pharmacology

Abstract: Saussurea lappa Clarke (Compositae) is a traditionally known and potent plant which is well considered for its medicinal uses in different indigenous Indian systems of medicine. It is popularly known as Kuth root or costus and used in various traditional system of medicine for its anti-ulcer, anti-convulsant, anti-cancer, hepatoprotective, anti-arthritic, anti-viral activities. Several of its activities are well proved and established through in-vitro, in-vivo methods which gave a rationale scientific approach to the traditional claims. Phytochemical compounds isolated from this plant such as costunolide, Isodihydrocostunolide, cynaropicrin etc. were proven to be bio-active and potential source for developing new molecules. Due to the significant proven activities Saussurea lappa is having considerable chance for new drug discovery. This review is an effort to explore the different phytoconstituents and the pharmacological activities of Saussurea lappa.

Investigation of gastro protective activity of Xanthium strumarium L. by modulation of cellular and biochemical marker

Abstract: Peptic ulcer owes its pathological features to disregulated oxido-nitrosative and necrotic changes in gastrointestinal mucosa. Xanthium strumarium L. is a ubiquitous, abundant herb possessing an array of pharmacological properties. In view of anti-inflammatory and antioxidant activity of Xanthium strumarium L., the present investigation was designed to unravel its antiulcer potential in pylorus ligation induced gastric ulcer in laboratory animals. X. srtumarium L. leaves were extracted by refluxing with 95 % ethanol to obtained X. srtumarium L. ethanolic extract (XSEE). After 1 h pretreatment period of XSEE (100, 200 and 400 mg/kg) gastric ulcer was induced by ligation of pylorus portion of stomach. Various parameters including volume of gastric fluid, pH of gastric fluid, free as well as total acidity were measured in the gastric fluid whereas ulcer area, ulcer index, mucin content, superoxide dismutase, myeloperoxidase, nitric oxide, total calcium, histamine level, membrane bound inorganic phosphate (Na-K-ATPase), TNF-α level, DNA fragmentation were determined in the gastric tissue. Pretreatment with XSEE (200 and 400 mg/kg) significantly and dose dependently (P < 0.01 and P < 0.001) decreased ulcer area, ulcer index, macroscopical gastric damage score, volume of gastric fluid, free acidity as well as total acidity and mucin content. It also significantly increased pH of gastric fluid. Rats treated with XSEE (200 and 400 mg/kg) significantly and dose dependently (P < 0.01 and P < 0.001) attenuated decreased level of superoxide dismutase, nitric oxide and Na-K-ATPase. It also significantly decreased level of myeloperoxidase, calcium and inflammatory cytokine i.e. TNF-α. XSEE treated rats showed significant reduction in the pylorus ligation induced apoptotic changes. The possible mechanism by which Xanthium strumarium exerts its gastro-protective action may be due to free radical quenching, DNA repair and down regulation of oxidative-nitrosative stress along with cytokines.

Phytochemical and pharmacological aspects of Siraitia grosvenorii , luo han kuo

Abstract: Siraitia grosvenorii, an herbaceous perennial vine, is native to Southern China and Northern Thailand. This species is well known for its fruit, which is commonly called “luo han guo” or “luo han kuo” in Chinese; “la han qua” in Vietnamese; or arhat, Buddha, or monk fruit in English. Phytochemical research has shown that the fruit of this species is rich in triterpene glycosides that are very sweet, low in calories, and may be used as a substitute for sugar. In addition, many compounds have been isolated from the vines and leaves of S. grosvenorii, including β-amyrin, aloe emodin, aloe-emodin acetate, 5α,8α-epidioxy-24(R)-methylcholesta-6,22-dien-3β-ol, p-hydroxyl benzyl acid, n-hexadecaoic acid, 12-methyltetradecanoic acid, β-sitosterol, and daucosterol. Moreover, a new flavandiol, siraitiflavandiol, has been obtained from ripe S. grosvenorii fruit, while 2 kaempferol glycosides have been isolated from the unripe fruit. Pharmacological results have also shown that S. grosvenorii extracts and purified mogrosides exhibit antidiabetic, anticarcinogenic, antibacterial, antioxidant, and antiallergic effects. Overall, S. grosvenorii could potentially serve as an important source of pharmaceutical and sweetener compounds for a wide range of food products.

Determination of role of GABA and nitric oxide in anticonvulsant activity of Fragaria vesca L. ethanolic extract in chemically induced epilepsy in laboratory animals

Abstract: The aim of the present study was to investigate anticonvulsant effect of Fragaria vesca L. ethanolic etract in chemically induced epilepsy.Fragaria vesca L. ethanolic extract (FVEE) was prepared by extracting the fruit with 95 % ethanol. Seizures were induced by intraperitoneal injection of pentylenetetrazole, strychnine, isoniazid and subcutaneous injection of picrotoxin in male swiss albino mice. The in-vitro parameters were also determined including brain gamma amino butyric acid, nitric oxide.Single dose of PTZ, PTX, STR and INH resulted in resulted in hind-limb, tonic-clonic convulsion along with mortality in mice. Treatment with FVEE (250 and 500 mg/kg, p.o.) significantly and dose dependently (P < 0.01 and P < 0.001 respectively) attenuated onset of convulsion and duration of tonic convulsion induced by PTZ, PTX and INH. It also significantly inhibited the incidence of convulsion and mortality in the mice. Mice treated with FVEE (250 and 500 mg/kg, p.o.) showed significant elevation in brain GABA level and lowering in NO level as compared to vehicle treated mice. Mice treated with FVEE showed significant reduction in the locomotor activity. Treatment with FVEE failed to produce any significant change in STR induced convulsion.The findings of present investigation suggest that FVEE bears a profile similar to agent elevating the inhibitory neurotransmitter in brain and restoring the excitatory neurochemistry behind epileptic seizures. Further investigations are being carried out to characterize the biochemical nature to understand the active principles along with structure activity relationship.

