Kupeelu (Strychnos nux-vomica Linn.) commonly known as nux vomica is a poisonous plant used extensively in various ayurvedic formulations, with great therapeutic significance. Ayurveda recommended the administration of Kupeelu only after purification in different media like cow's urine (Go mutra), cow's milk (Go dugdha), cow's ghee (Go ghrita), Kanji (sour gruel), and so on. Apart from the classical methods some other methods are also adopted by the traditional practitioners using castor oil (Eranda taila), ginger juice (Ardraka swarasa), in the purification of Kupeelu seeds. In the present study an attempt has been made to purify the seeds by performing two different methods (one classical and another traditional) using Kanji and Ardraka
swarasa as Shodhana media. This study reveals that both the methods studied reduce the strychnine and brucine contents in comparison to the raw seeds as determined by high performance thin layer chromatography (HPTLC). After purification in Kanji and Ardraka swarasa, the strychnine content was reduced by 39.25% and 67.82%, respectively, and the brucine content in the purified seeds was also found to have decreased by 17.60% and 40.06%, in comparison to the raw seeds.
Ardraka swarasa; brucine; kanji; kupeelu; shodhana; strychnine
A simple, sensitive, and specific thin layer chromatography (TLC) densitometry method has been developed for the simultaneous quantification of strychnine and brucine in the seeds of Strychnos nux-vomica.
Materials and Methods:
The method involved simultaneous estimation of strychnine and brucine after resolving it by high performance TLC (HPTLC) on silica gel plate with chloroform–methanol–formic acid (8.5:1.5:0.4 v/v/v) as the mobile phase.
The method was validated as per the ICH guidelines for precision (interday, intraday, intersystem), robustness, accuracy, limit of detection, and limit of quantitation. The relationship between the concentration of standard solutions and the peak response was linear within the concentration range of 50–1000 ng/spot for strychnine and 100–1000 ng/spot for brucine. The method precision was found to be 0.58–2.47 (% relative standard deviation [RSD]) and 0.36–2.22 (% RSD) for strychnine and brucine, respectively. Accuracy of the method was checked by recovery studies conducted at three different concentration levels and the average percentage recovery was found to be 100.75% for strychnine and 100.52% for brucine, respectively.
The HPTLC method for the simultaneous quantification of strychnine and brucine was found to be simple, precise, specific, sensitive, and accurate and can be used for routine analysis and quality control of raw material of S. nux-vomica and several unani and ayurvedic formulations containing this as an ingredient.
HPTLC; method development; strychnine; brucine; validation
Strychnos nux-vomica, commonly known as kuchla, contains strychnine and brucine as main constituents. Minor alkaloids present in the seeds are protostrychnine, vomicine, n-oxystrychnine, pseudostrychnine, isostrychnine, chlorogenic acid, and a glycoside. Seeds are used traditionally to treat diabetes, asthma, aphrodisiac and to improve appetite.
The present study was aimed to evaluate the various pharmacognostical characters and antidiabetic activity of S. nux-vomica seed.
Materials and Methods:
Pharmacognostical characters were performed as per the WHO guideline. Extraction was carried out in petroleum ether, chloroform, alcohol, hydroalcoholic, aqueous, and phytochemical constituents present in extracts were detected by different chemical tests. Among these extracts hydroalcoholic, aqueous extracts were evaluated for antidiabetic activity on the basis of extractive yield and phytoconstituents, in alloxan-induced diabetic rats using gliclazide as standard.
Various analytical values of S. nux-vomica extract were established. Phytoconstituents present in S. nux-vomica extracts were detected.
S. nux-vomica extracts show antihyperglycemic activity in experimental animals.
Antidiabetic activity; alloxan; extract; kuchla
Ayurvedic preparations claim on their label only the quantity of crude drugs and not the quantity of active ingredients present therein. So work was taken up to find the percentage of strychnine and brucine from Ayurvedic pills of Nux vomica powder by TLC spectrophotometric analysis, which study has not been reported earlier. However, the literature survey only revealed the following work.
