bluuebunny/crossref_metadata_2025_split huggingface dataset:
Hypotensive and spasmolytic activities of ethanolic extract of Capparis cartilaginea
Authors: Gilani Anwar‐Ul Hassan , Aftab Khalid 
Published: October 2006

AbstractAn ethanolic extract of Capparis cartilaginea (CC) at a dose of 1–10 mg/kg caused a dose‐dependent fall in blood pressure and heart rate in anaesthetized rats. These effects were not blocked by atropine (1 mg/kg) and pretreatment with CC did not alter the pressor response to norepinephrine, indicating that the cardiovascular effects of CC are independent of cholinergic or adrenergic receptor involvement. In spontaneously beating guinea‐pig atria, CC induced a concentration‐dependent (0.1–1 mg/mL) decrease in force and rate of atrial contractions. In rabbit thoracic aorta, CC caused inhibition of norepinephrine or K+‐induced contractions. In guinea‐pig ileum, CC (1 mg/mL) inhibited submaximal contractions induced by acetylcholine, histamine or 5‐HT. Spontaneous contractions of rat uterus were also abolished when CC was added to the tissue bath at similar concentrations. These results suggest that the direct relaxant action of CC on myocardium and blood vessels may be responsible for its hypotensive and bradycardiac effects observed in the in vivo studies. Moreover, CC exhibits general spasmolytic activity in different smooth muscle preparations.
Toxicological evaluation of Nerium oleander on isolated preparations
Authors: Mazumder P. K. , Rao P. V. Lakshmana , Kumar Deo , Dube S. N. , Gupta S. Das 
Published: October 2006

AbstractIn vitro toxicological evaluation of Nerium oleander was carried out using different isolated preparations. The methanolic leaf extract potentiated both spontaneous and electrically evoked contractions of vas deferens of rats and guinea‐pig ileum in a concentration dependent manner. The effect was not antagonized by the adrenergic blocker, tolazoline. The extract inhibited electrically stimulated neurogenic twitch responses of rat phrenic nerve diaphragm preparation. The dose dependent inhibition of twitch response in this preparation could not be reversed by the anticholinesterase drug, neostigmine. The extract evoked a persistent depolarizing effect on the phrenic nerve diaphragm preparation. The extract exhibited its most potent action on the isolated right atrial preparation of rat. It inhibited the rate of spontaneously beating atria in a concentration dependent manner. The negative chronotropic effect was not antagonized either by antimuscarinic drug or adrenergic agonist.
Toxicity testing of organic solvent extracts from Annona squamosa: Effects on rabbit eyes and ear skin
Authors: Sookvanichsilp Nongluck , Gritsanapan Wandee , Somanabandhu Aim‐On , Lekcharoen Khanong , Tiankrop Pongkrit 
Published: October 2006

AbstractSome organic solvent extracts of seeds and leaves from Annona squamosa exhibit insecticidal activity. They were studied for the management of human lice. However, toxicological data of these extracts have not yet been widely reported. In this experiment, the extracts of active compounds of leaves and seeds from A. squamosa in four organic solvents, i.e. petroleum ether, ether, chloroform and ethanol were tested for toxicity to the eyes and ear skin of rabbits, using 1:10 (w/v) dilutions of dried extracts in propylene glycol as test substances. The results revealed that some extracts caused conjunctival redness, chemosis, rugged cornea, skin erythema and oedema. The organic solvent extracts that produced adverse effects on rabbit eyes were in the following order of severity: ether > petroleum ether > chloroform > ethanol, and those on rabbit ear skin were petroleum ether > ether > chloroform > ethanol. Ethanol extracts of leaves and seeds seemed to produce mildest toxicity to rabbit eyes and no toxicity to rabbit ear skin.
Analgesic antiinflammatory action of Pfaffia paniculata (Martius) kuntze
Authors: Mazzanti G. , Braghiroli L. 
Published: October 2006