Study of clinically used and recently developed antimycobacterial agents

Abstract: Tuberculosis is one of most pervasive, respiratory transmitted diseases and has spread to every corner of the globe According World Health Organization report, as much as one-third of the world’s population is currently infected by tuberculosis There has been considerable interest in the currently used antimycotubercular compounds to inhibit or prevent mycobacterium species These mycobacterium species have developed resistant against currently used drugs and produced toxic effect on long duration of therapy These agents have different structure and almost all compounds having heterocyclic ring having one and more than one heteroatoms These observations have been guiding for the currently used and newly developed antitubercular agents that possess potent antimicrobial activity and their side effects, activity against multi drug resistance MDR, XDR mycobacterium, and also in patient co-infected with HIV/AIDS

Hepatoprotective and antioxidant activities of crude fractions of endophytic fungi of Ocimum sanctum Linn. in rats

Abstract: Endophytic fungi are a rich source of novel organic compounds with interesting biological activities and a high level of biodiversity. In the present investigation, an attempt has been made to isolate, characterize and screen the Tulsi (Ocimum sanctum Linn.) root fungal endophytic fractions (TRF) for hepatoprotective and antioxidant activities. Endophytic fungi from Ocimum sanctum Linn. roots were isolated and cultured aseptically in PDA media. The full fledged grown fungus cultures were fermented in potato dextrose broth and fractionated using ethyl acetate. TRF-1 and TRF-2 were subjected free radical scavenging activities against 2,2-diphenyl-1-picrylhydrazyl, hydroxyl free radicals and reducing power assay. TRF-1 was found to be potential free radical scavenger with IC50 values of 71.83 μg/ml for DPPH and 110.85 μg/ml for hydroxyl radical respectively. TRF-1 and TRF-2 were further assessed for hepatoprotective activity in CCl4 induced hepatotoxicity in-vivo. Results showed that TRF-1 (200 mg/kg p.o.) and TRF-2 (200 mg/kg p.o.) significantly reversed the actions of carbon tetrachloride induced hepatotoxicity, as evident by restoration of serum AST, ALT, ALP, bilirubin, triglycerides and protein level to normal values as compared to CCl4 treated group. Restoration of altered LPO (p < 0.001), GSH (p < 0.01) and catalase (p < 0.01) by TRF-1 suggests that the hepatoprotective activity may be attributed to its antioxidant action. This was further supported by histopathological studies. TRF-1 was subjected to rDNA sequencing studies by PCR technique. Based on the morphological and molecular characterization, the fungus was identified as Paecilomyces variotti Bain. Therefore, endophytes from medicinal plants represent great potential for the discovery of new pharmacologically active metabolites.

Comparative antihyperglycaemic and antihyperlipidemic effect of Origanum majorana extracts in NIDDM rats

Abstract: Diabetes mellitus is a metabolic disorder prevailing throughout the world irrespective of age, sex and race. The present study deals with phytochemical, antioxidant, antihyperglycaemic and antihyperlipidemic potential of Origanum majorana (OM) leaves. Various extracts of OM were used for the study such as, hydrodistilled volatile oil (OMO), petroleum ether extract (OMPE), methanolic extract (OMM) and aqueous extract (OMW). Three doses of each extract viz. 100, 200 and 400 mg/kg p.o. were used for the study. Streptozotocin, STZ (65 mg/Kg, i.p.) along with nicotinamide (120 mg/kg, i.p.) was used to induce non insulin dependent diabetes mellitus (NIDDM) in rats. Various biochemical markers of blood and tissue origin were estimated. The results were statistically analyzed by ANOVA followed by Dunnett’s test. Glibenclamide, a well known antidiabetic drug, was used as a standard. Volatile oil (OMO, 200 and 400 mg/kg p.o.) and methanolic extract (OMM, 200 and 400 mg/kg p.o.) exhibited dose dependent significant (p < 0.01) antihyperglycaemic activity. The aqueous (OMW, 200 and 400 mg/kg p.o.) had moderate (p < 0.05) effect on blood sugar level. The volatile oil (OMO, 100 mg/kg p.o.) was less significant (p < 0.05) in lowering the elevated triglyceride and cholesterol levels. Whereas; methanolic (OMM, 200 and 400 mg/kg p.o.) and aqueous (OMW, 200 and 400 mg/kg p.o.) extracts substantially (p < 0.01) showed antihyperlipidemic effect. From this study, it was concluded that the volatile oil and methanolic extract of Origanum majorana leaves could prove to be beneficial in management of NIDDM and its associated lipid imbalance.

Anti-hyperglycaemic and lipid lowering potential of Adenanthera pavonina Linn. in streptozotocin induced diabetic rats.

