Amounts Of Alkaloids Research Articles

Stereoselective Mannich Reactions in the Synthesis of Enantiopure Piperidine Alkaloids and Derivatives

AbstractPiperidine alkaloids are members of the alkaloid family that is characterized by the presence of a six‐membered nitrogen‐containing heterocycle. Piperidine alkaloids are found mainly in plants and often exhibit interesting biological and pharmacological activities. Despite the accumulation of these natural products in plants, relatively low quantities of alkaloids are produced in absolute terms and thus synthesis of alkaloids and derivatives thereof remains relevant to identify targets for drug discovery. Throughout the years, researchers have come up with a myriad of methods to synthesize piperidine derivatives. This review describes methods that employ stereoselective Mannich reactions to create the core of piperidine alkaloids. Asymmetric induction in the Mannich reaction has been achieved by a range of methods that have been divided into three conceptual approaches: (1) chiral pool‐based (internal asymmetric induction), (2) chiral auxiliary‐based (relayed asymmetric induction) and (3) asymmetric catalysis‐based (external asymmetric induction). Of each approach, we describe the reaction mechanism and rationalize the stereochemical outcome of the Mannich products.

STUDY OF ALKALOIDS FROM THE SPECIES Mahonia bealei (FORT.) CARR. INTRODUCED IN GEORGIA

The aim of the work was to study the introduced plant on the Black Sea coast of Adjara Mahonia bealei (Fort.) Carr. for the content of alkaloids. A comparative analysis of the quantitative yield of the total amounts of alkaloids isolated from the aerial organs of M. bealei, collected in the phase of active flowering, showed the advantage of the amount obtained from flowers - 2.48%. Based on the results of the HPLC analysis, it was concluded not only about the percentage of the main protoberberine and aporphine alkaloids, but also in which fractions, which alkaloid is dominant (in leaves, three bases dominate at once: berberine (27%), jatrorrhizine (23%), magnoflorin (18%), in branches and flowers - dominated by one base - berberine (50%) and palmatin (57%), respectively, the rest are present in the form of traces). The results of the preliminary investigation suggest that the alkaloid containing substances obtained from the aboveground vegetative organs of the plant demonstrate antioxidant and anti-inflammatory activities.

Phytochemicals, Elemental and Proximate analyses of Piper Guineense Leaves

Piper guineense leaves were studied for their phytochemical, proximate, and mineral content. Standard methods, such as elemental determination with an atomic absorption spectrophotometer and Flame Photometry, were used for the analyses. The carbohydrate content, crude fat, crude protein, crude fiber, ash content, and moisture content were 40.60%, 2.00%, 17.55%, 9.55%, 14.00%, and 12.00%, respectively, according to the experimental results. Phytochemical analysis revealed that the leaf samples included a high quantity of alkaloids, flavonoids, reducing sugar, phenols, tannins, quinones, and cardiac glycosides. The mineral compositions of the investigated leaf show the presence of Fe (20.49 ± 0.25 Mg/100g), Zn (5.67 ± 0.10 Mg/100g), Mg (23.03 ± 5.10 Mg/100g), K (12.06 ± 0.10 Mg/100g) and Ca (120.98 ± 10.00 Mg/100g). The presence of essential minerals, phytochemicals such as alkaloids, flavonoids, tannins, and cardiac glycosides, as well as carbohydrate and crude protein, suggests that it might function as a spice, food, preservative, insecticide, herbal medicine, fragrance in the cosmetic industry, and alternative source of medicine.

Comparison of production of bioactive components in Zanthoxylum nitidum taproots from different regions in southern China.