AbstractThe alcoholic extract of Pfaffia paniculata dried roots was studied for analgesic antiinflammatory activity in the rat paw oedema test, writhing test, hot plate test and increased vascular permeability. Pfaffia paniculata inhibited the carrageenin‐induced rat paw oedema and increased vascular permeability and showed analgesic activity on inflammatory pain but not on noninflammatory pain. Moreover the extract was devoid of local irritant action.
Aloe vera: Antiulcer and antidiabetic effects
Authors: Koo M. W. L. 
Published: October 2006

AbstractA health product containing aloe vera gel was examined for its effects on gastric mucosal lesions induced by cold‐restraint or by oral administration of 70% v/v ethanol (2 mL/kg), and on plasma glucose levels in alloxan‐induced diabetic rats. Pretreatment with the preparation orally did not protect against lesion formation. There was no beneficial effect on the healing of ethanol‐induced gastric mucosal damage when the preparation was given twice daily for 3 days. The plasma glucose level of alloxan‐injected rats (120 mg/kg, s.c.) was about twice as high as that of their controls. It was further elevated by a single oral dose of the preparation. Chronic treatment with the preparation, given twice daily for 10 days, produced a sustained increase in the plasma glucose levels. The findings do not support the claimed efficacy of the preparation in treating gastric ulceration and diabetes mellitus.
Contraceptive efficacy of Carica papaya seed extract in male mice (Mus musculus)
Authors: Chinoy N. J. , D'Souza J. M. , Padman Priya 
Published: October 2006

AbstractThe effects of an aqueous extract of Carica papaya seeds (20 mg/kg body weight/animal/day orally and 5 mg/kg body weight/animal/day i.m. for 60 days) were investigated for contraceptive efficacy and other related side effects in male albino mice, Mus musculus. The data revealed that the extract might be causing an androgen deprived effect to target organs resulting in alterations in the internal milieu of the cauda epididymis especially. The treatment did not, however, affect the testicular sperm count suggesting that it acted at the post‐testicular level which lead to a reduction of cauda epididymal sperm motility and thus the treatment brought about a significant reduction in fertility rate. The induced effects were transient and reversible upon withdrawal of the treatment, elucidating that functional sterility could be induced by the aqueous papaya seed extract in rodents.
Cardiovascular active substances from the straw mushroom, Volvariella volvacea
Authors: Chiu K. W. , Lam A. H. W. , Pang P. K. T. 
Published: October 2006

AbstractThe straw mushroom Volvariella volvacea is one of the common edible mushrooms in Hong Kong and is widely cultivated in Southeast Asian countries. It has been reported to produce a hypotensive response in animals including humans. An aqueous extract of the mushroom (SME) was prepared and given through intravenous injections to normotensive rats. The blood pressure changes produced by SME alone or in the presence of various drugs were studied. The effects of SME on the kidney function of water‐loaded rats and on isolated tissue preparations of the tail artery and right atrium were examined. An i.v. injection of SME produced a hypotensive effect in rats with an ED50 of 25 mg dry weight/kg body weight. This hypotensive effect of SME was attenuated or blunted in the presence of hexamethonium, phentolamine, pyrilamine and cimetidine suggesting the involvement of the α‐adrenergic component of the autonomic system and/or histamineergic stimulation. SME did not increase urinary excretion nor sodium diuresis. It produced positive chronotropic and inotropic effects on isolated right atria and induced contraction of isolated tail artery strips. This latter contractile response was inhibited by antagonists of serotonin and α‐adrenoceptor, ketanserin and phentolamine respectively. Partial purification using dialysis and liquid chromatography revealed that the hypotensive active substances had molecular masses between 8000 and 12000 dalton. These substances were heat stable and resistant to trypsin digestion. In view of the similarity in blood pressure and cardiovascular response, SME might contain serotonin‐like substances.
Evaluation of oestrogenicity and pregnancy interceptory efficacy of lapachol (2‐hydroxy‐3‐(3‐methyl‐2‐butenyl)‐1,4‐naphthoquinone) in the mouse
Authors: Sareen Vineeta , Jain Sunita , Narula Anita 
Published: October 2006