Abstract: In India, Adenanthera pavonina is traditionally used in the treatment of diabetes mellitus and lipid disorders. In the present study, the antihyperglycaemic and lipid lowering effect of Adenanthera pavonina seed aqueous extract (APSAE) was evaluated using streptozotocin induced diabetes in rats. Streptozotocin was given at the dose of 55 mg/kg, i.p. After induction of diabetes, APSAE was administered for 30 days p. o. and simultaneously different biochemical parameters like plasma glucose, HbA1c, serum triglyceride, cholesterol, LDL-cholesterol and HDL-cholesterol were estimated. Diabetic control showed significant increase (P < 0.01) in plasma glucose, serum triglyceride, cholesterol, LDL-cholesterol and significant decrease (P < 0.01) in serum HDL-cholesterol and HbA1c. Treatment with APSAE showed significant reduction (P < 0.01) in plasma glucose when compared with diabetic control. The elevated levels of serum triglyceride and cholesterol levels were significantly reduced (P < 0.01) by APSAE. APSAE treatment for 30 days showed significant decrease in serum LDL-cholesterol (P < 0.01) and significant increase in serum HDL cholesterol level (P < 0.01). Moreover, diabetic control there was significant decrease in HbA1c which was significantly increased (P < 0.05) by treatment with APSAE. Hence, from the result obtained in the present study it can be confirmed that Adenanthera pavonina has the potential to treat diabetes condition and associated lipid disorders.

Effect of Cynodon dactylon on rotenone induced Parkinson's disease

Abstract: In the present study, the aqueous extract of Cynodon dactylon (AECD) Pers. (Graminae) was evaluated for anti-parkinson’s activity in rats. The anti-parkinson’s effect of AECD was studied against rotenone (2 mg/kg, s.c.) - induced parkinsons in rats. In this study, chronic administration of rotenone in rats (28 days) produced motor dysfunctions like catalepsy and muscle rigidity along with a reduction in locomotor activity. Rotenone administration was also found to generate oxidative stress in the brain as evident from an increase in the level of TBARS and decrease in the levels of SOD and GSH. Pretreatment with AECD resulted in a significant (p < 0.001) decrease in catalepsy and muscle rigidity along with a significant (p < 0.001) increase in locomotion as compared to the rotenone-treated control group. AECD treated rats also showed a reduction in the TBARS level and an increase in the GSH, SOD and CAT levels; thus reducing the oxidative stress in the brain of animals. The study thus proved that Cynodon dactylon treatment significantly attenuated the motor defects and also protected the brain from oxidative stress, both induced by rotenone. These results strongly indicate the possible therapeutic potential of Cynodon dactylon as an antioxidant in Parkinson’s disease and other movement disorders.

Discovery of potential aldose reductase inhibitors using in silico docking studies

Abstract: The primary objective of this study was to investigate the aldose reductase inhibitory activity of flavonoids using in silico docking studies. In this perspective, flavonoids like Apigenin, Baicalin, Daidzein, Epigallocatechin, Galangin, Genistein, Hesperitin, Naringenin, and Scopoletin were selected. Epalrestat, a known aldose reductase inhibitor was used as the standard. In silico docking studies were carried out using AutoDock 4.2, based on the Lamarckian genetic algorithm principle. In the docking studies, three important parameters like binding energy, inhibition constant and intermolecular energy were determined. The results showed that all the selected flavonoids showed binding energy ranging between −9.91 kcal/mol to −7.52 kcal/mol when compared with that of the standard (−8.73 kcal/mol). Intermolecular energy (−11.40 kcal/mol to −8.71 kcal/mol) and inhibition constant (54.78 nM to 3.10 μM) of the flavonoids also coincide with the binding energy. All the selected flavonoids contributed aldose reductase inhibitory activity because of its functional groups. These molecular docking analyses could lead to the further development of potent aldose reductase inhibitors for the treatment of diabetes.

Gynura procumbens modulates the microtubules integrity and enhances distinct mechanism on doxorubicin and 5-flurouracil-induced breast cancer cell death

Abstract: Recent studies both in vitro and in vivo of G. procumbens exhibits chemopreventive properties for tumor inhibition on several types of cancer. Our study was carried out to observe the anticancer property of ethyl acetate fraction of G. procumbens leaves (FEG) on breast cancer cells as well as the co-chemotherapeutic potential, and to investigate its molecular mechanisms. 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to measure the growth inhibitory effect of FEG, doxorubicin (DOX), and 5-fluorouracil (5-FU) and their combination. Flowcytometry, 4′,6-diamidino-2-phenylindole (DAPI) staining, and immunobloting were used to explore the mechanism of cell cycle arrest and apoptosis. FEG inhibited cell proliferation, induced G1 phase arrest and apoptosis. The inhibitory effect of FEG was enhanced when combined with Dox and 5-FU. The apoptosis induction was related to the increase of c-PARP expression after combination treatment of FEG and Dox or 5-FU on MCF-7 cells. However, treatment of DOX, 5-FU, and FEG on T47D cells, resulting no significance DNA fragmentation and nuclei condensation evidance. Only combination treatment of 5-FU + FEG showed c-PARP expression in T47D cells. In T47D cells, The FEG treatment also caused the decrease of microtubule expression as shown by Western blotting assay. The decreasing level of microtubul expression might be caused by protein aggregation, as shown by immunostaning using α-tubulin antibody. All these results suggest that FEG potentiates the DOX and 5-FU efficacy on MCF-7 and T47D cells. FEG induces T47D cell death through different mechanism than MCF-7 that proposed to be mitotic catastrophe. The FEG may have specific targeted on microtubule integrity modulation leading to the cell cycle arrest and proliferation inhibition. Further FEG could be developed as a co-chemotherapeutic agent for reducing side effect and have specific molecular target for breast cancer.