Some plants used in Unani system of medicine are toxic, even deadly poisonous. The drugs having such plants as their components are detoxified before they are dispensed to the patients. One such drug, capsule Hudar, has Strychnos nux-vomica L. (Azraqi) seeds as one of its components and is very effectively used to elevate blood pressure. Ancient manuscripts describe many methods of its detoxification. It has been found that the detoxification processes studied reduce the strychnine content, as determined either by using uv-vis spectrophotometer or HPLC, present in Strychnos nux vomica seeds which is responsible for Strychnos nux vomica toxicity. The decrease in strychnine amount was best when the seeds were immersed for detoxification in excess of water for 5 days, in milk for 2 days followed by their boiling in milk. Strychnine in small amounts has been reported to give subjective feeling of stimulation
Strychnos nux vomica; detoxification; Unani medicine
Seeds of Kupeelu (Strychnos nux-vomica Linn.), a known poisonous drug, is used extensively in various Ayurvedic formulations with great therapeutic significance. Ayurveda recommends the administration of Kupeelu only after passing through specific purificatory procedures in different media like cow's urine (Go mutra), cow's milk (Go dugdha), cow's ghee (Go ghrita), Kanji (thin gruel) etc. Strychnos nux vomica seeds are extensively advocated for nervous debility, paralysis, and weakness of limbs, sexual weakness, dyspepsia, and dysentery and in rheumatism where it can be assumed that besides other properties, Kupeelu may have some sort of anti-inflammatory activity too. In the present study, the powder of raw and processed Kupeelu seeds (processed / purified with Kanji i.e sour gruel) as test drugs were assessed for anti-inflammatory activity by employing Carrageenan and Formaldehyde induced hind paw oedema in Wistar strain albino rats at a dose of 22.5 mg/kg body weight orally. This study reveals that both raw and purified Kupeelu showed presence of highly significant anti-inflammatory activity against formaldehyde induced hind paw oedema, but did not have similar activity against Carrageenan induced hind paw oedema.
Kupeelu; Kanji; anti-inflammatory; purification; Shodhana; purificatory procedure
Strychnos nux vomica Linn.(Loganaceae) commonly known as Nux vomica (Kupeelu), is a poisonous plant and its seeds are used widely in Ayurvedic system of medicine since time immemorial. Ayurveda advocates that nux vomica seeds are to be administered in therapeutics only after going through certain purificatory measures (Shodhana). There are more than six media: cow's urine (Go mutra), cow's milk (Go dugdha), cow's ghee (Go ghrita), Kanji (thin gruel), castor oil (Eranda taila) and fresh ginger juice (Ardraka swarasa) etc., which have been reported in different classical texts of Ayurveda for proper processing of nux vomica seeds. In this study, an attempt has been made to purify the seeds by using three different methods as described in ancient treatise by using cow's urine and cow's milk as media alone and together. This study revealed that all the methods studied reduced the toxicity of strychnine and brucine contents in comparison to the raw seeds as determined by HPTLC. Out of these three methods maximum reduction in strychnine and brucine contents was found when the seeds were purified by keeping them in cow's urine for seven days followed by boiling in cow's milk for three hrs.
Kupeelu; Strychnos nuxvomica; Shodhana; strychnine; Ayurveda; brucine; Cow's milk; Cow's urine
Brucine was encapsulated into stealth liposomes using the ammonium sulfate gradient method to improve therapeutic index.
Materials and methods:
Four brucine stealth liposomal formulations were prepared, which were made from different phosphatidylcholines (PCs) with different phase transition temperatures (Tm). The PCs used were soy phosphatidylcholine (SPC), dipalmitoyl phosphatidylcholine (DPPC), hydrogenated soy phosphatidylcholine (HSPC), and distearoyl phosphatidylcholine (DSPC). The stabilities, pharmacokinetics, and toxicities of these liposomal formulations were evaluated and compared.