AbstractLapachol, a naphthoquinone isolated from Tectona grandis was evaluated for its oestrogenicity and antinidational activity in the mouse and was found to possess a statistically significant (p < 0.001) uterotrophic effect after administration of the drug at a dose of 20 mg/kg body weight/day/mouse, intramuscularly. However, in comparison with conjugated oestrogen, the drug proved to be a relatively weak oestrogenic. Lapachol when administered at the same dose level exhibited interceptory activity at all stages of early pregnancy.
Screening of various plant extracts used in ayurvedic medicine for inhibitory effects on human immunodeficiency virus type 1 (HIV‐1) protease
Authors: Kusumoto Ines Tomoco , Nakabayashi Takeshi , Kida Hiroaki , Miyashiro Hirotsugu , Hattori Masao , Namba Tsuneo , Shimotohno Kunitada 
Published: October 2006

AbstractTo identify substances with anti‐human immunodeficiency virus (HIV) activity in traditional medicines, water and methanol extracts of crude drugs used in Indian traditional medicine (Ayurveda) were subjected to screening for their inhibitory effects on HIV type 1 protease (PR). The enzyme activity was determined by HPLC and of the 39 crude drugs tested, the extracts of the seeds of Areca catechu, the bark of Eugenia jambolana, the bark of Saraca indica and the stem bark of Terminalia arjuna inhibited the HIV‐1 PR activity by more than 70% at a concentration of 0.2 mg/mL. The most potent inhibition was shown by the A. catechu extract, from which some procyanidins were isolated. One of them, arecatannin B1 showed significant HIV‐1‐PR inhibitory activity.
Shilajit induced morphometric and functional changes in mouse peritoneal macrophages
Authors: Ghosal Shibnath , Baumik Sraboni , Chattopadhyay Sukumar 
Published: October 2006

AbstractThe dose‐ and time‐dependent effects of processed shilajit (SJP) on morphometric and functional changes of mouse peritoneal macrophages were evaluated. Several dynamic aspects of cellular modulations were observed in response to SJP treatment (0.025–900 mcg per mouse, i.p.) for different periods of time (0 min to several hours). A plausible mechanism of drug‐receptor interactions, involving different types of transition states, is postulated. Dose and time dependent bond formation‐deformation in the complex transitions were reflected in the morphometric and functional manifestations of the adherent cells. These findings suggest the necessity of carefully determining the dose and period of administration of shilajit even when accepted as a panacea.
Isolation and partial characterization of biologically active polysaccharides from Plantago major L.
Authors: Samuelsen Anne Berit , Paulsen Berit Smestad , Wold Jens Kristian , Otsuka Hanako , Yamada Haruki , Espevik Terje 
Published: October 2006

AbstractPolysaccharide fractions were isolated from Plantago Major L. leaves by extraction with cold water, hot water and with dimethylsulphoxide (DMSO). Each of the three crude extracts obtained was further separated by ionexchange chromatography. Only the two acidic fractions from the 50°C crude extract were biologically active, demonstrated by in vitro testing of activation of the complement system and induction of tumour necrosis factor alpha (TNF‐α) production from human monocytes. One of the fractions, PM I50, contains polysaccharide material comprising arabinose, galactose and xylose with smaller proportions of galacturonic acid, glucose, mannose and rhamnose. This fraction was further fractionated by size exclusion chromatography to give three fractions PM Ia, PM Ib and PM Ic. PM Ia is probably an arabinogalactan and PM Ib is mainly a 1,4‐linked xylan. The other biologically active fraction, PM II50 is composed of 75% galacturonic acid, 3% rhamnose, 6% arabinose and 8% galactose. Structure analysis indicates that PM II50 is a pectin type polysaccharide.
Studies on the antiulcer activity of Moringa oleifera leaf extract on gastric ulcer models in rats
Authors: Pal Saroj K. , Mukherjee Pulok K. , Saha B. P. 
Published: October 2006