Anti arthritic activity of aqueous extract of Indian black tea in experimental and clinical study

Abstract: Aim of the study was to evaluate the anti-arthritic activity of aqueous black tea extract against experimental arthritis model and in clinical study. Black tea leave (Assam, CTC, India) was collected commercially from authenticated tea supplier. BTE was prepared with MilliQ water and expressed in terms of dry weight. Rheumatoid arthritis was developed in male albino rats by FCA injection into the sub planter surface of hind foot and divided into five groups: Group-1 (Gr.1): Sham control; Group-2 (Gr.2) : Arthritic control, Group-3 (Gr.3): Standard anti-arthritic drug Indomethacin, Group-4 (Gr.4) & Group-5 (Gr.5) : BTE (high and low dose). Anti-arthritic activity of BTE was examined in animal models through physical, urinary, serum parameters and clinical serum samples. Histological studies of joints were done. Clinical study with BTE performed on the rheumatoid arthritis patients and the serum cytokines (IL-10, IL-6, IL-4) was done. Data was expressed in terms of mean ± SEM (n = 6). The data were subjected to one way analysis of variance (ANOVA) followed by Tukey’s test using Graph Pad InStat3 software to establish statistical significance. Physical, urine, serum parameters and anti-oxidant markers, changed significantly in FCA induced arthritic rats but restored in BTE treated groups. Histological studies of joints showed restoration of the structural architecture of the joint after BTE treatment. Clinical study showed decreased cytokines level in the BTE treated group of patients as compared with the arthritis control group of patients. Data was expressed in terms of mean ± SEM (n = 6). The data were subjected to one way analysis of variance (ANOVA) followed by Tukey’s test to establish statistical significance (*p < 0.05, **p < 0.01, ***p < 0.001). The findings showed BTE had anti-arthritic activity in both experimental and clinical study. Further studies required to ascertain the action of BTE extract at molecular level.

In vivo evaluation of anti-diarrheal activity of the rhizome of Nymphaea alba (Nymphaeaceae)

Abstract: Ethanol extract of the of rhizome of Nymphaea alba, at graded doses was investigated for anti-diarrhoeal activity in term of reduction in the rate of defecation in castor oil induced diarrhoea and anti-inflammatory activity in term of reduction in inflammation of rat paw. To understand the mechanism of its anti-diarrhoeal activity, its effect was further evaluated on intestinal transit and castor oil induced intestinal fluid accumulation (enteropooling). At various doses (100 & 200 mg/kg body weight) the extract showed a remarkable anti-diarrhoeal activity evidenced by the reduction in the rate of defecation. Results are comparable to that of standard drug diphenoxylate (5 mg/kg body weight). A single oral dose of N. alba extract of 100 mg/kg body weight produced a significant decrease in the severity of diarrhoea. Extract produced profound decrease in intestinal transit (25.73 and 37.29%) also significantly inhibited castor oil induced enteropooling comparable to that of intraperitoneal injection of standard drug atropine sulphate at doses of 0.1 mg/kg body weight and loperamide at 5 mg/kg body weight respectively. Results indicate N. alba possess significant anti-diarrhoeal activity and may be a potent source of anti-diarrhoeal drug in future. But the extract did not show anti-inflammatory activity.

Formulation, standardization and pharmacological evaluation of a poly herbal traditional remedy -Ashwagandharishtam

Abstract: Ayurvedic formulations were considered the best and safer alternatives for synthetic drugs. But the demand to such products is diminishing due to lack of standardization. Ashwagandharishtam, a fermented kind of ayurvedic formulation, is used to treat epilepsy, nervous disorders, skin diseases, immune disorders and rheumatism. In the present study, the standardization of Ashwagandharishtam using sophisticated techniques were attempted for assessing the quality and safety of herbal products involved in it. It was formulated according to a working formula and its physico-chemical, pharmacological and biological parameters were determined. The results of physicochemical studies showed that the values were under acceptable limits as per the Ayurvedic Pharmacopoeial specifications. FTIR studies of formulation revealed the presence of functional groups similar to Ashwagandha powder. The heavy metal content in the formulation is determined using Atomic Absorption Spectroscopy. HPTLC reports proved the presence of biomarker, withanolide-A in ashwagandharishtam which helped in its chemical standardization. The anti-epileptic activity of ashwagandharishtam was evaluated by Maximal electro shock (MES) method in rats. It exhibited a dose dependent significant (P < 0.001) reduction in various phases of epileptic seizures when compared with that of standard phenytoin. It was also assessed for its anti inflammatory activity in carrageen induced paw edema method which showed a good activity comparable to standard thus making it biologically standardized.