Size, zeta potential, and entrapment efficiency of brucine-loaded stealth liposomes (BSL) were not influenced by PC composition. In vitro release studies revealed that drug release rate increased with decreased Tm of PCs, especially with the presence of rat plasma. After intravenous administration, the area under the curve (AUC) values of BSL-SPC, BSL-DPPC, BSL-HSPC, and BSL-DSPC in plasma were 7.71, 9.24, 53.83, and 56.83-fold as large as that of free brucine, respectively. The LD50 values of brucine solution, BSL-SPC, BSL-DPPC, BSL-HSPC, and BSL-DSPC following intravenous injection were 13.17, 37.30, 37.69, 51.18, and 52.86 mg/kg, respectively. It was found in calcein retention experiments that the order of calcein retention in rat plasma was SPC < DPPC << HSPC < DSPC stealth liposomes.
PC composition could exert significant influence on the stabilities, pharmacokinetics, and toxicities of brucine-loaded stealth liposomes. DSPC or HSPC with Tm above 50°C should be used to prepare the stealth liposomal formulation for the intravenous delivery of brucine. However, it was found in the present paper that the pharmacokinetics and toxicity of BSL were not influenced by the PC composition when the Tm of the PC was in the range of −20°C to 41°C.
brucine; stealth liposomes; phosphatidylcholine; pharmacokinetics; toxicity
Respiratory tract infections have gained worldwide recognition especially due to the increased incidence of HIV/AIDS. The bacteria responsible for these infections have also become increasingly resistant to chemotherapeutic agents in lower respiratory infections in Kibwezi in Kenya. Interviews were conducted using semi-structured questionnaires and detailed discussions with respondents. During the field surveys direct observations were made on how these plants are used. From the ethnobotanical survey the modes of preparation used included chewing and boiling. The plant parts used were mostly bark and root, which implies that the main methods of harvesting these plants are destructive in nature. Water and methanolic extracts of the three most popular plants, Acacia nilotica, Strychnos heninngsii and Microglossa densiflora were tested against three test organism: Staphylococcus aureus, Streptococcus pneumoniae and Escherichia coli for their antimicrobial properties. The efficacy of the extracts was tested by bioassay method using the disk diffusion test. It was interesting to note that none of the tested water extracts showed any activity against the test organisms. This is despite the fact that about 83% of the local people used water for extraction. Methanolic extracts of Acacia nilotica and Strychnos heninningsii showed efficacy against S. aureus, S. pneumoniae and E. coli. The findings of this research indicate that A. nilotica and S. heninngsii have antimicrobial properties and further work especially using mammalian models is recommended.
Medicinal plants; lower respiratory infections; antimicrobial growth inhibitory potential
Topical retinoids inhibit matrix metalloproteinases and accelerate collagen synthesis, thereby triggering antiaging effects in the skin. However, topical retinoids can cause severe skin reactions, including scaling, erythema, papules, and inflammation. The present study demonstrates that the ethanolic bark extract of Alstonia scholaris R. Br. can significantly inhibit all-trans retinoic acid-induced inflammation in human HaCat keratinocyte cells. Furthermore, two representative retinoid-induced proinflammatory cytokines, monocyte chemoattractant protein-1 and interleukin-8, were significantly suppressed by A. scholaris extract (by 82.1% and 26.3% at 100 ppm, and dose-dependently across the tested concentrations) in vitro. In a cumulative irritation patch test, A. scholaris extract decreased retinol-induced skin irritation, while strengthening the ability of retinoids to inhibit matrix metalloproteinase-1 expression, which is strongly associated with aging effects. These results suggest that A. scholaris is a promising compound that may increase the antiaging function of retinoids while reducing their ability to cause skin irritation.
Brucine (BRU) extracted from the seeds of Strychnos nux-vomica L is glycine receptor antagonist. We hypothesize that BRU may modify alcohol consumption by acting at glycine receptors, and evaluated the pharmacodynamic profiles and adverse effects of BRU in rat models of alcohol abuse.
