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Hyperglycemia is a unique characteristic that initiates the pathogenesis of diabetic complications and causes the delay observed in healing of diabetic wound. Sphenocentrum jollyanum, a flowering part of the Menispermaceae family, plays important roles in ethno-medicine and is reputed in folklore as an antihyperglycemic agent and in chronic wound dressing. This study evaluates the effect of Sphenocentrum jollyanum root and leaf extracts on glycemic state and wound closure in a type 2 diabetic rat induced by high fat diet and streptozotocin (STZ). The experimental animals were fed high fat diet for 14 days, and low dose (35 mg/kg) of streptozotocin (STZ) was afterwards administered intraperitoneally. The blood glucose of the animals were measured after 72 h of STZ administration and wound subsequently created. The rats were given S. jollyanum extracts (100 and 200 mg/kg b.w) through oral gavage and also administered topically on the wound area for two weeks. An increased level of glucose, glycated hemoglobin, and lipids, as well as activities of α-amylase, α-glucosidase, and lipase observed in diabetic rats was reduced significantly (P

Background. Tinomiscium petiolare Hook.f. & Thomson is a medicinal species of the family Menispermaceae. This species is currently being intensively exploited for therapeutic purposes. Precise and rapid identification of T. petiolare is critical and essential for the classification, propagation, use and conservation of its genetic resources. In recent years, DNA barcoding has been known to be a fast and sensitive method for identifying species at any stage of development, using short DNA sequences. In this study we have performed the identification of T. petiolare specimens in Vietnam based on the sequence analysis of 4 DNA barcode loci: ITS, matK, rbcL and rpoC.Materials and methods. Total DNA was extracted from leaf samples using DNeasy Plant Mini Kit. PCR amplification of the ITS, matK, rbcL and rpoC regions was carried out on the GeneAmp PCR System 9700 with specific primers. The purified PCR products were sequenced on the ABI 3500 Genetic Analyzer system, using BigDye®Terminator v3.1 Cycle Sequencing Kit. These genetic sequences were analyzed and compared, and a phylogenetic tree was constructed using BioEdit, BLAST, and MEGA 6 programs.Results and conclusion. The success rate of amplification and sequencing was 100% for all 4 DNA barcode loci (ITS, matK, rbcL and rpoC) in the studied specimens. The produced sequence sizes of ITS, matK, rbcL and rpoC in the specimens were 574 bp, 810 bp, 527 bp and 488 bp, respectively. Further, we identified that all studied specimens were genetically related to each other and associated with the same species T. petiolare. Overall, the results of the study generated the most complete DNA barcode database of T. petiolare collected in Vietnam, contributing to the taxonomy and identification of this species.

Cissampelos owariensis is a perennial climber widely used as traditional medicine throughout its distributional range in tropical Africa. This study was aimed at providing a critical review of the pharmacological properties, phytochemistry and medicinal uses of C. owariensis. Documented information on medicinal uses, phytochemical and pharmacological properties of C. owariensis was collected from several online sources such as Scopus, Google Scholar, PubMed, Science Direct and MEDLINE and pre-electronic sources such as book chapters, books, journal articles and scientific publications obtained from the University library. This study showed that the bark, leaves, leaf sap, rhizomes, roots, stems and whole plant parts of C. owariensis are widely used as diuretic, and traditional medicine for ulcers, skin diseases, menstrual problems, gastro-intestinal problems, pregnancy problems, scorpion sting and snakebite. Phytochemical compounds identified from the species include alkaloids, anthraquinones, cardiac glycosides, essential oils, fatty acids, flavonoids, phenols, saponins, steroids, tannins and triterpenoid. Pharmacological research revealed that C. owariensis extracts have antibacterial, anti-mycobacterial, antifungal, antidiarrheal, anti-diabetic, antioxidant, antiproliferative, anti-ulcer, insecticidal, nephroprotective, tocolytic and cytotoxicity activities. There is need for extensive toxicological evaluations of crude extracts and compounds isolated from the species since C. owariensis contains potentially toxic compounds.

