Pharmacognostic characterization of Dicleptera chinensis by scanning electron microscopy, light microscopy, and analytical techniques.

Dicleptera chinensis J. (Acanthaceae) has been employed in traditional medicinal systems for treating various ailments. It has been used as an anti-inflammatory, wound healing, diuretic, and detoxifying agent in different regions of the world. This study determines several pharmacognostic standards, which are useful to ensure safety, efficacy, and purity of D. chinensis. Different parts of the plant were examined through a scanning electron microscope and light microscope, and cross-section images revealed several useful botanical features of the plant. The color, size, odor, shape, and surface characteristics of plant parts were also examined macroscopically. Pharmacognostic standardization parameters including ash values, loss on drying, swelling index, hemolytic index, and foaming index were determined in accordance with WHO guidelines. Heavy metal analysis was executed through atomic absorption spectrophotometer which depicted the presence of heavy metals and trace elements within the acceptable range. Qualitative phytochemical tests for alkaloids, flavonoids, saponins, glycosides, tannins, carbohydrates, lipids, protein, and so forth of plant extract were also performed, which showed the valuable amount of these phytochemicals useful for medicinal purposes. Preliminary phytochemical tests provide an indication for major phytoconstituents classes present in the plant. These quantitative and qualitative microscopic features are helpful in establishing the pharmacopeia standards of plant. Assessment of various pharmacognostic features such as morphology of various plant parts explained along with physicochemical and phytochemical analysis could be very helpful for future research. RESEARCH HIGHLIGHTS: Pharmacognostic standardization is employed as reported evidence for correct identification of D. chinensis. Structures identified by scanning electron microscopy and light microscopy serve as diagnostic features of plant. Important secondary metabolites present in the plant suggest the need for further exploration through advanced metabolomics and other analytical techniques.

Evaluating the Aphrodisiac Potential of Mirabilis jalapa L. Root Extract: Phytochemical Profiling and In Silico, In Vitro, and In Vivo Assessments in Normal Male Rats.

The traditional use of Mirabilis jalapa L. roots to enhance male sexual performance prompted us to assess the in silico, in vitro, and in vivo aphrodisiac activities of its hydroethanolic extract using normal male rats. Spectroscopic characterization indicated the presence of ß-D-glucopyranoside, methyl-1,9-benzyl-2,6-dichloro-9H-purine, and Bis-(2-ethylhexyl)-phthalate; these compounds have a significant inhibitory effect on the phosphodiesterase-5 (PDE-5) enzyme in silico evaluation and minerals (including zinc, cadmium, and magnesium). Other phytochemical analyses revealed the presence of phenolic compounds and flavonoids. These phytochemicals and minerals may contribute to the aphrodisiac activities of the extract. Additionally, the in vivo study revealed that the administration of M. jalapa root extract (300 mg/kg) significantly enhanced (p < 0.01, p < 0.03) mount, intromission, and ejaculation frequencies while significantly (p < 0.05) decreasing the mount and intromission latencies, as well as the post-ejaculatory interval time, in comparison with the standard drugs sildenafil and ginseng, resulting in enhanced erection and sexual performance in the rats. Furthermore, the extract significantly (p < 0.05) increased penile reflexes and also elevated the levels of testosterone and luteinizing hormones. Extract (300 mg/kg) significantly (p < 0.05) inhibited the PDE-5 enzyme in an in vitro study. Concludingly, the comprehensive findings of this study suggest that a standardized herbal extract derived from M. jalapa roots alleviates erectile dysfunction and premature ejaculation in male rats. M. jalapa root extract proved to be an alternative treatment for erectile dysfunction and premature ejaculation.

