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
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
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
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.
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
In Ayurveda, a series of pharmaceutical procedures which converts a poisonous drug into a therapeutically very effective medicine for various ailments is termed as Shodhana. Various medias are being used for processing the herbal poisonous drugs, are quite interesting to understand with modern scientific technology. The analysis of media before and after Shodhana (purification /processing) will give clear rationale behind the selection of the particular media for the particular drug. The change that takes place during the Shodhana process can be explored by modern analytical methods. Researchers have proved the presence of strychnine and brucine in milk after Shodhana of Nux-vomica highlighting the role media for Shodhana. Importance of Shodhana, the role of media used for Shodhana process of few poisonous drugs is dealt briefly with scientific view.
Shodhana; Purification; Processing; Poisonous herbs; Media
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
The apparatus and technique used in the preparation and observation of explants of brain tissue capable of producing spontaneous potentials in vitro are described. The magnitude and pattern of spontaneous potentials from explants of telencephalon of 15 day chick embryos (measured using external bare platinum electrodes) and some aspects of their "normal" behavior during 12 days in vitro are also described. No change was noted in these potentials with change of amplifiers, recorders, or electrodes. The response of the potentials to change in temperature and proportionate composition of the atmosphere around the explant was such as to suggest that the potentials arise as a result of a living process. The changes brought about by the administration of anesthetics, strychnine, brucine, and barbiturates were those that might be anticipated in a normal functional activity of the central nervous system. It is concluded that these potentials are a true physiological phenomenon and arise from living cells of the central nervous system.
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.
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
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
• Background and Aims The phenotypic plasticity of leaf life span in response to low resource conditions has a potentially large impact on the plant carbon budget, notably in evergreen species not subject to seasonal leaf shedding, but has rarely been well documented. This study evaluates the plasticity of leaf longevity, in terms of its quantitative importance to the plant carbon balance under limiting light.
• Methods Seedlings of four tropical tree species with contrasting light requirements (Alstonia scholaris, Hevea brasiliensis, Durio zibethinus and Lansium domesticum) were grown under three light regimes (full sunlight, 45 % sunlight and 12 % sunlight). Their leaf dynamics were monitored over 18 months.
• Results All species showed a considerable level of plasticity with regard to leaf life span: over the range of light levels explored, the ratio of the range to the mean value of life span varied from 29 %, for the least plastic species, to 84 %, for the most. The common trend was for leaf life span to increase with decreasing light intensity. The plasticity apparent in leaf life span was similar in magnitude to the plasticity observed in specific leaf area and photosynthetic rate, implying that it has a significant impact on carbon gain efficiency when plants acclimate to different light regimes. In all species, median survival time was negatively correlated with leaf photosynthetic capacity (or its proxy, the nitrogen content per unit area) and leaf emergence rate.
• Conclusions Longer leaf life spans under low light are likely to be a consequence of slower ageing as a result of a slower photosynthetic metabolism.
Alstonia scholaris; carbon balance; Durio zibethinus; Hevea brasiliensis; Lansium domesticum; leaf life span; light; plasticity
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
HIV-1 (Human immunodeficiency virus type 1) is a member of retrovirus family that could infect human and causing AIDS
disease. AIDS epidemic is one of most destructive diseases in modern era. There were more than 33 million people infected by HIV
until 2010. Various studies have been widely employed to design drugs that target the essential enzymes of HIV-1 that is, reverse
transcriptase, protease and integrase. In this study, in silico virtual screening approach is used to find lead molecules from the
library or database of natural compounds as HIV-1 reverse transcriptase inhibitor. Virtual screening against Indonesian Herbal
Database using AutoDock4 performed on HIV-1 reverse transcriptase. From the virtual screening, top ten compounds were
mulberrin, plucheoside A, vitexilactone, brucine N-oxide, cyanidin 3-arabinoside, alpha-mangostin, guaijaverin, erycristagallin,
morusin and sanggenol N.