Zanthoxylum nitidum (Roxb.) DC is a traditional Chinese herb from southern China and its 3-4-year old roots are used in medicine. However, there is a scarcity of studies on the differences in the content of different regions of the roots, as well as comprehensive evaluations of Z. nitidum from the main areas of production in China. This study used ultra performance liquid chromatography, triple quadrupole tandem mass spectrometry, HPLC, and Fourier-transform infrared spectroscopy to detect and identify the bioactive components from different parts and eight regions of 4-year-old roots of Z. nitidum. Our results revealed that the types and quantities of compounds extracted were similar in root bark and root wood, although the amount of alkaloids in the former was substantially higher. The contents of four alkaloids in samples from Guangdong were higher than those in Guangxi Province. Meanwhile, hierarchical cluster analysis and principal component analysis showed that the samples from different regions were effectively identified and evaluated based on alkaloids and other bioactive substances. Our findings have significant implications for Z. nitidum harvesting and usage, as well as for origin identification, quality evaluation, and sensible use of Z. nitidum resources.

Phytochemical Screening and Antibacterial Activity of Bark Exudates in Selected Tree Species

Plants have evolved multiple defense mechanisms against microbial pathogens and various types of environmental stress. Qualitative screening of phytochemical analysis from bark exudates of tree species (Cassia siamea, Araucaria, Artocarpus heterophyllus) were analysed. Tannins, alkaloids, steroids, saponins, reducing sugars, flavonoids, phenols, glycosides are present in aqueous and acetone extracts. But proteins and starch are present in acetone extracts of three bark samples. The maximum flavonoid content was observed in bark sample of Artocarpus heterophyllus, followed by Cassia siamea which was par with Araucaria. The highest amount of alkaloid and phenols were seen in Cassia followed by Artocarpus and Artocarpus heterophyllus. The maximum zone of inhibition were observed in aqueous and acetone extract of Cassia siamea by E. coli (20 mm) and Proteus vulgaris (18 mm). This was followed by acetone extract of Araucaria (15 mm) and Artocarpus heterophyllus (12 mm) by Proteus vulgaris. Whereas minimum zone of incubation were noted in aqueous extract of bark samples of Araucaria, Cassia (5.0 mm) and Artocarpus heterophyllus (4.0 mm) by E. coli and Bacillus subtilis. Bacterial antibiotic streptomycin which was used as positive controls were more effective compared to all the plant extracts tested against the bacterial pathogens. The aqueous extract of Cassia and Araucaria and acetone extract of Artocarpus heterophyllus showed the highest scavenging activity (Dark coloration) upon addition of FeCl3 which could be due to the high phenol content.

Qualitative and Quantitative Analysis of Phytochemicals and Anti-microbial Activity of Madhuca bourdillonii (Gamble) Lam.

The aim of the present study was to investigate the qualitative and quantitative analysis of Madhuca bourdillonii extracts and demonstrate its biological activities. The results of phytochemical analysis showed that the leaf water extract consists of more amount of total phenolics and tannins respectively of 7.4 mg of gallic acid/g and 113.28 mg%. Flavonoid content was found to be more in water extract of bark amounting to 40.73 mg of quercetin/g while the acetone extract of leaves showed more amounts of alkaloids accounting to 30.25 mg%. All the extracts of leaves and stems were evaluated for antimicrobial activity against gram-positive, gram-negative bacteria and pathogenic fungi using agar disc diffusion as well as well diffusion assays and subsequently MIC and MBC values were determined. Among all the bacteria tested, S. flexneri was most susceptible in both the assays exhibiting a zone of inhibition of 12.4 mm & 14.2 mm and 12.2 mm & 14.6 mm respectively for water and acetone extracts of bark. The IC50 values were found to be in the range of 4.52 - 31.34 mg/ml for all the tested bacteria. Among the fungal species tested, C. albicans was found to be susceptible with a zone of inhibition of 7.63 mm for bark water extract in disc diffusion assay and 12.36 mm with leaf ethanol extract in well diffusion assay. The IC50 values were found to be 12.37 - 31.65 mg/ml for C. albicans and F. oxysporium. The results show that Madhuca bourdillonii has excellent anti-bacterial properties which might help the development of novel lead drugs for treatment of various diseases.

Anatomical and phytochemical studies and ethnomedicinal uses of Colchicum autumnale L.