In vitro, in vivo and in silico evaluation of analgesic, anti-inflammatory, and anti-pyretic activity of salicylate rich fraction from Gaultheria trichophylla Royle (Ericaceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal properties of Gaultheria have been used in traditional medicine to treat pain and inflammation. AIM OF THE STUDY: Hence, the purpose of this study was to evaluate the analgesic, antipyretic, and anti-inflammatory properties of Gaultheria trichophylla Royle extract and salicylate-rich fraction in vivo, in vitro, and in silico. MATERIALS AND METHODS: In vivo analgesic, antipyretic, and anti-inflammatory of extract and a salicylate-rich fraction (at doses of 100, 200, 300, and 150 mg/kg) were assessed using healthy albino mice employing acetic acid-induced writhing, tail immersion test, carrageenan-induced inflammation, and croton oil-induced edema. For in vitro testing of extracts COX and LOX enzyme inhibition assays were used. Molecular docking studies were conducted for in silico testing of the inhibitory activity of the dominant compound Gaultherin against COX and LOX. RESULTS: G-EXT 200 and 300 and G-SAL 150 mg/kg reduced pyrexia significantly (P < 0.05 and P < 0.01). G-EXT-200, 300, and G-SAL 150 reduce the writing to a significant level (p > 0.05, p < 0.01). G-EXT 200 and 300 and G-SAL 150 mg/kg doses the analgesic effect was significant (p > 0.05, p > 0.01) and was comparable to tramadol. G-EXT 100 200, 300 mg/kg showed 43.8%, 47.94% and 56% respectively. G-SAL 150 mg, rich in salicylates, showed maximum inhibition of 65.75% next to standard drug diclofenac with 76.7% inhibition. G-EXT 100 and 200 mg/kg dose showed significant (p < 0.05) reduction in ear edema. With 300 mg/kg dose the effect was more (61.89%, p < 0.01). The salicylate-rich fraction G-SAL and Celecoxib showed an almost similar effect (p < 0.01). Significance inhibition was shown in the COX-2 test (G-EXT 39.70 and G-SAL 77.20 IC50 µg/ml) and in the 5-LOX test (G-EXT 28.3 and G-SAL 39.70 IC50 µg/ml). The preliminary in silico results suggest that the investigated compound showed excellent inhibitory activity against COX and LOX enzymes as evident from the free binding energy. Molecular docking revealed that Gaultherin binds well in the COX and LOX enzyme catalytic region. CONCLUSION: The extract and salicylate-rich fraction obtained from G. trichophylla showed significant analgesic, anti-inflammatory, and antipyretic effects in vivo, in vitro, and in silico assays that support its use in traditional medicine.

Citrus flavonoids as potential therapeutic agents: A review.

The plants Rutaceae family are known to have contributed a lot toward food and medicine. The most important metabolites of the family are flavonoids. A systematic review was conducted to collect chemical and pharmacological information of flavonoids isolated from family Rutaceae till 2018. A plethora of flavonoids have been isolated and studied systematically for various bioactivities, including anticancer, antibacterial, antiviral, analgesic, antioxidant, antidiabetic, antiinflammatory, in bronchitis, ulcers, and so on. The important groups of flavonoids isolated are naringin, poncirin, rhoifolin, marmesin, hesperidin, tangeretin, nobiletin, glychalcone, glyflavanone, lemairone, acacetin 3,6-di-C-glucoside, vicenin-2, lucenin-2 4'-methyl ether, narirutin 4'-O-glucoside, apigenin 8-C-neohesperidoside, phloretin 3',5'-di-C-glucoside, rutin, rhamnetin, dihydrokaempferol, dihydrokaempferol 3-O-rhamnoside (engeletin) and kaempferol, excavaside A and B, myricetin 3-O-ß-D-rutinoside, myricetin 3,3'-di-α-l-rhamnopyranoside, myricetin 3'-α-l-rhamnopyranoside, and others. The flavonoids isolated from the citrus family need to be considered from a nutraceutical, therapeutic, and pharmaceutical point of view for future medicine.

Phytochemical, antimicrobial, antioxidant and enzyme inhibitory potential of medicinal plant Dryopteris ramosa (Hope) C. Chr.

