Management of Psoriatic Erythroderma with Ayurvedic herbomineral preparations: A case report.

Psoriatic Erythroderma (PsE) is a presentation of Erythroderma due to a history of psoriasis showing inflammation and exfoliation of epidermal skin characterized by erythema and scaling. There is no definite treatment in contemporary medical science but the principle-based Ayurvedic approach has been proved to be effective. We present a case of PsE treated for 3 months with Ayurvedic herbomineral preparations and dietary restrictions for non-vegetarian and dairy items. As per the Ayurvedic diagnostic view, the presented case is correlated with Audumbara Kushtha and Ekakushtha due to their intricate features. Thus, Ayurvedic approaches were directed to eliminate vitiated doshas responsible for acute exacerbation of Kushtha (∼dermatitis) and to maintain equilibrium among them. The patient was initially considered as a case of Saam stage of Kushtha with Pitta-Rakta-Vata predominance. Thus, management was planned into different domains-treatment of Saam stage of Kushtha, Vyadhipratyanika chikitsa (∼disease antagonistic treatment), Rasayana intervention (∼Immunomodulation therapy) and Ayurvedic drugs were given accordingly. The assessment was done based on subjective parameters and PASI score. The patient was followed for about one and half year without any complication and relapse. This case study shows PsE can be managed with an Ayurvedic approach and proper diet planning.

Alcohol alters hypothalamic glial-neuronal communications involved in the neuroendocrine control of puberty: In vivo and in vitro assessments.

The onset of puberty is the result of the increased secretion of hypothalamic luteinizing hormone-releasing hormone (LHRH). The pubertal process can be altered by substances that can affect the prepubertal secretion of this peptide. Alcohol is one such substance known to diminish LHRH secretion and delay the initiation of puberty. The increased secretion of LHRH that normally occurs at the time of puberty is due to a decrease of inhibitory tone that prevails prior to the onset of puberty, as well as an enhanced development of excitatory inputs to the LHRH secretory system. Additionally, it has become increasingly clear that glial-neuronal communications are important for pubertal development because they play an integral role in facilitating the pubertal rise in LHRH secretion. Thus, in recent years attempts have been made to identify specific glial-derived components that contribute to the development of coordinated communication networks between glia and LHRH cell bodies, as well as their nerve terminals. Transforming growth factor-α and transforming growth factor-ß1 are two such glial substances that have received attention in this regard. This review summarizes the use of multiple neuroendocrine research techniques employed to assess these glial-neuronal communication pathways involved in regulating prepubertal LHRH secretion and the effects that alcohol can have on their respective functions.

Insulin-like growth factor-1 stimulation of hypothalamic KiSS-1 gene expression is mediated by Akt: effect of alcohol.

Kisspeptin, as well as insulin-like growth factor-1 (IGF-1), act centrally to stimulate luteinizing hormone-releasing hormone (LHRH) secretion at puberty. IGF-1 can induce KiSS-1 gene expression as an early pubertal event; however, the signaling pathway mediating this effect is not known. Since alcohol (ALC) blocks IGF-1 induced LHRH release acutely, we assessed whether this drug could affect IGF-1 stimulated prepubertal KiSS-1 gene expression following a binge type of exposure. Immature female rats were administered either ALC (3 g/kg) or water via gastric gavage at 07.30 h. At 09.00 h the ALC and control groups were subdivided where half received either saline or IGF-1 (200 ng) into the third ventricle. A second dose of ALC (1.5, 2 and 3 g/kg) or water was administered at 11.30 h. These regimens produced moderate blood alcohol concentrations of 77, 89 and 117 mg/dl, respectively, over the time course of the experiment. Rats were sacrificed 6 h after the IGF-1 injection and tissues containing the anteroventral periventricular (AVPV) and arcuate (ARC) nuclei were collected. IGF-1 stimulated (P<0.01) KiSS-1 gene expression in the AVPV nucleus at 6 h, but did not affect expression of the kisspeptin receptor, GPR54. While ALC did not alter basal expression of either gene, its dose dependently blocked IGF-1-induced KiSS-1 gene expression in the AVPV nucleus. No changes were observed in the ARC nucleus. Assessment of IGF-1 signaling indicated that the acute administration of IGF-1, ALC, or both did not alter the basal expression of IGF-1 receptor protein. However, IGF-1 stimulated (P<0.05) phosphorylated Akt protein over basal levels, an action blocked by ALC. Our results indicate that the IGF-1 induction of KiSS-1 gene expression is mediated by Akt activation, and that ALC alters this important prepubertal action of IGF-1.