Background: In the world, great importance is attached to the intensification of plants. To date, most medicinal plants are only partially used. In case of Colchicum autumnale L. currently mainly the corms are used for the extraction of alkaloids. The purpose of this study was to investigate the intensification of the use of this perspective plant reported from the study area. This article examines the anatomy and phytochemistry of leaf and corm of C. autumnale, which is grown as a medicinal crop in Uzbekistan. Methods: The leaves were fixed in 70% ethanol according to the generally accepted method; transverse and paradermal sections were examined on the fixed material. When studying the anatomical features of the leaf, preparations was formed by manually cutting a transverse section of the leaf were observed by a MOTIC V1 microscope. The slides were stained with glycerin jelly having safranin. Cells and tissues were measured using a micrometer MOB-15. To determine the amount of alkaloids contained in the leaves and in corms, a chemical analysis was carried out in the laboratory of alkaloids of the Institute of Chemistry of Plant Substances. Results: On the transverse section of the stomata of the leaves of Colchicum autumnale anomocytic type, 2-3 rows of parenchyma and palisade cells, the characteristic size of the stomata. The root structure of C. autumnale consists of 4-5 rows of corolla, 4 protoxylems and 1 metaxylem, and the presence of rhomboid calcium oxalate crystals in its parenchyma is a characteristic feature of the species. As a result of studying the chemical composition of the plant in the conditions of the Tashkent region, it was observed that the amount of alkaloids in the aerial part of the colchicum, in the leaves was 0.4% and in the corm 0.14%. Conclusion: The current work sought to resolve taxonomic issues involving species that share the majority of their physical characteristics and to clarify relationships between important taxa by utilizing leaf epidermal characteristics. As a result of chemical analysis, it was revealed that the amount of alkaloids in the leaves of Colchicum autumnale, introduced in the conditions of the Tashkent region (Uzbekistan), is higher than in natural regions. This proves that in the conditions of Uzbekistan it is possible to grow Colchicum and obtain high-quality raw materials. Key words: autumn crocus, meadow saffron, anatomy, phytochemistry, ethnomedicine.

Maternal chemical defenses predict offspring defenses in a dendrobatid poison frog.

Within and among populations, alkaloid defenses of the strawberry poison frog (Oophaga pumilio) vary spatially, temporally, and with life history stage. Natural variation in defense has been implicated as a critical factor in determining the level of protection afforded against predators and pathogens. Oophaga pumilio tadpoles sequester alkaloids from nutritive eggs and are, thus, entirely dependent on their mothers for their defense. However, it remains unclear how tadpole alkaloid composition relates to that of its mother and how variation in maternally provisioned defenses might result in varying levels of protection against predators. Here, we demonstrate that natural variation in the alkaloid composition of a mother frog is reflected as variation in her tadpole's alkaloid composition. Tadpoles, like mother frogs, varied in their alkaloid composition but always contained the identical alkaloids found in their mother. Alkaloid quantity in tadpoles was highly correlated with alkaloid quantity in their mothers. Additionally, alkaloid quantity was the best predictor of tadpole palatability, wherein tadpoles with higher alkaloid quantities were less palatable. Mother frogs with greater quantities of alkaloids are, thus, providing better protection for their offspring by provisioning chemical defenses during one of the most vulnerable periods of life.

INFLUENCE OF SIMULATED DROUGHT AND SALINITY IN THE PRODUCTION OF PHYTOCHEMICALS IN ACALYPHA WILKESIANA

In this study, 3 month old Acalypha wilkesiana plants grown from stem cuttings were exposed to simulated drought and salinity separately to assess the effects of such abiotic factors on the phytochemical production level in this plant. Preliminary study, based on the qualitative analysis, showed the presence of alkaloids, cardial glycosides, flavonoids, saponins, steroids, and tannins in A. wilkesiana leaves. Results of the quantitative analysis showed that plants under drought and salinity stresses produce lower quantity of alkaloids, flavonoids, and tannins while saponin production was increased

Foliar spraying of elicitors in pear trees induced resistance to Cacopsylla bidens