BACKGROUND: Dryopteris ramosa has numerous potentials uses in the treatment of different maladies as old traditional medication. The fronds of D. ramose are edible and orally administered for producing antibiotic effect. They are also used as astringent and febrifuge, and as a pesticide. METHODS: Extraction of fronds of D. ramosa using solvents of increasing polarity, namely, ethyl acetate, methanol and water were tested for phytochemical (qualitative tests, GC-MS), antimicrobial (well method), antioxidant (DPPH), antifungal (tube dilution), cytotoxic activity (brine shrimps lethality assay) and LOX and COX inhibitory activities were performed using standard methods. RESULTS: The phytochemical analysis of the crude methanolic extract revealed that the fronds are rich in flavonoids, alkaloids, saponins, tannins, glycosides and triterpenoids. The total flavonoid content of the ethyl acetate fraction was 46.28 µg QE/mg extract. The GC-MS analysis revealed nine major compounds that constituted the crude drug and potentially had a role in reported activities. The crude extract was the most active amongst all the fractions against the bacterial and fungal strains used such that it inhibited the growth of P. aeruginosa with a zone of 13 mm and a MIC value of 16 µg/ml as compared to the standard cefixime, which inhibited the zone by only 10 mm and a MIC value of 32 µg/ml. The highest antioxidant potential in DPPH assay was shown by the crude extract with 91.948% free radical scavenging activity. The bring shrimps lethality potential of the crude extract was the highest, with a LD50 value of 47.635 µg/ml. The ethyl acetate fraction inhibits 91.36% of alpha glucosidase enzyme at a concentration of 0.5 mg/ml. In case of acetylcholine esterase inhibition assay, the methanol fraction inhibits 58.26% of the enzyme activity. Similarly, for butyrylcholine esterase inhibition, the maximum inhibitory effect was seen in the methanol fraction, with a percentage inhibition of 47.32%. CONCLUSION: These test results support traditional medicinal uses of the plant. Dryopteris ramosa could be imperative for being used as a therapeutic agent and the medicinal importance of this plant should be further investigated.

Phytochemical investigation, anti-inflammatory, antipyretic and antinociceptive activities of Zanthoxylum armatum DC extracts-in vivo and in vitro experiments.

Zanthoxylum armatum (ZA) a commonly used medicinal plant was investigated for phytochemical, anti-nociceptive, anti-inflammatory and antipyretic effects. Extract and total alkaloids from fruit and leaves significantly (p < 0.001) reduced the rectal temperature in mice. The effects of bark and root extracts were less significant. In writhing and tail flick methods both the extract and total alkaloids from fruit showed significant (p < 0.05 and p < 0.001) antinociceptive activity. The fruit extract and crude alkaloids showed significant (p < 0.01) lowering of inflammation of paw edema in mice. Crude alkaloids from fruit and leaves showed significant enzyme inhibition with lower IC50 values for 15 and 69 against COX and 21 and 62 µg/ml against LOX. This study rationalize the usage of this spice in traditional medicine for management of pain and inflammation involving LOX and COX inhibition as possible mechanism. GC-MS analysis revealed the presence of various constituents which might contributed towards the pain and inflammation alleviation.

Phenolic contents, elemental analysis, antioxidant and lipoxygenase inhibitory activities of Zanthoxylum armatum DC fruit, leaves and bark extracts.

Zanthoxylum armatum (DC) is a traditional spice and important herb used in Asia as a part of food and household medicine for the treatment of various conditions. The present study was designed to investigate in vitro for phenolic/flavonoid contents, antioxidant activities, lipoxygenase inhibitory activity, minerals and heavy-metal contents. The leaves, bark and fruit of Zanthoxylum armatum were extracted with organic solvent and evaluated for phenolic contents (Folin-Chiocalteu method), for flavonoids contents (colorimetric method), for in vitro antioxidant assays (DPPH and FRAP), lipoxygenase inhibitory activity (5-LOX assay), mineral contents (atomic absorption), and for heavy-metal contaminants (atomic absorption). The fruit contained the highest phenolic (25.6±1.2mg GAE/g) and flavonoid (26.3±1.4mg QE/g) contents and therefore, exhibited the most effective antioxidant properties in DPPH (88.5±0.9% inhibition) and FRAP (94.21±3.2% inhibition) assays. The extracts also inhibited the LOX enzyme, and the fruit showed more inhibition (63.8±1.2 %) as compared with the leaves and bark. Z. armatum contain valuable minerals and fortified with magnesium (4.948±0.2, 3.07±0.03 and 3.53±0.12) and potassium (0.19±0.011, 1.91±0.003, and 1.90±0.05) for leaves, fruit, and bark, respectively. The chemical profiling for heavy metals showed that their concentrations were within permissible limits. The data suggest that Z. armatum is a safe and valuable natural agent with functional properties for food and pharmaceutical industries.