Many Bangladeshi medicinal plants have been used to treat Alzheimer’s disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Extracts were prepared using a gentle cold extraction method. In vitro cholinesterase inhibitory effects were measured by Ellman’s method in 96-well microplates. Blumea lacera (Compositae) and Cyclea barbata (Menispermaceae) were found to have the highest acetylcholinesterase inhibitory (IC50, 150 ± 11 and 176 ± 14 µg/mL, respectively) and butyrylcholinesterase inhibitory effect (IC50, 297 ± 13 and 124 ± 2 µg/mL, respectively). Cyclea barbata demonstrated competitive inhibition, where Blumea lacera showed an uncompetitive inhibition mode for acetylcholinesterase. Smilax guianensis (Smilacaceae) and Byttneria pilosa (Malvaceae) were also found to show moderate AChE inhibition (IC50, 205 ± 31 and 221 ± 2 µg/mL, respectively), although no significant BChE inhibitory effect was observed for extracts from these plant species. Among others, Thunbergia grandiflora (Acanthaceae) and Mikania micrantha (Compositae) were found to display noticeable AChE (IC50, 252 ± 22 µg/mL) and BChE (IC50, 314 ± 15 µg/mL) inhibitory effects, respectively. Molecular docking experiment suggested that compounds 5-hydroxy-3,6,7,3′,4′-pentamethoxyflavone (BL4) and kaempferol-3-O-α-L-rhamnopyranosyl-(1⟶6)-β-D-glucopyranoside (BL5) from Blumea lacera bound stably to the binding groove of the AChE and BChE by hydrogen-bond interactions, respectively. Therefore, these compounds could be candidates for cholinesterase inhibitors. The present findings demonstrated that Blumea lacera and Cyclea barbata are interesting objects for further studies aiming at future therapeutics for Alzheimer’s disease.

A new dimeric aporphine alkaloid, biscocsarmine, 2, together with lirioferine, 1, and cocsarmine, 3, were isolated from the ethanol extract of the stems of Triclisia dictyophylla Diels (Menispermaceae) using a preparative pH-zone refining CCC in a single step. The first solvent system family tested for this fractionation was hexane–ethyl acetate–methanol–water (HEMWat) at a series of solvent ratios, and hydrochloric acid and triethylamine at 5 mM as eluter/retainer. None of these HEMWat ratios, however, gave suitable K for the target alkaloids. Ethyl acetate–n-butanol–water (EBuWat) was tested instead and the selected solvent system was composed of ethyl acetate–n-butanol–water 5:5:10 (v/v), where triethylamine (60 mM) was added to the upper organic stationary phase as a retainer and hydrochloric acid (5 mM) to the aqueous mobile phase as an eluter. The chemical structures of the isolated compounds were elucidated based on comprehensive spectroscopic and spectrometric techniques. This is the first report of aporphine alkaloids in this plant species.

The aims of this study are to evaluate phytochemical composition, antimicrobial and antioxidant activities of different solvent-assisted blood fruit pulp extracts. The extracts of blood fruit were prepared with various solvents namely, water, ethyl acetate, methanol and acetone. These extracts were divided into two groups, first group of extract were thermosonicated (treated) and the second group were not exposed to thermosonication (untreated). The sample extracts were then evaluated for their antimicrobial properties against various microorganisms. The results revealed that the antimicrobial activity of thermosonicated ethyl acetate extracts at 12 mg/mL concentration exhibited the highest inhibition zone of 19.4 mm against Staphylococcus aureus. The phenolic content of ethyl acetate extract was found to be the highest as compared to that of other solvent extracts and the values were 1508.08 and 1478.34 mg GAE/100 g for treated and untreated samples, respectively. The treated ethyl acetate extract antioxidative activity by DPPH, ORAC, ABTS, and FRAP assay were 1627.68, 2119.82, 938.11, and 2360.18 µmol TE/g, respectively. The minimum bactericidal concentration (MBC - 1.5 mg/mL) against the selected foodborne pathogens was obtained with thermosonicated ethyl acetate blood fruit extract. In the present study, it was observed that the thermosonicated ethyl acetate extract exhibits maximum antioxidant and antimicrobial activities than any other examined solvent extracts. The major bioactive volatile compounds found in treated ethyl acetate extracts were 2-bromotetradecane, tetracosane, heptadecane, eicosane and palmitic acid. These bioactive compounds can be utilizable for the development of functional, nutraceutical and pharmacological products.

Three new alkaloids (1-3) were isolated from the rhizomes of Menispermum dauricum. The structures and configurations were established by extensive spectroscopic analyses, including 1D, 2D NMR, and ECD.

A rare dimeric sesquiterpenoid (tinosposinoside, 1) and a phenylpropanoid (cordifolioside C, 2), two undescribed metabolites, were isolated from the methanolic extract of the stems of Tinospora sin...