In silico docking studies of phosphodiesterase inhibitory activity of commercially available flavonoids

Abstract: The primary objective of this study was to investigate the phosphodiesterase inhibitory activity of flavonoids using in silico docking studies In this perspective, flavonoids like Apigenin, Baicalin, Chrysin, Genistein, Scopoletin and Caffeine were selected Caffeine, a known phosphodiesterase inhibitor was used as the standard In silico docking studies were carried out using AutoDock 42, based on the Lamarckian genetic algorithm principle In the docking studies, three important parameters like binding energy, inhibition constant and intermolecular energy were determined The results showed that all the selected flavonoids showed binding energy ranging between −759 kcal/mol to −566 kcal/mol when compared with that of the standard (−477 kcal/mol) Inhibition constant (272 μM to 7103 μM) and intermolecular energy (−849 kcal/mol to −626 kcal/mol) of the flavonoids were coincide with the binding energy All the selected flavonoids contributed phosphodiesterase inhibitory activity because of its functional groups These molecular docking analyses could lead to the further development of potent phosphodiesterase inhibitors for the treatment of inflammatory disorders

Syzygium cumini (L.) skeels seed extract ameliorates in vitro and in vivo oxidative potentials of the brain cerebral cortex of alcohol-treated rats Syzygium cumini (L.) skeels seed extract inhibits oxidative potentials of brain

Abstract: We investigated the effect of Syzygium cumini(L.) Skeels seed extract on the oxidative stress of brain cortical tissues of alcohol-treated rats. The in vitro antioxidative effect of methnolic S. cumini seed extract was initially compared with those of the buytylated hydroxyl toluene (BHT) and Vitamin C, by determining their DPPH-free radical scavenging activity. The S. cumini seed extract exhibited stronger free radical scavenging activity than those of the BHT and Vitamin C. Cortex homogenates were then directly incubated with 15% ethanol and/or Fenton’s reagent (H2O2 + Fe2SO4) to induce in vitro oxidative stress in the absence or presence of S. cumini seed extract . The S. cumini seed extract significantly reduced the levels of lipid peroxide (LPO) in the cortical homogenates. Twenty four rats were then divided into four groups: Control, S. cumini seed extract (SE)-administered, 15% ethanol-fed (EtOH) and EtOH + SE rats. The oral administration of the extract (400 mg/kg BW.day) for 8 weeks significantly (P < 0.05) decreased the levels of LPO in the cortex of the EtOH + SE rats, suggesting that S. cumini seed not only scavenged the DPPH-free radicals and obstructed the ethanol/Fenton’s reagents-induced in vitro oxidative stress of the cortical tissues but also reduced their in vivo formation. These results suggest that S. cumini seed could be used as a potential antioxidant therapy for alcoholics.

Anticataract activity of rhamnocitrin isolated from Bauhinia variegata stem bark

Abstract: A cataract is any clouding or opaque area in the eye’s natural lens, which is normally crystal clear, is the leading cause of blindness worldwide. It accounts for approximately 42% of all blindness. Approximately 25% of the population over 65 and about 50% over 80 age has serious loss of vision because of cataract. Most cataracts progress and eventually hamper vision. Multiple mechanisms have been implicated in the development of cataract. But the exact pathogenesis which leads to opacification is not clearly known. Oxidative damage to the lens has been recognized as the initiating event in the pathogenesis of cataracts. In cataract, the oxidation-antioxidant equilibrium shift more towards oxidative stress. Accordingly, antioxidants could prove potential anticataract agents. Rhamnocitrin, a flavonoid, possess strong antioxidant effects; can be used effectively to manage the cataract. Therefore, anticataract activity of rhamnocitrin (10, 20, 40 and 80 μg), isolated from Bauhinia variegata (Leguminosae) stem bark, was studied in ovine and chick embryo lens model. It showed a significant protection against cloudiness in lenses induced by hydrogen peroxide and hydrocortisone in a dose dependent manner. The findings suggest that rhamnocitrin possess significant anticataract activity and act most likely due to its antioxidant property.

CNS depressant activity of Castanopsis indica leaves

Abstract: Castanopsis indica (Roxb. ex Lindl.) A.DC. (Fagaceae) is commonly known as ‘Dhalne katus’ and ‘Indian chestnut tree’, found throughout the Himalayan region. The purpose of this investigation was to evaluate the effect of methanol extract of C. indica leaves (MECI) on Central Nervous System using a number of neuropharmacological experimental models in Swiss albino mice. The treatment with MECI at doses of 25 and 50 mg/kg, i.p. caused: signs of central nervous system depressant action confirmed by significant inhibitory effect on acetic acid induced writhing as compared with acetic acid control group indicate an analgesic effect. Anticonvulsant activity was seen as there was delays in the onset of pentylenetetrazole (PTZ) induce convulsion as well as decrease in its mortality rate. The MECI produced a dose-dependent reduction of the onset and potentiated duration of pentobarbitone-induced hypnosis, reduction of locomotor and muscle relaxant activities determining by using actophotometer and rotarod tests. MECI in a dose-dependent manner significantly reduced the immobility time of mice in both forced swim test (FST) and tail suspension test (TST). These results suggest that the MECI has an analgesic effect, behave as a potential anticonvulsant and central nervous system depressant action.