• Elicitors influence the Cacopsylla pyricola population. • Chitosan induced resistance to Cacopsylla pyricola. • Chitosan for IPM of Cacopsylla pyricola. • Activity of detoxifying enzymes in pear psyllid is altered by elicitor application. • Elicitors influence secondary metabolites. The pear psylla, Cacopsylla pyricola is a serious pest of pear worldwide. In this research, the effects of salicylic acid (SA), chitosan, γ-aminobutyric acid (GABA), and Serenade Aso ( Bacillus subtilis QST713) were studied on the induced resistance of pear trees to C. pyricola . The treatments showed a significant difference in terms of population growth of C. pyricola after 7 and 14 days during two years. In 2019, the mean population growth of total life stages of C. pyricola in the studied treatments was significantly lower than control after 7 and 14 days of spraying. In 2020 (7 and 14 days after spraying), the percent decline in the mean population of pear psylla (total life stages) was highest on chitosan treatment (75 and 85 %, respectively) and the lowest on control (30 and 48 %, respectively). GC-MS analysis revealed the range of chemicals in the pear leaves under different treatments. Based on the results, 23 compounds were identified, including 9 alkaloids, 6 flavonoids, 4 polyphenols, 3 terpenoids, and one glycoside. In all treatments except Serenade, the amounts of alkaloids increased compared to the control. Furthermore, the activity of catalase and glutathione S- transferase enzymes in C. pyricola under chitosan treatment was significantly higher than others; but the activity of peroxidase significantly decreased on chitosan compared to SA and GABA. The lower levels of peroxidase in C. pyricola reared on trees treated with chitosan indicate this insect has not been able to detoxify plant secondary metabolites effectually. In addition, our findings suggested that chitosan on pear trees could act effectively in reducing the C. pyricola population and can be considered in integrated management programs of this pest.

Phytochemical Analysis and In-vitro Antimicrobial Activity of Methanolic Leaves, Root and Stem Extracts of Bryophyllum pinnatum, Cochlospermum tintorium and Erythrina senegalensis

Aim: This Study was design to determine the phytochemical and antimicrobial activities of leaves, roots and stem bark of Cochlospermum tentorium, Bryophyllum pinnatum, and Erythrina senegalensis obtained in Takum Town of Taraba state.
 Methods: The leaves, roots and stem bark of Cochlospermum tentorium, Bryophyllum pinnatum, and Erythrina senegalensis were obtained, dried, ground, and extracted using methanol. The antimicrobial activity of the extract at various concentration was tested using agar well diffusion techniques against three human pathogens by measuring zones of inhibition after incubation 24 hours
 Results: Phytochemical screening revealed the presence of alkaloids, glycoside, flavonoids, phenols, saponins, tannins and steroids. Flavonoids were however absent in the leaf and stem bark of Cochlospermum tintorium, leaf and roots of Bryophyllum pinnatum, and leaf and roots of Erythrina senegalensis. Phenol and tannins were absent in the roots of Bryophyllum pinnatum. The quantitative screening shows that the leaf of Cochlospermum tintorium had the highest amount of glycoside (1.55mg/dl) while the roots had the least amount (0.81mg/dl). Stem bark of Bryophyllum pinnatum showed the highest amount of tannins (7.51mg/dl) while the leaf had the least (3.54mg/dl). Stem bark of Cochlospermum tintorium showed the highest amount of flavonoid (6.54mg/dl) while the leaf had the least (3.66mg/dl). Stem bark of Cochlospermum tintorium recorded the highest amount of phenol (4.37mg/dl) while the roots had the least (1.48mg/dl). The stem bark of Bryophyllum pinnatum recorded the highest amount of alkaloid (1.30mg/dl) while the leaf recorded the least (0.72mg/dl). Stem bark of Bryophyllum pinnatum showed the highest amount of saponins (2.85mg/dl) while the roots showed the least (1.57mg/dg). The methanolic leaf, root and stem bark extract of Cochlospermum tentorium had potent antibacterial activity, while Bryophyllum pinnatum, and Erythrina senegalensis had minimal antibacterial activities against Escherichia coli, Klepsiella pneumonae and staphylococcus aureus.
 Conclusion: This result indicates that the methanolic leaf, root and stem bark extract of Cochlospermum tentorium had antimicrobial activity confirming the folklore claim. Thus, making a strong case for the isolation of novel antimicrobial agent from this plant.