Synthesis and anticonvulsant activity of some potential thiazolidinonyl 2-oxo/thiobarbituric acids.

A series of 5-[(N-substituted benzylidenylimino)amino]-2-oxo/thiobarbituric acids (3a-3h) have been synthesized by the condensation of 5-hydrazino-2-oxo/thiobarbituric acids (2a-2b) with various aromatic aldehydes. Cycloaddition of thioglycolic acid to 3a-3h, yielded 5-[(2'-substituted phenyl-4'-oxothiazolidin-3'-yl)amino]-2-oxo/thiobarbituric acids (4a-4h). All these compounds were screened, in vivo, for their anticonvulsant activity and acute toxicity studies. Compounds 4f and 4g were found to be most potent compounds of this series and were compared with the reference drugs, phenytoin sodium, lamotrigine and sodium valproate. The structures of these compounds have been established by IR, 1H NMR and mass spectroscopic data.

Hepatoprotective activity of Beta vulgaris against CCl4-induced hepatic injury in rats.

Ethanolic extract of Beta vulgaris roots given orally at doses of 1000, 2000 and 4000 mg/kg exhibited significant dose-dependent hepatoprotective activity against carbontetrachloride (CCl(4))-induced hepatotoxicity in rats. Hepatotoxicity and its prevention were assessed by serum markers viz. cholesterol, triglyceride, alanine amino transferase and alkaline phosphatase.

Synthesis and antiinflammatory activity of heterocyclic indole derivatives.

Chalcones of indole 1-5 and their corresponding products; pyrazolines 6-10 and azo compounds 11-15 were synthesised and evaluated for their antiinflammatory activity against carrageenan induced oedema in albino rats at a dose of 50 mg x kg(-1) oral. The structure of compounds was confirmed by IR, (1)H-NMR and mass spectral data. All the compounds of this series showed promising antiinflammatory activity. The most active compound of this series is 3-[1-acetyl-5-(p-hydroxyphenyl)-2-pyrazolin-3-yl]indole (7) was found to be most potent, which has shown higher percent of inhibition of oedema, lower ulcerogenic liability and acute toxicity than the standard drug phenylbutazone.

Synthesis of some newer derivatives of substituted quinazolinonyl-2-oxo/thiobarbituric acid as potent anticonvulsant agents.

5-[1'-[3"-Aminoacetyl-2"-methyl-6",8"-dihalosubstitutedquinazolin-4"(3"H)-onyl]-thiosemicarbazido]-2-oxo/thiobarbituric acids 3a-3h and 5-[2'-amino-5'-[3"-aminomethylene-2"-methyl-6",8"-dihalosubstitutedquinazolin-4"(3"H)-onyl]-1',3',4'-thiadiazol-2'-yl]-2-oxo/thiobarbituric acid 5a-5h were prepared by incorporating 1-[3'-aminoacetyl-2'-methyl-6",8"-dihalosubstituted-quinazolin-4'(3'H)-onyl]-thiosemicarbazides 2a-2d and 2-amino-5-[3'-aminomethylene-2'-methyl-6',8'-dihalosubstituted-quinazolin-4'(3'H)-onyl]-1,3,4-thiadiazoles 4a-4 h respectively at 5(th) position of 2-oxo/thiobarbituric acids (via Mannich reaction). All the newly synthesized compounds were screened for their anti-convulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valproate. Interestingly, these compounds were found to be devoid of sedative and hypnotic activities when tested. Out of the compounds studied, the most active compound 5h, that is 5-[2'-amino-5'-[3"-aminomethylene-2"-methyl-6",8"-dibromoquinazolin-4"(3"H)-onyl]-1',3',4'-thiadiazol-2'-yl]-2-thiobarbituric acid showed activity (90%) more potent than the standard drug.