Butyrlycholine esterase inhibitory activity and effects of extracts (fruit, bark and leaf) from Zanthoxylum armatum DC in gut, airways and vascular smooth muscles.

BACKGROUND: Fruit, bark and leaves of Zanthoxylum armatum DC are popular remedies for gastrointestinal, cardiovascular and respiratory disorders in the subcontinent traditional practices. The aim of the study was to individually probe the profile of methanol extracts from three different parts of Zanthoxylum armatum. METHODS: The ex-vivo muscle relaxant effects of extracts were assessed in the isolated intestine, trachea and thoracic aortic rings and were compared with the positive controls and CRC were constructed. The anti-diarrheal effect of extracts was evaluated in mice by inducing diarrhea with castor oil. The extracts were also studied for acute toxicity and butyrylcholine esterase inhibition. RESULTS: The extracts from fruit, bark and leaves of Z. armatum showed inhibitory effect against the butyrylcholine esterase enzyme with percent inhibition of 50.75 ± 1.23, 82.57 ± 1.33, and 37.52 ± 1.11respectively, compared to standard serine (IC50: 0.04 ± 0.001 µmol/L). The fruit and bark extracts provided 75, and 52% diarrheal protection, compared to verapamil (96%). In isolated rabbit jejunum strips, increasing addition of the extracts inhibited the spontaneous and high K+ precontractions with EC50 values of 0.71 and 3 mg/mL for fruit, EC50 values of 0.61 and 0.5 mg/mL for bark, EC50 0.81 and 3.1 mg/mL for leaves, like verapamil. The extracts induced a concentration-dependent relaxation of the carbachol (1 µM) and high K+ (80 mM) precontractions with EC50 values of 2.4 and 0.9 mg/mL for fruit, EC50 values of 1.2 and 3 for leaves. The bark extract was equipotent against both contractions with EC50 3.1 and 0.7 mg/mL, respectively. In the aortic rings, the fruit extract completely relaxed the phenylephrine (1 µM)-induced contractions with (EC50 value = 0.8 mg/ml) and a partial inhibition of high K+ induced contractions. The leaves extract completely relaxed the aortic contractions with (EC50 values = 1.0 and 8.5 mg/ml). The extracts caused no acute toxicity up to 3 g/kg dose. CONCLUSIONS: The experiments revealed that the extracts of aerial parts of Z. armatum have antidiarrheal properties in vivo and showed spasmolytic effect in intestinal and tracheal preparations with possible mechanism involving the blockage of Ca++ channels. These experiments provide enough justification for use of this plant in ethnomedicine in diarrhea, gut and bronchial spasms.

Enzymes inhibitors from natural sources with antidiabetic activity: A review.

Natural products have been extensively investigated for antidiabetic therapy. Many of the natural products have direct or indirect effect in diabetes pathways as enzyme inhibitors. The most involved mechanisms are inhibition of intestinal alpha-glucosidase and alpha-amylase, lens aldose reductase, oxidative stress protection, inhibition of formation of advanced glycation end products, inhibition of aldose reductase, lowering plasma glucose levels, altering enzyme activity of hexokinases and glucose-6-phosphate, synthesizing and releasing of insulin, postprandial hyperglycemia inhibition, stimulation of GLUT-4, decreasing activity of G6P, lowering the level of skeletal hexokinases, etc. The following medicinal plants products or extracts showed promising effects as enzyme inhibitors: Abelmoschus moschatus, Alangium salvifolium, Azadirachta indica, Bidens pilosa, Boerhaavia diffusa, Capsicum frutescens, Cassia alata, Eclipta alba, Embellica officinalis, Ficus carica, Gentiana Olivier, Glycyrrhiza glabra, Gymnema sylvestre, Hordeum vulgare, Ipomoea aquatica, Juniperus communis, Mangifera indica, Momordica charantia, Ocimum sanctum, Punica granatum, and Zingiber officinale. Some of the group of phytochemicals isolated with enzyme inhibition activities are Alkaloids, sesquiterpene and saponins, polysaccharides, flavonoids, dietary fibers, ferulic acid, tannins, limonene, and oleuropeoside. This review will provide very useful material to enhance the efficiency of rational antidiabetic drug design.

Zanthoxylum armatum DC extracts from fruit, bark and leaf induce hypolipidemic and hypoglycemic effects in mice- in vivo and in vitro study.