Identification of Photocatalytic Alkaloids from Coptidis Rhizome by an Offline HPLC/CC/SCD Approach.

Natural products continue to be a valuable source of active metabolites; however, researchers of natural products are mostly focused on the biological effects, and their chemical utility has been less explored. Furthermore, low throughput is a bottleneck for classical natural product research. In this work, a new offline HPLC/CC/SCD (high performance liquid chromatography followed by co-crystallization and single crystal diffraction) workflow was developed that greatly expedites the discovery of active compounds from crude natural product extracts. The photoactive total alkaloids of the herbal medicine Coptidis rhizome were firstly separated by HPLC, and the individual peaks were collected. A suitable coformer was screened by adding it to the individual peak solution and observing the precipitation, which was then redissolved and used for co-crystallization. Seven new co-crystals were obtained, and all the single crystals were subjected to X-ray diffraction analysis. The molecular structures of seven alkaloids from milligrams of crude extract were resolved within three days. NDS greatly decreases the required crystallization amounts of alkaloids to the nanoscale and enables rapid stoichiometric inclusion of all the major alkaloids with full occupancy, typically without disorder, affording well-refined structures. It is noteworthy that anomalous scattering by the coformer sulfur atoms enables reliable assignment of absolute configuration of stereogenic centers. Moreover, the identified alkaloids were firstly found to be photocatalysts for the green synthesis of benzimidazoles. This study demonstrates a new and green phytochemical workflow that can greatly accelerate natural product discovery from complex samples.

Comparative Study on Phytochemical Properties and Antifungal Activities of Different Plant Extracts on Infected Fruit of Carica papaya

The comparative studies of phytochemical properties and antifungal activities of different plant extracts; Ageratum conyzoides L., Phyllanthus amarus Schum. & Thonn, Senna alata (L.) Roxb. and Mangifera indica L. on infected fruit of Carica papaya was carried out using standard methods for analysis of all the tested parameters. The test was conducted using the selected plant extracts at five different concentrations (100 - 500mg/ml) against the isolated fungi. Molecular analysis was done to identify the isolated fungi. The results of the qualitative phytochemical screening revealed the presence of alkaloid, tannins, saponins, phenols and flavonoid in all the plant extracts. The quantitative phytochemical screening results showed varying quantities of alkaloids, tannins, saponins, flavonoids and phenols present in the extracts. The quantitative screening showed that A. conyzoides had the highest quantity of the constituents present in its extracts. Four fungal pathogens were isolated from paw-paw fruits and were identified as Rhizopus species, Aspergillus glavus, Aspergillus flavus and Penicillium species. The results of the antimicrobial assay on fungi isolated from infected pawpaw fruits showed that inhibition of fungal growth increased with a corresponding increase in concentration for all the fungal isolates. Penicillium species showed resistance to all the extracts. A. conyzoides showed the highest inhibition from 200mg/ml for the isolates followed by P.amarus. Molecular analysis identified the isolates as Rhizopus arrhizopus, R. delemar, R. oryzae and Aspergillus clavatus. The phylogenetic tree showed that Rhizopus oryzae, R. delemar, R arrhizus are closely related. A. conyzoides and P. amarus can be used to minimize the infection of paw-paw fruit by microbes.

Antihyperlipidemic effect and increased antioxidant enzyme levels of aqueous extracts from Liupao tea and green tea in vivo.

Liupao tea (fermented dark tea) may improve the active function of hyperlipidemia. Utilizing a hyperlipidemia Sprague-Dawley model and UPLC-MS/MS metabolomics, we examined how the effect of Liupao and green tea extracts on hyperlipidemia and antoxidant enzyme levels and compared their constituents. The results showed that the two types of tea could reduce the levels of total cholesterol (TC), total triglyceride, and low-density lipoprotein cholesterol (LDL-C); increase the contents of bile acids and cholesterol in feces; and improve catalase and glutathione peroxidase (GSH-Px) activities. Compared with the model control group, Liupao tea effectively reduced TC and LDL-C levels by 39.53% and 58.55% and increased GSH-Px activity in the liver by 67.07%, which was better than the effect of green tea. A total of 93 compounds were identified from two samples; the amounts of alkaloids and fatty acids increased compared with green tea, and ellagic acid, hypoxanthine, and theophylline with relatively high contents in Liupao tea had a significantly positive correlation with antihyperlipidemic and antioxidant effects. Therefore, Liupao tea had better antihyperlipidemic and antioxidant activities in vivo than green tea, which might be related to the relatively high content of some active substances.