Alcohol-preferring Fawn-Hooded (FH/Wjd) rats were administered BRU (10, 20 or 30 mg/kg, sc). The effects of BRU on alcohol consumption were examined in ethanol 2-bottle-choice drinking paradigm, ethanol/sucrose operant self-administration paradigm and 5-d ethanol deprivation test. In addition, open field test was used to assess the general locomotor activity of FH/Wjd rats, and conditioned place preference (CPP) was conducted to assess conditioned reinforcing effect.
In ethanol 2-bottle-choice drinking paradigm, treatment with BRU for 10 consecutive days dose-dependently decreased the ethanol intake associated with a compensatory increase of water intake, but unchanged the daily total fluid intake and body weight. In ethanol/sucrose operant self-administration paradigms, BRU (30 mg/kg) administered before each testing session significantly decreased the number of lever presses for ethanol and the ethanol intake, without affecting the number of sucrose (10%) responses, total sucrose intake, and the number of lever presses for water. Acute treatment with BRU (30 mg/kg) completely suppressed the deprivation-induced elevation of ethanol consumption. Treatment with BRU (10, 20, and 30 mg/kg) did not alter locomotion of FH/Wjd rats, nor did it produce place preference or aversion.
BRU selectively decreases ethanol consumption with minimal adverse effects. Therefore, BRU may represent a new pharmacotherapy for alcoholism.
alcoholism; ethanol; brucine; glycine receptor antagonist; Fawn-Hooded (FH/Wjd) rat
The need for an alternative drug for malaria initiated intensive efforts for developing new antimalarials from indigenous plants. The information from different tribal communities of northeast India along with research papers, including books, journals and documents of different universities and institutes of northeast India was collected for information on botanical therapies and plant species used for malaria. Sixty-eight plant species belonging to 33 families are used by the people of northeast India for the treatment of malaria. Six plant species, namely, Alstonia scholaris, Coptis teeta, Crotolaria occulta, Ocimum sanctum, Polygala persicariaefolia, Vitex peduncularis, have been reported by more than one worker from different parts of northeast India. The species reported to be used for the treatment of malaria were either found around the vicinity of their habitation or in the forest area of northeast India. The most frequently used plant parts were leaves (33%), roots (31%), and bark and whole plant (12%). The present study has compiled and enlisted the antimalarial plants of northeast India, which would help future workers to find out the suitable antimalarial plants by thorough study.
Alkaloids; malaria; medicinal plants; mosquito repellents; northeast India; traditional knowledge of medicine
The aim of this work was to formulate Alstonia boonei dried stem bark powder into tablets by wet granulation method using acacia, gelatine and sodium carboxymethyl cellulose as binders at concentrations of 1, 2, 4 and 8% w/w. The phytochemistry of the stem bark of Alstonia boonei was evaluated. The micromeritic properties of the granules prepared were studied. The tablets were evaluated using the necessary official and unofficial tests. The results of the phytochemical analysis showed that alkaloids, tannins, steroids, saponins, glycosides, flavonoids and terpenoids were present while anthroquinones and acidcompounds were absent. Micromeritic studies showed that Alstonia boonei granules had good flowability. The formulated tablets complied with British Pharmacopoeial specification for weight uniformity, hardness (≥5 kgf) and tablet friability (<1%). For disintegration test, tablets formulated with gelatine and acacia at concentrations of 1, 2 and 4% w/w complied with Pharmacopoeial specification. However, tablets formulated with SCMC (1-8% w/w) and 8% w/w of acacia and gelatine failed the disintegration tests (Disintegration time more than 15 min).