AbstractThe methanol fraction of M. oleifera leaf extract was found to possess significant protective actions in acetylsalicylic acid, serotonin and indomethacin induced gastric lesions in experimental rats. A significant enhancement of the healing process in acetic acid—induced chronic gastric lesions was also observed with the extract‐treated animals.
Medicinal plants of euphorbiaceae occurring and utilized in thailand. V. Skin irritants of the daphnane and tigliane type in latex of Excoecaria bicolor and the uterotonic activity of the leaves of the tree
Authors: Karalai C. , Wiriyachitra P. , Sorg B. , Hecker E. 
Published: October 2006

AbstractFrom latex of Excoecaria bicolor (Euphorbiaceae) four TLC‐homogeneous fractions highly enriched in diterpene esters were obtained (F1–F4). Fraction F3 by NMR was found to be a mixture of 9,13,14‐orthoester‐20‐esters (1a) of 5β‐hydroxyresiniferonol‐6α,7α‐epoxide (1). Alkaline transesterification yielded from 1a a mixture of 5β‐hydroxyresiniferonol‐6α,7β‐epoxide‐9,13‐14‐orthoesters (1f) carrying unsaturated orthoester groups as a TLC‐homogeneous material (final isolation of Excoecaria factors B1/B2, B3 and B4). The transesterification mixture also contained, according to GC‐MS, methyl n‐carboxylates corresponding to the even numbered C22−C30 acids from 20‐positions in 1a. Fraction F4 by NMR contained molecular species (2a) structurally closely related to 1a, carrying 5β,12β‐dihydroxyresiniferonol‐6α, 7α‐epoxide (2) as the parent alcohol. From 2a, by alkaline transesterification, a two‐component mixture of Excoecaria factors B5/B6, i.e. 5β,12β‐dihydroxy‐resiniferonol‐6α,7α‐epoxide‐9,13,14‐ortho(2,4,6‐hexadecatrienoate)/‐(2,4,6,8‐hexadecatetraenoate) (2b/2c) was obtained. GC‐MS of the transesterification mixture revealed methyl n‐carboxylates corresponding to even numbered C16‐C16 acids from 20‐positions in 2a (omitting C18 and C20). Fractions F1 and F2 by alkaline transesterifications yielded 12‐deoxyphorbol (3) and its 13‐(3,5‐tetradecadienoate) 3b (Excoecaria factor B7). Moreover 4,12‐dideoxy(4α)phorbol (4), its 13‐(3,5‐tetradecadienoate) 4b and the natural 4‐epimer of 4b 4,12‐dideoxyphorbol‐13‐(3,5‐tetradecadienoate) (5a) (new Excoecaria factor B8) were obtained. GC‐MS of the transesterification mixtures revealed mainly methyl n‐carboxylates corresponding to even numbered C16‐C30 acids. Thus the latex and the fractions F1 and F2 contain 13,20‐diesters of the parent alcohols 12‐deoxyphorbol (3) and 4,12‐dideoxyphorbol (5). 4,12‐dideoxy(4α)phorbol (4) and its derivatives may be considered artifacts from alkaline epimerization of 5. The daphnane type Excoecaria factors B1‐B6 are structurally very closely related to diterpenes such as yuanhuacine occurring in certain Daphne and Wikstroemia species. Daphnane type esters of this kind are currently used routinely in China for fertility regulation. Similarly, daphnane and tigliane type Excoecaria factors present in the latex of E. bicolor may be responsible for the uterotonic activity of its leaves utilized in Thai herbal medicine.
Preventive and curative effects of Berberis aristata Fruit extract on paracetamol‐ and CCl4‐induced hepatotoxicity
Authors: Gilani Anwar‐Ul Hassan , Janbaz Khalid Hussain 
Published: October 2006