Plant halogenated natural products are rare and harbor various interesting bioactivities, yet the biochemical basis for the involved halogenation chemistry is unknown. While a handful of Fe(II)- and 2-oxoglutarate-dependent halogenases (2ODHs) have been found to catalyze regioselective halogenation of unactivated C–H bonds in bacteria, they remain uncharacterized in the plant kingdom. Here, we report the discovery of dechloroacutumine halogenase (DAH) from Menispermaceae plants known to produce the tetracyclic chloroalkaloid (−)-acutumine. DAH is a 2ODH of plant origin and catalyzes the terminal chlorination step in the biosynthesis of (−)-acutumine. Phylogenetic analyses reveal that DAH evolved independently in Menispermaceae plants and in bacteria, illustrating an exemplary case of parallel evolution in specialized metabolism across domains of life. We show that at the presence of azide anion, DAH also exhibits promiscuous azidation activity against dechloroacutumine. This study opens avenues for expanding plant chemodiversity through halogenation and azidation biochemistry., Halogenated plant natural products are rare and plant halogenation enzymes are thus far unknown. Here Kim et al. identify a dechloroacutumine halogenase from Common Moonseed that catalyzes the final chlorination step in the biosynthesis of acutumine, a chloroalkaloid with selective cytotoxicity to cultured T cells.

Inhibition of acetylcholinesterase (AChE) is a promising strategy for the management of Alzheimer’s disease (AD). Prolyl endopeptidase (PEP) is a post-proline cleaving enzyme that plays an importan...

Context: Cepharanthine (CEP) extracted from the roots of Stephania cepharantha Hayata (Menispermaceae), has a range of therapeutic potential in clinical conditions. Whether it affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. Materials and methods: The effects of CEP (100 μM) on eight human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19 and 2C8) were investigated in vitro using human liver microsomes (HLMs) with specific probe actions and probe substrates. In addition, the enzyme kinetic parameters were calculated. Results: The results showed that the activity of CYP3A4, CYP2E1 and CYP2C9 was inhibited by CEP, with IC50 values of 16.29, 25.62 and 24.57 μM, respectively, but other CYP isoforms were not affected. Enzyme kinetic studies showed that CEP was not only a non-competitive inhibitor of CYP3A4 but also a competitive inhibitor of CYP2E1 and CYP2C9, with Ki values of 8.12, 11.78 and 13.06 μM, respectively. Additionally, CEP is a time-dependent inhibitor for CYP3A4 with KI/Kinact value of 10.84/0.058 min/μM. Discussion and conclusions: The in vitro studies of CEP with CYP isoforms indicate that CEP has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP3A4, CYP2E1 and CYP2C9. Further clinical studies are needed to evaluate the significance of this interaction.

A phytochemical investigation on chemical constituents from the rhizomes of Menispermum dauricum DC. identified eight undescribed dimeric alkaloids with structurally diverse monomeric isoquinoline. Alkaloid structures were elucidated by a combination of spectroscopic data analyses and time-dependent density functional theory (TDDFT) ECD calculation. The isolates were evaluated for inhibitory effect on dopamine D1 receptor and compound 1 exhibited potent D1 receptor antagonistic activity with an IC50 value of 8.4 ± 2.0 μM.

To explore the possible bioactive compounds and to study the antioxidant capacity of Coscinium fenestratum (Goetgh.) Colebr (Menispermaceae), the qualitative and quantitative phytochemical screening for various secondary metabolites were evaluated. Using the GC–MS analysis, a total number of 30 phytochemical compounds were predicted with their retention time, molecular weight, molecular formula, peak area, structure and activities. The most prevailing heterocyclic compound was Bis(2,4,6- triisopropylphenyl) phosphinicazide (6.70%). The antioxidant activity was evaluated by spectrophotometric methods using the reducing power assay and the DPPH· and ABTS·+ scavenging assays. The activity was determined to be increased in all the test samples with the increase in the volume of the extract. C. fenestratum possess a good source of many bioactive compounds that are used to prevent diseases linked with oxidative stress. Keywords: Coscinium fenestratum, Menispermaceae, Biochemical characterization, Antioxidant activity

A new dimeric quaternary protoberberine alkaloid, bispalmatrubine (1), and thirteen known compounds (2-14) were purified from the tubers of Tinospora dentata. Their structures were determined by spectroscopic and spectrometric analytical methods. Among the isolates, eight compounds were examined for their in vitro anti-inflammatory potential and several tested alkaloids displayed moderate inhibitory effects of N-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release.