BACKGROUND: Zanthoxylum armatum DC is an important medicinal plant of south East Asia, and has been used to treat various ailments in traditional medicine including diabetes. This study investigated the in vitro and in vivo antidiabetic and biochemical effects of extracts of Z. armatum in mice. METHOD: The extracts of fruit, bark and leaf from Z. armatum were tested for α-glucosidase inhibition activity. Albino mice of either sex weighing (26-30 g) assigned into groups. Diabetes was induced by IP injection of alloxan monohydrate (150 mg/kg). The extracts (500 mg/kg) and standard (Glibenclamide 10 mg/kg) were administered to mice for 15 days. Serum biochemical parameters were monitored for the period of study. RESULTS: The leaves and bark extracts showed maximum α-glucosidase inhibition (96.61 ± 2.13 and 93.58 ± 2.31% respectively). The extracts treated and the standard treated groups showed significant decrease in the fasting blood glucose levels compared to diabetic control. The effect was more pronounced in mice treated with leaves extract. In the in vivo studies body weights of diabetic mice treated with Z. armatum extracts and the standard did not reduced to extent as observed in diabetic control and this difference was significant (p < 0.05). There was a significance (p < 0.001) improvement in blood hemoglobin, urea, creatinine, cholesterol, and triglycerides of the extracts treated diabetic mice. The extracts showed hypolipidemic effect by reducing the LDL level. The extracts produced no prominent changes in proteins levels. CONCLUSION: It can be concluded that Z. armatum extracts showed excellent antidiabetic potential in vivo and in vitro and could be considered for further appraisal in clinical assessment and drug development.

Psoralea corylifolia L: Ethnobotanical, biological, and chemical aspects: A review.

Psoralea corylifolia L. (Leguminosae) is a well-known traditional medicinal plant used from ancient times for treatment of various ailments. It is widely distributed and an important part of therapeutics in Ayurveda and in Chinese medicines. The aim of this review is to present comprehensive and most up to date report on its ethnobotanical, ethnopharmacological, clinical, phytochemical, and side effects. Studies on the ethnobotanical, ethnopharmacological, clinical, phytochemical, and side effects of P. corylifolia were published until year 2017 and were searched using various scientific databases. The scientific literature searched revealed that these plant species has been extensively investigated in vivo and in vitro for various biological and phytochemical studies. It has cardiotonic, vasodilator, pigmentor, antitumor, antibacterial, cytotoxic, and anti-helminthic properties and locally used for alopecia, inflammation, leukoderma, leprosy, psoriasis, and eczema. So far, about a hundred bioactive compounds have been isolated from seeds and fruits, and most important compounds identified belongs to coumarins, flavonoids, and meroterpenes groups. This review article summarized the most updated scientific literature on bioactive phytochemical and biological activities of P. corylifolia. This article will be a useful addition to providing information for future research, and more standard clinical trials are needed for the plant to be used as therapeutic agent.

Evaluation of Zanthoxylum armatum Roxb for in vitro biological activities.

Zanthoxylum armatum fruits are used traditionally as a spice in various food preparations. The aim of this study was analysis of antimicrobial, cytotoxic, phytotoxic, insecticidal, and anti-leishmanial activity. The crude extract showed 86 ± 10% antifungal activity (Agar tube dilution method) against Trichophyton longifusis while n-hexane, chloroform, and aqueous-methanol fractions inhibited this pathogen by 90 ± 7, 85 ± 10 and 70 ± 9% respectively. The n-hexane and aqueous-methanol fraction also, respectively, showed 40 ± 10 and 87 ± 9% inhibition of Microsporum canis. Chloroform fraction also displayed antifungal activity against Aspergillus flavus (60 ± 10%) and aqueous-methanol fraction against F. solani (40 ± 8%). The crude ethanolic extract and its chloroform and aqueous-methanol fraction exhibited significant toxicity (Brine shrimps lethality assay) against brine shrimps having LC50 value of 6.66 ± 1.1, 21.4 ± 3.3 and 29.6 ± 3.9 µg/ml, respectively. The crude ethanolic extract and its n-hexane soluble portion exhibited good anti-leishmanial activity (well serial dilution method) each having IC50 values of 50 ± 5 µg/ml. The crude extract and various fractions possessed excellent herbicidal activity (Lemna minor assay), and caused more than 90% inhibition of the plant growth at 1000 µg/mL. The ethanolic extract, n-hexane and chloroform soluble portions caused 90% mortality in insecticidal activity (direct contact method) of Rhyzopertha dominica. The ethanolic extract and its n-hexane soluble portion, respectively, caused 80 and 90% mortality of Callosobruchus analis. The present study showed that the tested fruit extracts of Z. armatum exhibited strong antifungal, cytotoxic, phytotoxic, insecticidal, and anti-leishmanial effects.