Evaluation of analgesic, antipyretic and anti-inflammatory activity of spirobarbitunylphenothiazines in rodents.

Analgesic, antipyretic and anti-inflammatory activities of newly synthesized spirobarbitunylphenothiazines viz 10-[7, 11-Di(4-4' dimethoxphenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5.5] undecane 1, 5 dione] acetylphenothiazine (test drug A) and 10-[7, 11-Di (N.N-dimethylaminophenyl)-3-oxo-9-methylaminoimino-2, 4-diazaspiro [5, 5] undecane-1, 5 dione] acetylphenothiazine (test drug B) have been screened in Swiss mice and Wistar rats. The peripheral analgesic activity of test drugs A and B was investigated by acetic acid induced writhing test in Swiss mice while the central analgesic action was assessed by hot-wire (tail flick test) of the analgesiometer and tail-clip test in Wistar rats. Antipyretic activity was assessed on Brewer's yeast induced pyrexic model while antiinflammatory activity was seen on carrageenan induced hind paw oedema. Analgesic activity was found to be only of peripheral type as there was reduction of 66% in writhing responses by test drugs A and B in dose of 80 mg/kg in mice. No change in the tail flick responses was observed on analgesiometer or by tail clip by both the test drugs. Reduction of 1.5 to 2.0 degrees C in rectal temperature was observed in pyretic rats by test drugs A and B in dose of 80 mg/kg. 80% reduction in paw volume was noted in 80 mg/kg dose of both the test drugs which was comparable to the anti-inflammatory activity of 300 mg/kg, p.o. of phenylbutazone.

Synthesis of newer thiadiazolyl and thiazolidinonyl quinazolin-4 3H-ones as potential anticonvulsant agents.

A series of 3-[[5-(alkylbenzylideneamino)-1,3,4-thiadiazol-2-yl]methylamino-2]-methyl-6-monosubstitutedquinazolin-4(3H)-one (4a-4l) have been synthesized via condensation of 3-[(5-amino-1,3,4-thiadiazol-2-yl)methylamino]-2-methyl-6-monosubstitutedquinazolin-4(3H)-one (3a-3b) with various aromatic aldehydes. Cycloaddition of thioglycolic acid with 4a-4l yielded 3-([4-[2-(alkylphenyl)-4-oxo-1,3-thiazolidin-3-yl]-1,3,4-thiadiazol-2-yl]methylamino)-2-methyl-6-monosubstitutedquinazolin-4(3H)-one (5a-5l). The compounds were screened for their anticonvulsant activity and were compared with the standard drugs, phenytoin sodium, lamotrigine and sodium valproate. Out of the 30 compounds the most active compound was 3-([4-[2-(m-methoxy-p-hydroxyphenyl)-4-oxo-1,3-thiazolidin-3-yl]-1,3,4-thiadiazol-2-yl]methylamino)-2-methyl-6-bromo-quinazolin-4(3H)-one (5l).

Larvicidal activity of latex and stem bark of Euphorbia tirucalli plant on the mosquito Culex quinquefasciatus.

The methanolic, chloroform and ether extracts of Euphorbia tirucalli latex and stem bark were evaluated for larvicidal activity against laboratory-reared larvae of Culex quinquefasciatus (Diptera: Culicidae), vector of the brancroftian filariasis and worst urban nuisance mosquito. The latex extracts contain more potent larvicidal components (177.14 mg/L-326.37 mg/L) than the stem bark extracts (237.663 mg/L-513.39 mg/L). The order of toxicity (LC50) for the latex extracts was Methanol extract (177.14 mg/L) > Chloroform (200.76 mg/L) > Ether (326.37 mg/L) while the rank of order of toxicity (LC50) of stem bark extracts was Ether (237.66 mg/L) > Chloroform (343.515 mg/L) > Methanol (513.387 mg/L), Higher doses (LC90 24 h of mosquito larvae) of each extract did not cause any mortality among fishes after 24 h. The study gave a weight into the possibility of formulating suitable preparation from the latex and stem bark extracts of the plant for use in mosquito control programme.