Ethnobotanical and phytochemical study of the medicinal plants used by Kanawan Aytas in Morong, Bataan, Philippines

This study systematically evaluated the medicinal plants used by the Magbukún Ayta Negrito indigenous group in Sitio Kanawan, Morong, Bataan, Philippines through ethnobotanical methods, i.e. Use Value (UV), Fidelity Level (FL), and Informant Consensus Factor (ICF). Semi-structured interviews were used to gather data from 35 informants. All the plants mentioned were collected and identified. The World Health Organization (WHO) use category and the number of use report for each botanical specimen were taken into account as well. The therapeutic uses of 61 plant taxa were documented against 12 categories of ailments. Psidium guajava and Category II (Neoplasms) had the highest UV and ICF values respectively. Five plants with notable ethnobotanical index values were subjected to phytochemical screening for bioactive compounds; all tested positive for sterols, flavonoids, glycosides, and tannins, while Alstonia scholaris (Linn.) R. Br. and Gonocaryum calleryanum (Baill.) Becc. showed abundant amounts of alkaloids. This study highlights the rich culture and traditions of the Ayta Negrito indigenous group although results also indicate that ethnomedicinal knowledge is fading away. Nevertheless, this study opens up various avenues in pharmacological research and pharmacognosy.

Phytochemicals profile and in-vitro antidiabetic potentials of fractionated extracts of Entada Africana and Leptadenia Hastata

Aim: To confirm their use in the management of diabetes and to determine the numerous phytochemicals present that may be connected to the active performance of the plants, the fractionated extracts of Leptadenia hastata and Entada africana were subjected to an in vitro experiment. Material and methods: The plant leaves were dried, pulverized with a Sumeet CM/L 2128945 grinder, the particle size was 45.85 μm and extracted with methanol. The crude extracts were fractionated using a 30×8 cm diameter column and 60g of silica gel 60 F254 grade, using methanol as eluent and fractions were concentrated using a rotary evaporator, the fractionated extracts were run on thin layer Chromatographic plate (TLC) and their retardation factors (RF) were determined. Fractions of similar RF were pulled together and spotted again using TLC plate and the final (RF) were calculated. The crude extracts were quantified for the content of phytochemicals and the phytochemicals present in the fractionated extracts (LH1 and EA2) were identified using HPLC-UV detector. The extracts (LH1 and EA2) were tested for antidiabetic potentials using α -glucosidase and α-amylase enzymes in an in-vitro antidiabetic assay. Results: The yields of the fractionated extracts were 10.0 mg (Leptadenia hastata) and 11.5.0 mg (Entada Africana) and designated as LH1 and EA2, the RF for LH1 and EA2 were 0.75±0.01 and 0.77±0.03 respectively. The maximum amount of alkaloid was found in E. Africana (14.50±0.25 mg/g), while tannin was not found in L. Hastata. In the portion of L. Hastata (LH1), thirteen phytochemicals were discovered and out of these three were alkaloids. Thirteen phytochemicals were found in the E. Africana fraction (EA2), with eight of them being alkaloids and flavonoids. When compared to the usual acarbose, the plants' anti-diabetic properties were superior. EA2 had EC50 of 0.950.17 g/ml (α-amylase) and 0.970.41 g/ml (α-glucosidase), while LH1 had EC50 of 1.00±0.11 g/ml (α-amylase) and 0.90±0.35 g/ml (α-glucosidase). The presence of the detected phytochemicals may be linked to the active qualities of the plants' leaves. Conclusion: The phytochemical profile of fractionated extracts classified as flavonoids and alkaloids are stated to be antidiabetic agents, and this has proved that the researched plants have antidiabetic potential

Callus-Mediated High-Frequency Plant Regeneration, Phytochemical Profiling, Antioxidant Activity and Genetic Stability in Ruta chalepensis L.