Cytotoxic activity of extracts and crude saponins from Zanthoxylum armatum DC. against human breast (MCF-7, MDA-MB-468) and colorectal (Caco-2) cancer cell lines.

BACKGROUND: Zanthoxylum armatum DC has been an important traditional plant known for its medicinal properties. It is well known for its antimicrobial, larvicidal and cytotoxic activities. METHODS: The potential anticancer effects of the methanol extract and the crude saponins from fruit, bark and leaves of Z. armatum on breast (MDA-MB-468 and MCF-7) and colorectal (Caco-2) cancer cell lines using MTT, neutral red uptake(NRU) and DAPI stain assays were evaluated. RESULTS: In MTT assay the methanol extract of fruit (Zf), bark (Zb) and leaves (Zl) of Zanthoxylum armatum, showed significant and dose dependent growth inhibition of MCF-7, MDA MB-468 and Caco-2 cancer cell lines in a dose of 200 µg/ml and above. The saponins (Zf.Sa, Zb.Sa and Zl.Sa) showed significant activity against MDA MB-468 (95, 94.5 and 85.3%) as compared to MCF-7 (79.8, 9.43, 49.08%) and Caco-2 (75.8, 61.8, 68.62%) respectively. The extracts were further tested in more sensitive NRU assay and its was found that Zf extract showed higher cytotoxic activity as compared to Zb and Zl extracts with 100 µg/ml concentration. The breast cancer cell lines showed more sensitivity toward the crude saponins from fruit and bark with maximum inhibition of up to 93.81(±2.32) % with respect to 71.19(± 2.76) of Actinomycin-D. DAPI staining experiment showed that saponins from fruit induced apoptosis mode of cell death in all three types of cell lines while saponins form leaves and bark showed similar results against MDA MB-468 indicated by nuclear fragmentation and chromatin condensation. The effect of saponins from fruit, bark and leaves (Zf.Sa, Zb.Sa and Zl.Sa) against Caco-2 cell lines inhibited the growth of Caco-2 by 53.16 (±3.31) %, 66.43 (± 3.24) and 45.96 (± 10.67) respectively with respect to Actinomycin-D (4 µM) which showed the growth inhibition of 65.40(±4.29) %. CONCLUSION: The current study clearly demonstrates that the extract and crude saponins from fruit, bark and leaves of traditional medicinal plant Zanthoxyllum armatum DC., has the potential to exert its cytotoxic effect on cancer cell lines isolated form human by a mechanism involving apoptosis. The overall finding demonstrate that this plant specially fruits, could be potential source of new anticancer compounds for possible drug development against cancer.

Airways and vascular smooth muscles relaxant activities of Gaultheria trichophylla.

The aim of this experimental work was to explore the potential pharmacological activities of Gaultheria trichophylla Royle in hyperactive respiratory and vascular conditions. Gaultheria trichophylla was extracted with solvents, phytochemical detection tests were performed, and rabbit trachea and aorta strips were used to evaluate its effects on airways and vascular smooth muscles. Qualitative phytochemical tests showed the presence of flavonoids, alkaloids, anthraquinones, saponins, terpenoids, and condensed tannins. The methanol extract caused inhibition (EC50 values of 3.12 mg/mL) of carbachol (1 µM) and partial relaxation of K+(80 mM) caused contractions in tracheal strips. The chloroform extract was comparatively more potent against carbachol than K+ induced contraction with EC50 values of 0.64 and 2.26 mg/mL, respectively. However, the n-hexane extract showed more potency against K+ than cabachol induced contractions, as in case with verapamil, with EC50 values of 0.61 and 6.58 mg/mL, respectively. In isolated prepared trachea, the extracts displaced the carbachol concentration response curves and maximum response was suppressed. In rabbit aorta preparations, methanol and n-hexane extracts partially relaxed phenylephrine (1 µM) and K+ induced vasoconstrictions. However, the chloroform extract inhibited phenylephrine induced contractions and exhibited a vasoconstrictor effect at lower concentrations and a relaxant effect at higher concentrations against K+ precontractions. The data indicates that, in addition to others, the extracts of G .trichophylla possess verapamil like Ca++ channel blocking components which explain the possible role of this plant in respiratory and vascular conditions.