A multicentric study with arteether in patients of uncomplicated falciparum malaria.

Two hundred and sixty seven patients of uncomplicated P. falciparum malaria completed study in a multicentric phase III clinical trial of Arteether. Arteether was given intramuscularly in a dose of 150 mg daily for three consecutive days. Each patient was followed upto 28 days of alpha, beta arteether therapy. The cure rate was 97% with fever clearance time between 1-7 days (24-168 hours) and parasite clearance time between 1-3 days (24-72 hours). Parasite reappearance rate was found to be 3% and reported at only three of the centres. Following the treatment no adverse effect was observed on haematological, biochemical and vital clinical parameters.

Effect of arteether alpha/beta on uncomplicated falciparum malaria cases in Upper Assam.

Thirty patients of uncomplicated Plasmodium falciparum malaria completed a clinical trial of arteether alpha/beta conducted in a malaria endemic tea garden of district Dibrugarh, Assam. Arteether was given intramuscularly in once a day dose of 150 mg for three consecutive days. The cure rate was 100 per cent with mean fever and parasite clearance time of 42.4 +/- 17.5 and 37.6 +/- 13.6 h respectively. Recrudescence/reinfection rate was 6.7 per cent. Palpable spleens of twenty out of twenty one cases on day 0 became non palpable within 28 days. Following the treatment, percentage of hemoglobin improved marginally with no remarkable change in total and differential leucocyte count. Arteether alpha/beta, besides being a potent and fast acting schizontocidal drug, also exhibited gametocytocidal action on P. falciparum.

In vivo effect of cyanate on serum and eye lens in rat.

Supplementation of cyanate in rats caused a significant decrease in serum GSH and increase in calcium and phosphate level both in serum and lens. Consequently, these changes led to induce acidosis uremia in serum and hypercalcemia and hyperphosphatemia in lens which may be possible causing factor for cataract.

Beneficial effects of Allium sativum, Allium cepa and Commiphora mukul on experimental hyperlipidemia and atherosclerosis--a comparative evaluation.

Oral administration of petroleum ether extract of Allium sativum, Allium cepa and ethylacetate extract of Commiphora mukul in albino rats significantly prevented rise in serum cholesterol and serum triglyceride level, caused by atherogenic diet. All the three agents were also found to confer significant protection against atherogenic diet induced atherosclerosis.

In vitro propagation of Coleus forskohlii Briq., a threatened medicinal plant.

In vitro clonai multip1ication of Coleus forskahlii Briq a threatened plant, has been achieved on MS medium supplemented with Kn (2.0 mg/l) and IAA (1.0 mg/l) using nodal segments as explants, Shoots multiplied at a rate of 12 - fold every six weeks. Rooting was achieved upon transfer of shoots onto MS medium containing IAA (1.0 mg/l). The micropropagated plants were successfully established under field conditions. Forskolin content in tubers of plants obtained by micropropagation was found to be 0.1%, the same as that found in wild plants. This micropropagation procedure should be useful for conservation as well as production of this important plant.

Analgesic, antipyretic and ulcerogenic activity of Nyctanthes arbor tristis leaf extract.

The leaves of Nyctanthes arbor tristis, besides being used in the treatment of sciatica and arthritis, are advocated for various kinds of fevers and painful conditions by the Ayurvedic physicians. In the present study, the water-soluble portion of an ethanol extract of the leaves was screened for analgesic, antipyretic and ulcerogenic activities. The extract exhibited significant aspirin-like antinociceptive activity but failed to produce morphine-like analgesia. It was also found to possess antipyretic activity against brewer's yeast-induced pyrexia in rats. The extract also produced gastric ulcers following oral administration for six consecutive days in rats. Results of the present study tend to substantiate the use of this plant in fevers and painful conditions by Ayurvedic physicians.