Four undescribed bisbenzylisoquinoline alkaloids, designated as Stephtetrandrine A-D, were isolated from the roots of Stephania tetrandra. Their structures were elucidated by IR, HRESIMS, ECD spectra, 1 D and 2 D NMR spectra and comparison with the literature data. Additional five known compounds (limacine, tetrandrine, N-trans-Feruloyltyramine, 2′-N-chloromethyltetrandrine, 2,2'-N-N-dichloromethyltetrandrine) were also isolated. N-trans-Feruloyltyramine was isolated from Stephania tetrandra for the first time. The isolated compounds were tested for monoamine oxidase, acetylcholinesterase, phosphoinositide 3-kinase α and human hepatoma cell HepG2 inhibitory activities. Stephtetrandrine C showed obvious inhibitory effect on human hepatoma HepG2, with IC50 value of 16.2 μM. Limacine and 2′-N-chloromethyltetrandrine showed moderate monoamine oxidase inhibitory effect with the IC50 values of 37.7 and 29.2 μM, respectively.

Natural products obtained from species of the genusAbuta(Menispermaceae) are known as ethnobotanicals that are attracting increasing attention due to a wide range of their pharmacological properties. In this study, the alkaloids stepharine and 5-N-methylmaytenine were first isolated from branches ofAbuta panurensisEichler, an endemic species from the Amazonian rainforest. Structure of the compounds was elucidated by a combination of 1D and 2D NMR spectroscopic and MS and HRMS spectrometric techniques. Interaction of the above-mentioned alkaloids with acetylcholinesterase enzyme and interleukins IL-6 and IL-8 was investigatedin silicoby molecular docking. The molecules under investigation were able to bind effectively with the active sites of the AChE enzyme, IL-6, and IL-8 showing affinity towards the proteins. Along with the theoretical study, acetylcholinesterase enzyme inhibition, cytotoxic, and immunomodulatory activity of the compounds were assessed byin vitroassays. The data obtainedin silicocorroborate the results of AChE enzyme inhibition, the IC(50)values of 61.24 mu M for stepharine and 19.55 mu M for 5-N-methylmaytenine were found. The compounds showed cytotoxic activity against two tumor cell lines (K562 and U937) with IC(50)values ranging from 11.77 mu M to 28.48 mu M. Thein vitroassays revealed that both alkaloids were non-toxic to Vero and human PBMC cells. As for the immunomodulatory activity, both compounds inhibited the production of IL-6 at similar levels. Stepharine inhibited considerably the production of IL-8 in comparison to 5-N-methylmaytenine, which showed a dose dependent action (inhibitory at the IC(50)dose, and stimulatory at the twofold IC(50)one). Such a behavior may possibly be explained by different binding modes of the alkaloids to the interleukin structural fragments. Occurrence of the polyamine alkaloid 5-N-methylmaytenine was reported for the first time for the Menispermaceae family, as well as the presence of stepharine inA.panurensis.

Fangchi Radix is derived from Aristolochiaceae or Menispermaceae plants and contains a series of biologically active alkaloids. Fifteen alkaloids in Fangchi crude extracts, including acutumidine (1), magnoflorine (2), stepharine (3), sinomenine (4), acutumine (5), cyclanoline (6), fangchinoline (7), berbamine (8), tetrandrine (9), isotetrandrine (10), trilobine (11), aristolochic acid Π (12), aristolochic acid Ι (13), aristololactam (14) and isotrilobine (15), were separated completely by high-performance liquid chromatography (HPLC) within 60 min. UV detection at 254 nm with a linear gradient elution consisting of 20 mM CH3COONH4 (pH 4.81) and H2O-CH3CN was found to be the most efficient eluent for the LC and LC-MS separations. The structures of the compounds corresponding to the peaks in the LC chromatogram were identified by LC-MS. A total of 32 commercial samples of Fangchi Radix from Sinomenium acutumn, Stephania tetrandra, Aristolochia fangchi and Cocculus trilobus were collected from herbal markets in Taiwan, Japan and China. The contents (peak-area ratios) and structures of the fifteen constituents in these samples were readily determined by the proposed methods and the results could be used to estimate the origin and quality of an herbal drug.

Magnoflorine is an aporphine alkaloid present in plant species belonging to the Berberidaceae, Magnoliaceae, Menispermaceae, or Papaveraceae botanical families. The interest of magnoflorine has increased recently due to its multiplicity of pharmacological properties. The aim of this study was the analysis of combined anti-proliferative effect of magnoflorine and cisplatin and the assessment of drug&ndash, drug pharmacological interaction between these agents using isobolographic method in MDA-MB-468 human breast, NCIH1299 lung, TE671 rhabdomyosarcoma, or T98G glioblastoma cancer cell lines. Magnoflorine in combination with cisplatin at a fixed ratio of 1:1 augmented their anticancer action and yielded synergistic or additive pharmacological interactions by means of isobolographic method, therefore combined therapy using these two active agents can be a promising chemotherapy regimen in the treatment of some types of breast, lung, rhabdomyosarcoma, and glioblastoma cancers.