Gaultheria trichophylla (Royle): a source of minerals and biologically active molecules, its antioxidant and anti-lipoxygenase activities.

BACKGROUND: Gaultheria trichophylla (Royle) is used as food and for treating many ailments in folk medicine especially against inflammation. The purpose of this in vitro study was to evaluate the ability of extracts of G. trichophylla as anti-oxidant and anti-inflammatory agent and for its mineral contents. METHODS: Powdered plant material (100 g) was extracted with 100 ml each of methanol, chloroform, and n-hexane using soxhlet extractor. Antioxidant activity of methanol extract was assessed by DPPH radical scavenging and FRAP assays. Determination of enzyme inhibition activity was determined using 5-LOX inhibitory activity. Total phenolic and flavonoids contents were measured by Folin-Chicalteu and colorimeteric methods respectively. Minerals and heavy metals contents were determined using Atomic absorption spectrophotometer. Qualitative HPLC analysis were performed using some standard phenolic compounds. RESULTS: The highest phenolic (17.5 ± 2.5 mg GA equivalent/g) and flavonoids (41.3 ± 0.1 mg QE equivalent/g) concentrations were found in methanol extract, which also showed more scavenging activity of 1, 1-diphenyl-2-picrylhydrazyl and ferrous reducing power with IC50 = 81.2 ± 0.2 and IC50 = 11.2 ± 0.1 µg/ml, respectively. The methanol and chloroform extracts showed best inhibition of 5-lipoxygenase enzyme with 90.5 ± 0.7% and 66.9 ± 0.1% at 0.5 mg/ml, respectively. G. trichophylla extract was also evaluated for mineral contents (K, Na, Ca, Mg, Fe, and Cu), and for chemical profiling of heavy metals (Cr, Pb, Cd, Co, Zn, Ni and Hg). CONCLUSION: Our current findings suggest that this plant is good source of minerals and concentration of all heavy metals were within permissible limits. The results revealed that this ignored plant has great pharmaceutical and nutraceutical potential.

Gut modulatory and butyrylcholinesterase inhibitory activities of Gaultheria trichophylla.

CONTEXT: Gaultheria trichophylla Royle (Ericaceae) and related species have been used in the traditional system of medicine for the treatment of diarrhoea, pain and inflammation. OBJECTIVE: The present investigation explores G. trichophylla for its potential activity in hyperactive gut disorders. MATERIALS AND METHODS: Antidiarrheal activity was evaluated on castor oil induced diarrhoea in mice with reference to standard drug verapamil. Gut modulatory activity was performed on isolated jejunum tissue preparations on spontaneous and high potassium induced contractions. Butyrylcholinesterase (BChE) inhibitory activity was performed with an in vitro study. Extract was tested for toxicity in mice. RESULTS: In the in vivo studies, the methanol extract of G. trichophylla and verapamil significantly (p < 0.05, 0.01, 0.001) inhibited the frequency of defecation as well as wetting of faeces when compared with the negative control. The methanol (Gt. MeOH) extract of G. trichophylla caused a dose-dependent inhibitory effect on spontaneous contractions in isolated rabbit jejunum preparations and exhibited a partial inhibitory effect against high K+ (80 mM) induced precontractions. Gt. MeOH shifted the Ca2+ concentration-response curves (CRCs) to the right, suggesting calcium channel blocking like constituents. In an in vitro assay Gt. MeOH inhibited BChE enzyme with an IC50 values of 35.52 ± 1.17 µg/mL. The extract showed no toxicity in mice at the dose of 3 g/kg. DISCUSSION AND CONCLUSION: This study provides evidence that G. trichophylla possesses combinations of inhibitory and stimulatory effects mediated through possible cholinergic and less potent calcium blocking constituents, respectively. The latter may be responsible for the antidiarrheal effect.