AbstractThe effect of an aqueous‐methanol extract of Berberis aristata fruits (Berberidaceae) was investigated against paracetamol‐ and CCl4‐induced hepatic damage. Paracetamol produced 100% mortality at a dose of 1 g/kg in mice while pre‐treatment of animals with crude extract (500 mg/kg) reduced the death rate to 10%. Pre‐treatment of rats with fruit extract (500 mg/kg, orally twice daily for 2 days) prevented (p<0.05) the paracetamol (640 mg/kg) as well as CCl4 (1.5 mL/kg)‐induced rise in serum transaminases (GOT and GPT). Post‐treatment with three successive doses of extract (500 mg/kg, 6h) restricted the hepatic damage induced by acetaminophen (p<0.01) but CCl4‐induced hepatotoxicity was not altered (p>0.05). Plant extract (500 mg/kg) caused significant prolongation (p<0.01) in pentobarbital (75 mg/kg)‐induced sleep as well as increased strychnine‐induced lethality in mice suggestive of inhibitory effect on microsomal drug metabolizing enzymes (MDME). These results indicate that the crude extract of Berberis aristata fruits exhibits hepatoprotective action partly through MDME inhibitory action.
Tanzanian medicinal plants used traditionally for the treatment of malaria: In vivo antimalarial and in vitro cytotoxic activities
Authors: Gessler M. C. , Tanner M. , Chollet J. , Nkunya M. H. H. , Heinrich M. 
Published: October 2006

AbstractSeventeen fractions of extracts obtained from 11 Tanzanian medicinal plants, which had previously been shown to possess a high antimalarial activity in vitro were submitted to the 4‐day suppressive test in Plasmodium berghei‐infected mice, and were investigated for cytotoxic activity in human carcinoma cell lines in vitro. Several fractions administered orally to the mice (500 mg/kg body weight/day) produced a significant reduction of parasitaemia. The most effective plant fractions investigated were those of the root and stem bark of Maytenus senegalensis (90% and 63% suppression of parasitaemia, respectively) and of the roots of Cissampelos mucronata (59% suppression). Highest cytotoxic activities were found with all fractions of Maytenus senegalensis (IC50 1 μg/mL) and with the PE fraction of the roots of Salacia madagascariensis (median IC50=1.2 μg/mL for HT 29 and 2.3 μg/mL for KB).
Computer‐Assisted Structure‐Activity Relationship Analysis: Pattern Recognition Studies on Hypolipidemic Arylpropionic Acid Derivatives
Authors: Gombar Vijay K. , Jaeger Edward P. , Jurs Peter C. 
Published: October 2006

AbstractPattern recognition techniques are applied to analyze the structure‐activity relationships (SAR) among α‐substituted‐β‐arylpropionic acid derivatives possessing hypolipidemic properties. The triglyceride lowering activity of 116 such compounds is investigated. Twelve structural descriptors are identified which can discriminate derivatives more active than clofibrate from those which have activity to or less than that of clofibrate with a success rate greater than 97%. Among the 12 descriptors selected out of a total of about 70, three are electronic and two are geometric. In addition, certain chemical substructures and their environments have been found to be important in determining the activity class.
Quantitative Structure‐Activity Relationship (QSAR) Analysis Using the Partial Least Squares (PLS) Method: The Binding of Polycyclic Aromatic Hydrocarbons (PAH) to the Rat Liver 2,3,7,8‐Tetrachlorodibenzo‐P‐Dioxin (TCDD) Receptor
Authors: Johnels Dan , Gillner Mikael , Nordén Bo , Toftgård Rune , Gustafsson Jan‐åke 
Published: October 2006

AbstractIt is demonstrated that it is possible to obtain quantitative structure‐activity relationships from different molecular descriptors for the binding affinity of ten polycyclic aromatic hydrocarbons (PAH) for the rat liver 2,3,7,8‐tetrachlorodibenzo‐p‐dioxin (TCDD) receptor, by the use of the partial least squares method. The variables used as descriptors range from theoretical and measured electronic properties to simple descriptors of the molecular geometry. A two component model, explaining 85% of the variance of the binding affinity of the ten PAH for the TCDD receptor is obtained when all descriptor variables are included in the analysis. When only molecular geometry descriptors are utilized in the modelling, a one component model explaining 75% of the variance is obtained.
Rationalisations among Heterocyclic Partition Coefficients. Part 3: π‐Excessive Heterocycles. Some Comments on the CLOGP Algorithm
Authors: Bradshaw John , Taylor Peter J. 
Published: October 2006