Indonesian herbal database; HIV-1; molecular docking; virtual screening
An increased inclination has been observed for the use of herbal drugs in chronic and incurable diseases. Treatment of psychiatric diseases like schizophrenia is largely palliative and more importantly, a prominent adverse effect prevails with the majority of anti-psychotic drugs, which are the extrapyramidal motor disorders. Existing anti-psychotic drug therapy is not so promising, and their adverse effect is a matter of concern for continuing the therapy for long duration.
This experimental study was done to evaluate the neuroleptic activity of the ethanolic extracts of two plants Alstonia Scholaris and Bacopa Monnieri with different anti-psychotic animal models with a view that these plant extracts shall have no or at least reduced adverse effect so that it can be used for long duration.
Materials and Methods:
Two doses of both the extracts (100 and 200 mg/kg) and also standard drug haloperidol (0.2 mg/kg) were administered to their respective groups once daily with 5 different animal models. After that, the concentration of the dopamine neurotransmitter was estimated in two different regions of the brain viz. frontal cortex and striatum.
The result of the study indicated a significant reduction of amphetamine-induced stereotype and conditioned avoidance response for both the extracts compared with the control group, but both did not have any significant effect in phencyclidine-induced locomotor activity and social interaction activity. However, both the extracts showed minor signs of catalepsy compared to the control group. The study also revealed that the neuroleptic effect was due to the reduction of the dopamine concentration in the frontal cortex region of the rat brain. The results largely pointed out the fact that both the extract may be having the property to alleviate the positive symptoms of schizophrenia by reducing the dopamine levels of dopaminergic neurons of the brain.
The estimation of dopamine in the two major regions of brain indicated the alteration of dopamine levels was the reason for the anti-psychotic activity as demonstrated by the different animal models.
Alstonia; bacopa monniera; dopamine; dyskinesia; neuroleptic; psychosis
Alstonia boonei De Wild is a herbal medicinal plant of West African origin, popularly known as God's tree or “Onyame dua”. Within West Africa, it is considered as sacred in some forest communities; consequently the plant parts are not eaten. The plant parts have been traditionally used for its antimalarial, aphrodisiac, antidiabetic, antimicrobial, and antipyretic activities, which have also been proved scientifically. The plant parts are rich in various bioactive compounds such as echitamidine, Nα-formylechitamidine, boonein, loganin, lupeol, ursolic acid, and β-amyrin among which the alkaloids and triterpenoids form a major portion. The present paper aims at investigating the main research undertaken on the plant in order to provide sufficient baseline information for future work and for commercial exploitation.
Many diseases are being spread in the word by micro organisms. This necessitates the development of cost effective and easily available antimicrobial medicines. Plants have generally been source of alkaloids, steroids, terpenoids, carbohydrates, amino acids, vitamins, glycosides and various pigments. The chemical exploitation of varieties of indigenous plants is therefore likely to offer a cost effective treatment for many diseases leading to the development of the nation and welfare of the society. The present communication reports that hydrocarbons, triterpenes and phytosterols present in Alstonia scholaris, are responsible for its medicinal value.
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
A trans-cleaving asymmetric hammerhead ribozyme directed against an AUC decreases target motif within an RNA specific for human immunodeficiency virus type 1 (HIV-1) was generated. The AUC decreases motif of the target RNA was permutated in order to generate all 12 variants of an NUX decreases consensus target motif, wherein N = A, C, G or U and X = A, C or U. Four asymmetric hammerhead ribozymes differing in the nucleotide that is complementary to N were generated, of which each was specific for three of the 12 target motifs. The residual sequence context within helices I and III remained unchanged. All 12 combinations resulted in cleavage of the target RNA. Using single-turnover conditions, the detectable cleavage rate constants at 37 degrees C were determined, which varied considerably depending on the NUX decreases motif. The NUC decreases motifs were cleaved more efficiently, with AUC decreases being cleaved best. Comparison with previous studies indicates that the sequence context of the NUX decreases motif plays a major role for the detectable cleavage activity.