Alstonia boonei tablets; antimalarial; micromeritic; phyllotaxy; phytochemical analysis
Purpose: To evaluate phytochemical composition, antibacterial and antioxidant properties of methanolic extracts of different parts viz., leaves, follicles and latex of Indian devil tree (Alstonia scholaris Linn.) R. Br. Methods: Antibacterial activities of the methanol extracts against Gram +ve (Bacillus subtilis and Staphylococcus aureus) and Gram -ve (Escherichia coli, Pseudomonas aeruginosa) bacteria were determined by well diffusion techniques. Aantioxidant profiles of methanol extracts were determined by 1,1-diphenyl-2-picryl-hydrazil (DPPH) free radical scavenging, superoxide anion radial scavenging and ferric thiocyanate reducing assays. Results: Phytochemical composition revealed abundance of flavonoids (97.3 mg QE/g DW), proanthocynidins (99.3 mg CE/g DW) and phenolics (49.7 mgGAE/g DW) in the leaf extract. Extracts of follicles and latex had comparatively very content of phenolics, flavonoids and proanthocyanidins. However, in follicle extract level of proanthocyanidins was significantly higher (46.8 mg CE/gDW). Latex extract among others exhibited most potent antibacterial activity. All the extracts displayed strong DPPH free radical and superoxide anion scavenging activities, only leaf extract displayed powerful reducing and ferrous ion chelating activities. Conclusion: Study revealed significant antioxidant activities of A. scholaris leaf, follicles and latex extracts and potential antibacterial activity of latex extract.
Alstonia scholaris; Antibacterial; Antioxidant; Follicles; Latex; Phenolics
The arboreal ant, Crematogaster ashmeadi Emery (Hymenoptera: Formicidae), is the most dominant arboreal ant in the pine forests of the coastal plain of northern Florida. The majority of pine trees harbor a colony of these ants. The colonies inhabit multiple chambers abandoned by bark-mining caterpillars, especially those of the family Cossidae, in the outer bark of living pines. They also inhabit ground level termite galleries in the bark, often locating the queen in galleries. The density of chambers and ants is highest in the base of the tree and drops sharply with height on the trunk. Because chambers are formed in the inner layer of bark, they gradually move outward as more bark layers are laid down, eventually sloughing off the tree's outer surface. Chambers have a mean lifetime of about 25 yr. The abundant chambers in pine bark are excavated by a small population of caterpillars and accumulate over decades. Ant colonies also inhabit abandoned galleries of woodboring beetles in dead branches in the crowns of pines. Because newly mated queens found colonies in abandoned woodboring beetle galleries in the first dead branches that form on pine saplings, C. ashmeadi is dependent on cavities made by other insects throughout its life cycle, and does little if any excavation of its own. Mature colonies nest preferentially in chambers greater than 10 cm2 in area, a relatively rare chamber size. In natural pine forests, this does not seem to limit the ant's populations.
Founding queens containabout 50% fat and lose about half of their dry weight during the claustral period, converting approximately half of this lost weight into progeny. The claustral period is about 40 to 50 days at 27°C. Mature colonies contain several tens of thousands of workers (est. up to 80,000), and have a life expectancy of 10 to 15 years. Each colony occupies an entire tree, and sometimes two trees if they are close together. Within a colony, there is a single queen capable of laying up to 450 eggs/day during the warm season. Such queens weigh 12 to 18 mg, have 50 to 60 active ovarioles and 120 to 600 vitellogenic oocytes in their ovaries.
Mature colonies begin producing sexual brood in late April or early May. Sexual adults are present from late May through June. Mating flights commence in June and most sexuals have left their natal nests by late July. Female sexuals are an especially large investment; the energetic content of a single, flight-ready female sexual is almost 20 times that of a worker. The newly mated queen sequesters a mean of 2.64 × 106 sperm in her spermatheca, a supply that should last her for 16 years at the observed reproductive rates.
Formicidae; nest chambers; arboreal ants; colony founding; seasonality; colony longevity; Cossidae; Givira francesca (Dyar); Buprestidae; Cerambicidae; woodboring beetles; longleaf pine; slash pine; Pinus palustris; Pinus elliotti; red-cockaded woodpecker
During the last decades, the number of people suffering from dermatophytoses has seriously increased, mainly due to the development of resistant strains of microorganisms to a range of formally efficient antibiotics. Polyscias fulva, a medium size tree which grows in the West Region of Cameroon is traditionally used for local application against dermatoses and orally against venereal infections. The dichloromethane-methanol (1:1 v/v) extract from the stem bark of Polyscias fulva was evaluated for its in vitro and in vivo antifungal activities.