Pharmacognostic study and development of quality control parameters for fruit, bark and leaf of Zanthoxylum armatum (Rutaceae).

CONTEXT: Zanthoxylum armatum (Rutaceae) fruit, bark and leaves are used for various conditions of ailments in traditional systems of medicine since ancient times. AIMS: This study is designed to lay down the various pharmacognostic and phytochemical standards which will be helpful to ensure the purity, safety, and efficacy of this medicinal plant. MATERIALS AND METHODS: Various methods including macroscopic, microscopic, physicochemical, and phytochemical methods were applied to determine the diagnostic features for the identification and standardization of intact and powdered drug of Z. armatum leaf, fruit, and bark. RESULTS: The shape, size, color, odor, surface characteristics were determined for the intact drug and powdered materials of leaf, bark and fruit of Z. armatum. Light and electron microscope images of cross-section of leaf and powdered microscopy revealed useful diagnostic features. Histochemical, phytochemical, physicochemical including fluorescence analysis of powdered drug proved useful to differentiate the powdered drug material. High performance liquid chromatography analysis showed the presence of important phytoconstituents such as gallic acid and rutin. CONCLUSION: The data generated from this study would be of help in the authentication of various parts of Z. armatum, an important constituent of various herbal drug formulations. The qualitative and quantitative microscopic features would prove useful for laying down pharmacopoeial standards. Morphology as well as various pharmacognostic aspects of different parts of the plant were studied and have been described here along with phytochemical, physicochemical studies, which will help in authentication and quality control.

Pharmacognostic standardization and preliminary phytochemical studies of Gaultheria trichophylla.

CONTEXT: Gaultheria trichophylla Royle (Ericaceae) has long been used for various ailments in traditional systems of medicines; most importantly it is used against pain and inflammation. AIMS: This study determines various pharmacognostic and phytochemical standards helpful to ensure the purity, safety, and efficacy of medicinal plant G. trichophylla. MATERIAL AND METHODS: Intact aerial parts, powdered materials, and extracts were examined macro- and microscopically and pharmacognostic standardization parameters were determined in accordance with the guidelines given by the World Health Organization (WHO). Parameters including extractive values, ash values, and loss on drying were determined. Preliminary phytochemical tests, fluorescence analysis, and chromatographic profiling were performed for the identification and standardization of G. trichophylla. RESULTS: The shape, size, color, odor, and surface characteristics were noted for intact drug and powdered drug material of G. trichophylla. Light and scanning electron microscope images of cross section of leaf and powdered microscopy revealed useful diagnostic features. Histochemical, phytochemical, physicochemical, and fluorescence analysis proved useful tools to differentiate the powdered drug material. High-performance liquid chromatography (HPLC) analysis showed the presence of important phytoconstituents such as gallic acid, rutin, and quercetin. DISCUSSION AND CONCLUSIONS: The data generated from the present study help to authenticate the medicinally important plant G. trichophylla. Qualitative and quantitative microscopic features may be helpful for establishing the pharmacopeia standards. Morphology as well as various pharmacognostic aspects of different parts of the plant were studied and described along with phytochemical and physicochemical parameters, which could be helpful in further isolation and purification of medicinally important compounds.

Antimicrobial and cytotoxicity activities of the medicinal plant Primula macrophylla.

Primula macrophylla (Primulaceae) is reported as to be useful in asthma, restlessness, insomnia and fish poisoning. Antifungal and toxic activities of crude extract, fractions and a pure isolated compound exhibited statistically significant activities. Excellent antifungal activity was found in the crude extract, benzene and ethyl acetate fractions against T. longifusis and against M. canis with different MIC values. Antileishmanial activity (IC(50) = 50ug/mL) was observed as compared to standard drug Amphotericin B, and cytotoxic activity (LD(50) = 47.919microg/mL) was also found in the chloroform fraction. While pure compound 2-phenylchromone (Flavone) isolated from the chloroform fraction showed good activity (IC(50) = 25microg/mL) against Leishmania and cytotoxicity (LD(50) = 2.0116 microg/mL) in Brine Shrimp experiments. From antileishmanial and cytotoxic activity it can be concluded that 2-phenylchromone is the major compound responsible for these activities.