Efficient methods for callus induction and the high-frequency plant regeneration of Ruta chalepensis L. were established, and the phytochemical potential and antioxidant activity of a donor plant, ex-vitro-established micropropagated plants, and callus were also studied. Yellowish-green callus was induced with a frequency of 97.8% from internode shoot segments of the donor plant growing in soil in the botanical garden cultured on Murashige and Skoog (MS) medium containing 10 μM 2,4-D (2,4-dichlorophenoxyacetic acid) and 1 μM BA (6-benzyladenine). Adventitious shoots were regenerated from the yellowish-green callus on MS medium containing 5.0 μM (BA) and 1.0 μM 1-naphthaleneacetic acid (NAA), with a regeneration frequency of 98.4% and a maximum of 54.6 shoots with an average length of 4.5 cm after 8 weeks. The regenerated shoots were rooted in a medium containing 1.0 μM IBA (indole-3-butyric acid) and successfully transferred to ex vitro conditions in pots containing normal garden soil, with a 95% survival rate. The amounts of alkaloids, phenolics, flavonoids, tannins, and antioxidant activity of the ex-vitro-established micropropagated plants were higher than in the donor plant and callus. The highest contents of hesperidin and rutin (93.3 and 55.9 µg/mg, respectively) were found in the ex-vitro-established micropropagated plants compared to those obtained from the donor plant (91.4 and 31.0 µg/mg, respectively) and callus (59.1 and 21.6 µg/mg, respectively). The genetic uniformity of the ex-vitro-established micropropagated plants was appraised by the ISSR markers and compared with the donor plant. This is the first report describing the callus-mediated plant regeneration, as well as the production of phenolic compounds and antioxidant activities in R. chalepensis, which might be a potential alternative technique for the mass propagation and synthesis of bioactive compounds such as hesperidin and rutin.

Phytochemical screening and in-vitro evaluation of antimicrobial activity of invasive species Ageratina adenophora collected from Kathmandu valley, Nepal

Antimicrobial activity of invasive alien plant species Ageratina adenophora (Sprengel) R. King & H. Robinson was evaluated against six human pathogenic bacteria. The aqueous (distilled water) and alcoholic (methanol) crude extracts from the leaves of the plant were tested against three gram negative bacteria: Escherichia coli (ATCC 25922), Klebsiella pneumoniaea (ATCC 15380) and Proteus mirabilis (ATCC 49132) and three gram positive bacteria: Enterococcus faecalis (ATCC29212) Bacillus subtilis (ATCC6633) and Staphylococcus aureus (ATCC 25923) using disc diffusion method. Different concentrations of plant extracts (5, 10, 15, 20 and 25%) were applied and diameter of zone of inhibition (ZOI) of bacterial growth were recorded. Plant extract in both solvent exhibited pronounced results against tested bacteria. Methanolic extract of plant exhibited good activity against tested bacteria when compared with aqueous extract. The zone of inhibition of bacterial growth increased with increasing concentrations. Phytochemical screening of plant exhibited alkaloids, saponin, tannin and flavonoids and plant sample contains higher amount of alkaloid. The demonstration of activity against all tested organisms had shown that Ageratina adenophora can be used to produce raw materials/substances for further development of diverse antibiotics with broad spectrum of activity.