The plant extract was prepared by maceration of its stem bark powder in CH2Cl2-MeOH (1:1 v/v). The extract obtained was successively partitioned in hexane, ethyl acetate and n-butanol. Phytochemical screening was performed using standard methods. In vitro antidermatophytic activity was assayed by the well diffusion and broth microdilution methods. The degree of dermal irritation of the crude extract was determined in guinea pigs using the occluded dermal irritation test method. The in vivo antidermatophytic activity of the extract-oil formulation (1.25, 2.5 and 5% w/w concentrations) was evaluated using Trichophyton mentagrophytes-induced dermatophytosis in a guinea pigs model.
Phytochemical screening indicated that, the crude extract, ethyl acetate, n-butanol and residue fractions contain in general saponins, tannins, alkaloids, anthraquinones and phenols while the hexane fraction contains only alkaloids. The ethyl-acetate, n-butanol and residue fractions displayed higher antifungal activities (MIC = 0.125-0.5 mg.mL-1) against eight dermatophytes as compared to the crude extract (MIC = 0.5-1 mg.mL-1). This latter appeared to have slight perceptible erythema effects on guinea pigs as the primary irritation index (PII) was calculated to be 0.54. In vivo, the antidermatophytic activities of the extract-oil formulations were dose-dependent. Griseofulvin-oil 5% at 0.01 g/kg and formulated extract-oil (5%) at 0.1 g/kg eradicated the microbial infection after thirteen and fourteen days of daily treatment respectively.
The results of preclinical in vitro and in vivo evaluations indicate that the extract-oil formulation at 5% may constitute an alternative means to alleviate fungal infections caused by dermatophytes.
Antidermatophytic activity; Polyscias fulva; Extract-oil formulation; Irritation test; Primary irritation index; Guinea pigs
A new strategy for the synthesis of the Strychnos alkaloid (±)-strychnine has been developed and is based on an intramolecular [4+2]-cycloaddition/rearrangement cascade of an indolyl substituted amidofuran. The critical D-ring was assembled by an intramolecular palladium catalyzed enolate-driven cross-coupling of an N-tethered vinyl iodide.
This paper represents the first ethnobotanical study in Chail valley of district Swat-Pakistan and provides significant information on medicinal plants use among the tribal people of the area. The aim of this study was to document the medicinal uses of local plants and to develop an ethnobotanical inventory of the species diversity.
In present study, semi-structured interviews with 142 inhabitants (age range between 31–75 years) were conducted. Ethnobotanical data was analyzed using relative frequency of citation (RFC) to determine the well-known and most useful species in the area.
Current research work reports total of 50 plant species belonging to 48 genera of 35 families from Chail valley. Origanum vulgare, Geranium wallichianum and Skimmia laureola have the highest values of relative frequency of citation (RFC) and are widely known by the inhabitants of the valley. The majority of the documented plants were herbs (58%) followed by shrubs (28%), trees (12%) and then climbers (2%). The part of the plant most frequently used was the leaves (33%) followed by roots (17%), fruits (14%), whole plant (12%), rhizomes (9%), stems (6%), barks (5%) and seeds (4%). Decoction was the most common preparation method use in herbal recipes. The most frequently treated diseases in the valley were urinary disorders, skin infections, digestive disorders, asthma, jaundice, angina, chronic dysentery and diarrhea.
This study contributes an ethnobotanical inventory of medicinal plants with their frequency of citations together with the part used, disease treated and methods of application among the tribal communities of Chail valley. The present survey has documented from this valley considerable indigenous knowledge about the local medicinal plants for treating number of common diseases that is ready to be further investigated for biological, pharmacological and toxicological screening. This study also provides some socio-economic aspects which are associated to the local tribal communities.
Geo-ethnographical; Ethnoflora; Khyber Pakhtunkhwa; Pharmacological studies