Antioxidant, analgesic, cytotoxic and antidiarrheal activities of ethanolic Zizyphus mauritiana bark extract

Abstract: The primary objective of this study was to investigate the pharmacological potential of the ethanolic extract of Zizyphus mauritiana bark. Antioxidant, analgesic, cytotoxic and antidiarrheal activities of the extract were investigated using 1, 1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay, acetic acid induced writhing inhibition, brine shrimp lethality bioassay and castor oil induced diarrhea inhibition respectively. The extract showed remarkable free radical scavenging activity with an IC50 of 27.47 μg/mL. The extract produced significant (P < 0.001) writhing inhibition at the doses of 250 mg and 500 mg/kg in acetic acid induced writhing in mice. With the extract, significant lethality to brine shrimp was found with LC50 value at 92.79 μg/mL. In antidiarrheal activity test, the extract produced 1.25 h latent period of diarrheal induction and 75.2% inhibition in diarrheal episodes compared to positive standard which showed 1.3 h of latent period and 80.55% inhibition in diarrheal episodes. Different phytoconstituents present in the bark might be responsible for biological activities found with this study. The results of this study support the traditional uses of this plant part and could form the basis of further investigation including compound isolation.

Fermentation of traditional medicine: present and future

Abstract: Traditional medicine has been used for a very long time, but scientific evidence regarding the therapeutic properties of traditional medicine has recently been required. Many components of herbs have been isolated, and their biological activities, evaluated. However, many of these herbs need to be biotransformed by bacteria in the large intestine in order to be biologically activated. The presence or absence of metabolically active bacteria in the large intestine is therefore important for biological activation. Inter-individual differences exist in the composition of human intestinal bacteria; biotransformation of traditional medicine outside the human body by using bacterial strains such as lactic acid bacteria (which are considered safe) has been used in an attempt to overcome such differences. This process yields what is referred to as fermented traditional medicine (FTM). FTMs have garnered attention for their enhanced biological activity compared to traditional medicine. Several studies using single herbs and formula support the availability of FTMs. However, the concrete concept of FTM is not yet established, and further discussions regarding the bacterial strains that have been used during fermentation and their safety are necessary. This report provides a general review and discussion of FTM with a view to promote better usage and safety in the future.

Evaluation of hepatoprotective activity of ethanol extract of Coccinia grandis (L.) Voigt. leaves on experimental rats by acute and chronic models

Abstract: Coccinia grandis Linn. (Cucurbitaceae) is a climbing perennial branched herb, distributed throughout India. Other plants under the same family have been reported for their hepatoprotective activity. The aim of this work was to study the hepatoprotective effect of crude ethanolic extract from the leaves of C. grandis against liver damage induced by Paracetamol and CCl4 in rats. Administration of Paracetamol (750 mg/kg/day) and CCl4 (3 ml/kg/day) showed a marked increase in SGOT, SGPT, ALP, bilirubin (total, direct), total proteins, globulin, cholesterol and decrease in albumin in comparison with the normal control group. The effect of ethanol extract of C. grandis at 150 mg/kg and 300 mg/kg doses reduced the serum activities caused by Paracetamol and CCl4, which were observed to be statistically significant when compared with that of the control group. The activity exhibited/inhibited by the plant extract was found to be comparable to that of the standard hepatoprotective drug, Silymarin. Silymarin provided a better inhibition or exhibition of the biochemical parameters induced by paracetamol and carbon tetrachloride in rats. The activity may be due to the presence of either alkaloids or triterpenoids or reducing sugars or their combinations, as obtained from the preliminary phytochemical screening of the leaves of the plant. The extract showed no signs of acute toxicity up to a dose level of 3.2 g kg−1 in rats by oral route. Thus, it could be concluded that ethanolic extract of C. grandis leaves possessed significant hepatoprotective activity.

ACE inhibiton activity of standardized extract and fractions of Terminalia bellerica

Abstract: The fruit of Terminalia bellerica L. (Combretaceae) is an important ingredient of ‘Triphala’, which is a popular Ayurvedic formulation traditionally used to treat hypertension, to reduce cardiac depression and to decreases the risk factors associated with the heart. This study aimed to investigate the angiotensin converting enzyme (ACE) inhibitory activity of T. bellerica. Standardized hydro alcoholic extract (TBHA) and its various subfractions including hexane fraction (TBH), ethyl acetate fraction (TBE), n-butanol fraction (TBB) and aqueous fraction (TBW) at the concentration of 10–1000 μg/ml together with standard Captopril 3.6 ng/ml was compared. TBE fraction was undertaken to isolate the gallic acid. Further quantification of gallic acid in the crude extract and fractions was made with HPLC. Among all fractions the activity was found to be maximum in TBE with an IC50 = 338.54 ± 18.34 μg/ml while crude TBHA and other fractions TBB, TBH and TBW were found less potent. Isolated gallic acid from the TBE fraction shown ACE inhibitory activity with IC50 of 257.29 ± 9.39 μg/ml. TBE found to contain maximum amount of gallic acid (71.05 ± 6.274 mg/g of extract). The presence of gallic acid along with other metabolites in the extract and fractions might be responsible for the ACE inhibitory activity. T. bellerica extract/fractions suggested its suitability as a functional food for pharmaceutical purpose to be used against hypertension and other related diseases.