The interaction of alkaloids in Coptis chinensis Franch -Tetradium ruticarpum (A. Juss.) T.G. Hartley with hOCT1 and hOCT2

Ethnopharmacological relevanceZuojin Pill, a traditional poly-herbal drug, comprises Coptis chinensis Franch - Tetradium ruticarpum (A. Juss.) T.G. Hartley (6:1). The significant quantity of alkaloids found in the participating herbs is a key aspect of the Zuojin Pill. According to traditional Chinese medicine (TCM), these numerous alkaloidal compounds within Zuojin Pill have various essential therapeutic effects. Aim of the studyThe alkaloids in Tetradium are mainly indole alkaloids, while the alkaloids in Coptis are mostly isoquinoline alkaloids with low bioavailability. Alkaloids and their metabolites are nitrogen-containing compounds or weakly alkaline substances that can be partially ionized under physiological pH conditions. Fortunately, organic cation transporters (OCTs) play a crucial role in the cellular uptake of weakly alkaline compounds. Therefore, we speculated that the alkaloidal compounds might interact with liver cation transporters hOCT1 and kidney cation transporters hOCT2 to alter cell drug disposal. In order to clarify our hypothesis, a series of alkaloids-OCTs interaction experiments were conducted. Materials and methodsHEK293 cells stably expressing hOCT1 and hOCT2 were modeled and evaluated. Afterward, high-content screening (HCS) was conducted to analyze whether the main alkaloids and their metabolites of Coptis - Tetradium were inhibitors of hOCT1 and hOCT2 transporters. Meanwhile, LC-MS/MS was used to investigate whether the alkaloidal compounds were substrates of hOCT1 and hOCT2 transporters. Finally, drug interactions at the cellular level were assessed by LC-MS/MS after co-administration of berberine and rutacorine. ResultsBerberine, jateorhizine, coptisine, epiberberine, columbamine, demethyleneberberine, and berberrubine could significantly inhibit hOCT1 and hOCT2 activity. Isoquinoline alkaloids, including berberine, jateorhizine, coptisine, epiberberine, columbamine, and palmatine, were substrates of hOCT1 and hOCT2, but not the indole alkaloids evodiamine and rutaecarpine. Furthermore, evodiamine at a concentration of 20 μmol/L had a trivial effect on berberine accumulation in HEK293-hOCT2 cells. ConclusionsThese results support the idea that alkaloidal compounds within Coptis and Tetradium have hOCT1 and hOCT2 inhibitory activity or be their substrates, and the increased oral bioavailability of berberine in vivo was closely related to the potential interactions of small molecules in Coptis- Tetradium. Overall, our study provides a framework for investigating the potential interactions of small molecules in Coptis- Tetradium.

Phytochemistry, and Effects of Telfairia occidentalis Leaf Extracts on the Growth and Haematological Properties of Wistar Albino Rats

Standard protocols were used to assess the biochemistry, phytochemistry, and effects of Telfairia occidentalis leaf extracts on the growth and haematological parameters of wistar albino rats. Results revealed ascorbic acid and chlorophyll contents of 158.2+0.7mg/100g and 5.8+0.1mg/100g respectively in fresh leaf samples, while plant extracts contained abundant Tannin, Cardiac glucoside and Flavonoids with moderate amounts of Alkaloid, Saponin and Terpene. Acute toxicity of extracts determined by administering crude ethnaolic extracts intraperitoneally to rats at a dose range of 200mg/kg-1000mg/kg revealed an LD50 of 480 mg/kg. Three fractions (n-hexane, ethylacetate and n-butanol) were obtained and screened for rat growth promoting potentials. Results of weight, water intake and feed consumption revealed a net gain of 57.7g (22%) and 30.4g (11%) in weight; increased water intake of 3.9ml (19.7%) and 1.3ml (17%) and increased feed consumption of 1.5g (12.9%) and 1.3g (11.6%) in rats after 28 days treatment with n-butanol and ethylacetate fractions respectively. Studies of haematological potentials of n-butanol fraction of T. occidentalis leaf extracts showed significant (P<0.05) increase in Red Blood cells level (6.19+0.20x106/L), Haemoglobin (18.36+0.84g/dL) and platelet counts (747.33+2.03x103/mL). When compared to other fractions, the butanol fraction had the highest haematological activity, and additional analysis suggested that the bioactive molecule B2b may be responsible for this. The findings suggest that butanol fraction B2b is a safe and potent hematinic capable of alleviating anemic conditions, and they also confirm the use of T. occidentalis leaf decoction in traditional medicine for the treatment of anemia and other blood-related disorders, suggesting that it could be prescribed as an adjunct to dietary and main anemia therapy.