AbstractThe partition coefficients for 123 furans, thiophenes, pyrroles and their benzofused derivatives are listed and the results discussed in terms of Δπ, i.e. the difference in π‐value from that expected for benzene. The smaller internal bond angle of 5‐membered rings leads to characteristically larger π‐values for some bulky groups, notably tertiary amide, since these can approach planarity more closely than in benzene. By contrast, lone pair repulsion lowers π for some 2‐substituted furans. Otherwise, π is very slight in furans and thiophenes, demonstrating the absence of appreciable electronic interactions. Because pyrroles and indoles are proton donors, they superficially show electronic effects similar to anilines. Closer analysis, based partly on the existence of anomalous negative Δπ values, demonstrates complications which the CLOGP algorithm does not consider. The rationale of electronic interaction and its effect on log P is discussed in terms of the need to consider (a) separate proton donor and acceptor terms, (b) rises as well as falls in lone pair electron density. It is pointed out, inter alia, that π‐donor ring hetero‐atoms are not proton acceptors, and that aromatic ring hetero‐atoms in general do not behave like ring substituents. While no attempt is made to construct an alternative algorithm, various suggestions are made concerning the lines along which CLOGP might be modified.
Wiener Indices and Partition Coefficients of Unsaturated Hydrocarbons
Authors: Lukovits I. 
Published: October 2006

AbstractThe Wiener index W was defined originally for saturated hydrocarbons. In this work the definition of W was extended for unsaturated hydrocarbons: W = Ws + Wd + Wt + Wa, where s, d, t, and a refer to the contributions of single, double, triple and aromatic bonds, respectively. Good correlation (r = 0.95) could be demonstrated between the logarithms of n‐octanol‐water partition coefficients of the molecules and the components Ws, Wd, Wt and Wa.
Model‐based LFER Parameters and QSAR of Ligand‐β‐Adrenoceptor Interactions I. Equlibrium Models and Parameters of β‐Adrenergic Effectuation
Authors: Dove Stefan , Franke Rainer 
Published: October 2006

AbstractA separate consideration of ligand‐β‐adrenoceptor interactions responsible for affinity (recognition, binding) and agonistic activity, respectively, is very important for the explanation of molecular events eliciting the activating conformational change of the receptor. Equilibrium models of β‐adrenergic effectuation including receptor activation by agonists and partial agonists, receptor‐effector (G‐protein) coupling, and adenylate cyclase stimulation allow to obtain LFER‐related parameters of both interaction components from apparent dissociation constants and intrinsic activities. Two models, both containing “precoupling” of non‐activated receptor and effector molecules, are derived: a ternary complex model for the interaction of ligands, receptor, and effector in the absence, and an adenylate cyclase activation model for enzyme activation in the presence of GTP. Agonistic activity is represented by the equilibrium constant K* reflecting the concentration ratio of activated and non‐activated agonist‐receptor complexes. KD, the dissociation constant of non‐activated complexes, represents ligand‐receptor recognition and binding. K* can be estimated either from using ratios KL/KH of apparent low‐ and high affinity dissociation constants in GTP absence, or from using intrinsic activities of adenylate cyclase activation. According to our models, KL, which also describes apparent dissociation in binding assays with GTP, is related to KD and K* with KL = KD/(1 + K*). In terms of the free energy of ligand binding and receptor activation. ΔG° = RT ln KL, this corresponds to a decomposition of pKL into pKL = pKD + log (1 + K*). In QSAR, thus, log (1 + K*) is the parameter of choice for LFER‐related description of ligand‐receptor interactions eliciting agonistic activity.