Gastrointestinal effects of triterpenoid enriched extract of Trichosanthes dioica root in albino mice

Abstract: Trichosanthes dioica Roxb. (Cucurbitaceae), is a dioecious climber, traditionally used in India for several medicinal purposes including purgative. The present study aimed to evaluate the gastrointestinal effects (laxative and prokinetic) of triterpenoid enriched extract of T. dioica root (CETD) in Swiss albino mice. The laxative activity of CETD (50 and 100 mg/kg body weight per os) was evaluated by assessing the different excretory bowel activities in naive (non-constipated) and in drug (loperamide)-induced constipation in mice. Further, the gastrointestinal transit was measured in both naive and in constipated mice to ascertain the prokinetic effect. Castor oil (0.5 ml/mouse per os) was used as reference drug. CETD significantly and dose dependently increased all excretory bowel activities and gastrointestinal transit in both naive and in constipated mice. CETD at 100 mg/kg body weight was found to be the most active causing diarrhoea in mice. Therefore, T. dioica root extract demonstrated remarkable stimulant laxative and prokinetic effects in Swiss albino mice validating its prime ethnomedicinal usage in the Indian traditional medicine.

Effect of successive extracts of Stachys tibetica Vatke (Lamiaceae) in anxiety

Abstract: Stachys tibetica Vatke (Lamiaceae) is an important medicinal plant in the folk medicine of Ladakh, India and Tibet for the treatment of various mental disorders. Infusion and decoction of the whole plant is used as a cup of tea in severe fever, headache and to relieve tension. Present study is aimed to evaluate the anxiolytic effect of successive extracts of Stachys tibetica Vatke (SES). Stachys tibetica Vatke (1 kg) was subjected to successive extraction in a soxhlet apparatus with different solvents of increasing polarity like petroleum ether (40–60 °C), chloroform, ethyl acetate, methanol and finally decocted with water (yield 7.08 %, 3.98 %, 2.02 %, 16.40 % and 21.53 % w/w respectively). All successive extracts were subjected to phytochemical screening. Rutin was identified by TLC method in the extracts. SES were evaluated for anxiolytic activity using elevated plus maze and light/dark arena tests in rats. Phytochemical studies showed the presence of flavonoids, terpenoids, saponins, glycosides, tannins, alkaloids etc. which might be responsible for anxiolytic activity. TLC analysis of the extracts also showed the presence of flavonoids (rutin). SES increased number of entries and time spent in open arms on the elevated plus maze test while as in the light/dark arena test; they showed an increase in number of crossings and time spent in light arena. The results of both the models of anti-anxiety studies were reflected on the 1st, 3rd and 7th day. Methanol and aqueous showed the most, chloroform and petroleum ether (40–60 °C) intermediate and ethyl acetate the least anxiolytic activity (*P < 0.05, **P < 0.01, ***P < 0.001) in both the models. The results strongly justify the use of this plant for treatment of anxiety. Further studies are in progress in our laboratory to isolate and identify the components responsible for anxiolytic activity and the mechanism of action involved.

A simple, rapid and sensitive spectrofluorimetric method for the determination of camptothecin

Abstract: Camptothecin (CPT) represents a clinically useful class of anticancer agent. Proper identification and quantitation of the CPT in the plant extracts and in-vitro cell culture extracts is fundamental to assess the CPT content and its biosynthetic potential in plants. A simple, sensitive and rapid, spectrofluorimetric method has been developed and validated for the quantitative estimation of camptothecin. The method was validated in terms of linearity (2–20 ng/ml), precision (intra-day variation below 0.15, inter-day variation below 1.2), and accuracy (98.0 to 100.2%). The limit of detection and limit of quantification for CPT were found to be 0.10 ng/ml and 0.36 ng/ml, respectively. The developed spectrofluorimetric method provides a rapid and cost effective method for the routine analysis of CPT in plant extracts and tissue culture samples. The developed method was successfully used for the estimation of CPT in natural plant extracts and cell culture extracts. The Nothapodytes nimmoniana callus cells having nearly 3-fold higher CPT content over the leaf (0.005%) explant of the plant. The highest CPT content was found in the stem part (0.092%) followed by the fruit (0.088%). The method is simple, sensitive and precise; it can be used for the routine quality control testing of formulations containing CPT.

Evaluation of anti-inflammatory, analgesic, antipyretic and antiulcer activity of Punarnavasava: an Ayurvedic formulation of Boerhavia diffusa

Abstract: Punarnavasava, an Ayurvedic liquid dosage form containing self generated alcohol is commonly used to treat inflammatory conditions and edema. In the present study, we evaluated anti-inflammatory, analgesic, antipyretic, and antiulcer activity of three different brands of Punarnavasava. The formulation significantly inhibited carrageenan-induced rat paw edema, cotton pellet-induced granuloma, formalin-induced paw licking, yeast induced hyperpyrexia and pyloric ligated ulcers in rats. The study concludes that Punarnavasava has anti-inflammatory, central as well as peripheral antinociceptive, antipyretic and antiulcer activity and thus justifies its use in inflammatory conditions.

Formulation, characterization and in vitro evaluation of herbal sunscreen lotion

Abstract: Natural substances extracted from plants have recently been considered as potential sunscreen resources owing to high ultraviolet ray absorption and antioxidant activity. The decrease in the intensity of UV radiation reaching the skin through sunscreens may reduce the risk of sun-induced skin cancer. The present study attempts to develop sunscreen lotions, possessing broad spectrum of anti-UV radiation effectiveness with reduced concentration of chemical UV filters, from the extracts of bioactive products such as Curcuma longa L. (Zingiberaceae), Aloe vera (Liliaceae) and Alpinia galanga Willd. The effectiveness of the product was evaluated using Sun Protection Factor (SPF). Curcumin was selected as potential bioactive agents due to their phytochemical compositions possessing considerable content of polyphenolic compounds and Alpinia galanga is used as key ingredient in various commercial sunscreen lotions as it has skin protectant action against UV rays and boosts the activity of conventional sunscreens. The sunscreen lotions were prepared using three different compositions F1, F2 and F3 and evaluated for their stability, safety and SPF. Results showed that the sunscreen lotions were non-mutagenic, non-irritant, stable and possess SPF for normal skin. The efficacy when tested with a standard was observed to be same as that of a marketed sunscreen with SPF 55 and SPF 20. From the present study, formulation F2 having curcumin extract was proved to be stable and effective with high SPF compared to F1 and F3.

Phytochemical investigation and simultaneous study on antipyretic, anticonvulsant activity of different leafy extracts of smilax zeylanica Linn

Abstract: The present study was carried out to investigate the anti-pyretic and anticonvulsant activity of petroleum ether, ethyl acetate, n-butanol and ethanol extracts of Smilax zeylanica Linn, leaves using experimental animal models. The extracts were screened for alkaloids, steroids, proteins, flavanoids, saponins, mucilage, carbohydrates, tannins, fats and oils. Anti-pyretic activity was evaluated using the brewer’s yeast-induced pyrexia in rats. The extracts in dose levels of 200 mg/kg orally were used for anti-pyretic studies. The petroleum ether extracts of leaves of Smilax zeylanica Linn produced significant (P < 0.01) anti-pyretic activity. Anticonvulsant activity of above extracts was evaluated by using strychnine induced tonic convulsion of Swiss albino mice. All extracts were able to reduce convulsion in mice. The Ethyl acetate extracts of Smilax zeylanica was found to have good anticonvulsant activity in comparison to other extracts which was verified as statistically significant by using one way ANOVA at 1% level of significance *shows P value < 0.01.

Evaluation of anti-inflammatory and antioxidant potential of the kernel root of Xylocarpus mekongensis (Lamk.) M. Roem

Abstract: Anti-inflammatory and antioxidant activities of the crude ethanolic extract of the kernel root of Xylocarpus mekongenesis (Lamk.) M. Roem. (Meliaceae) was evaluated in different methods. The extract showed significant anti-inflammatory activity in carrageenan-induced oedema test in rats showing 69.42 % reduction in the paw volume (P < 0.01) comparable to that produced by the standard drug indomethacin (70.25 %) at 24 h when the extract was fed at the dose of 400 mg/kg body weight. The percentage inhibition of the oedema paw volume was statistically significant (p < 0.05) when compared with the indomethacin treated animals at 0.5, 1, 2, 4 and 6 h. The extract exhibited IC50 value 4.78 μg/ml in DPPH free radical scavenging activity test that was found to be very significant and comparable to that of the standard antioxidants ascorbic acid and BHA (1.9372 and 4.81 μg/ml) respectively. In nitric oxide radical scavenging test, the IC50 value was also found fairly significant 57.37 μg/ml when compared to standard ascorbic acid (36.81 μg/ml). In reducing power test, the maximum absorbance of the same extract was observed as 1.923 at 100 μg/ml and that of ascorbic acid and BHA were 2.8111 and 1.0314 respectively. The extract showed highest antioxidant capacity at 100 μg/ml concentration expressed as equivalents of ascorbic acid (1.44). The total phenolic content of the extract was also found quite high (342.15 ± 0.92 mg/g of gallic acid equivalent). Therefore, the results of this study suggest the probable anti-inflammatory and antioxidant activities of the ethanolic extract of X. mekongenesis kernel root and justify its use in traditional medicines.

Antihistaminic activity of Abrus precatorius using clonidine induced catalepsy in mice

Abstract: Abrus precatorius Linn (Fabaceae) is a climbing shrub; leaves are pinnate with many pairs of leaflets. Leaves 5-10 cm long, leaflets 10-20 pairs, opposite, flowers are pink clustered. The roots, stems, and leaves contain glycyrrhizin, sweet in taste. Leaves are traditionally have been used in the treatment of fever, asthma and caries of teeth. Clonidine induces catalepsy by releasing histamine from mast cells which is responsible for different asthmatic conditions. The leaves of A. precatorius traditionally used for asthma, hence objective of present study was to evaluate antihistaminic activity of A. precatorius using clonidine induced catalepsy in mice. In present study ethanol extract of A. precatorius leaves (EAPL) at doses 100, 125, 150 mg/kg i.p were evaluated for antihistaminic activity using clonidine and haloperidol induced catalepsy in mice. Finding of investiga- tion showed that chlorpheniramine maleate (CPM) and EAPL inhibit clonidine induced catalepsy significantly P<0.001 when compare to control group, while CPM fail to inhibit haloperidol induced catalepsy. Present study concludes that EAPL possesses antihistaminic activity.