The hepatotoxic potential of the methanolic extract of the stems of Tinospora crispa and of its furano-diterpenoid–borapetosides B, C, and F–was investigated in normal and health-compromised mice. Health-compromised condition was established by a single intraperitoneal injection of LPS (6 mg/kg). Two different sets of experiments were conducted to evaluate the hepatotoxic potential. A 21-day study where the mice were dosed with the extract of T. crispa (1 gm/kg b. wt./day) or standardized combination of borapetosides B, C and F (500 mg/kg b. wt.) with or without a single dose of LPS (1 gm/kg b. wt./day). In the acute toxicity study, mice were dosed with borapetosides B, C, and F (500 mg/kg b. wt.). Results showed that the ALT levels were normal and liver histopathology unaltered. No conclusive hepatotoxicity was observed in the methanolic extract or pure compounds tested under the given experimental conditions.

Sphenocentrum jollyanum seeds (MeOH extract and n butanol fraction) exhibited urease inhibitory activity (IC50 40.0 ± 0.92, 28.6 ± 0.41). The Ethyl acetate (EtOAc) fraction gave significant antacid activity with an increase in the baseline pH value of 1.2 to 1.61 ± 0.00 and 1.53 ± 0.00 at 50 and 100 mg, respectively, compared to the antacid activity of sodium bicarbonate (1.53 ± 0.00, 1.47 ± 0.00). Five known ecdysteroid compounds isolated from S. jollyanum ethyl acetate and n butanol fractions are Pinnatasterone (1), Polypodine B (2), 20-hydroxyecdysone (3), 20, 26–dihydroxyecdysone, (4) and Atrotosterone A (5). The compounds’ structures were determined using extensive 1D and 2D NMR experiments, and the molecular mass for each of the compounds was confirmed by FAB-MS. Compounds 1–5 were evaluated for their urease inhibitory and antacid activities. Fractions were active in comparison with the standard drug acetohydroxamic acid, and sodium bicarbonate, respectively. Compounds 2, 3 and 1 showed significant urease inhibitory activity (IC50 7.0 ± 0.56, 13.8 ± 0.49 and 14.1 ± 0.59), respectively. The activity of compounds 4 and 5 were moderate compared to that of acetohydroxamic acid (IC50 value 20.3 ± 0.43). Very few compounds have been isolated from this plant despite the numerous biological activities reported for it. The antacid and urease inhibitory activities of this plant and isolated compounds are described for the first time.

A phytochemical investigation of the roots and twigs of Penianthus zenkeri Diels led to the identification of twenty four compounds including one previously undescribed C-28 ecdysteroid (1 ) and previously described phytosteroids (2-5, 20, 22, 23 ), phenolic compounds (6-8, 12 ), diterpenoids (9-11 ), alkaloids (13,14, 18, 19 ), a dipeptide (15 ), ursane type triterpenoids (16-17 ), a carbohydrate (21 ) and a fatty alcohol (24 ). Three semi - synthetic derivatives (5b , 5a, 17a ) obtained from acetylation and acetonidation of rubrosterone (5 ), and ally- lation of ursolic acid (17 ), respectively, are also reported. The chemical structures of the compounds were determined using 1D and 2D NMR spectral data, mass spectrometry and by comparison with the data reported in the literature. The absolute configuration of compound 9 was established using X -Ray and ECD analysis. Different extracts of the twigs and roots, compounds 2 - 4 , 6 - 11 , 15 , and 17 - 21 were evaluated for their anti- bacterial, and cytotoxic activities. The twigs extract showed an antibacterial activity with an MIC of 62.5 mu g/mol against Staphylococcus aureus ATCC 4300, while ursolic acid exhibited a moderate cytotoxicity with an IC50 of 50.9 mu M. The chemotaxonomic relevance of the isolated compounds is discussed.

A number of bisbenzyilisoquinoline alkaloids have been previously isolated from Cissampelos sympodialis (Menispermaceae). The tertiary alkaloid fraction of the rhizomes (TAFrz) was prepared and the major alkaloid warifteine was isolated. Five TAFrz subfractions in addition to warifteine were tested against Dengue virus (DENV). We then used an epithelial (Vero) cell line to evaluate the cytotoxicity and effective concentrations of the samples against DENV. All TAFrz subfractions were active, but subfraction 6 (a mixture of the alkaloids methylwarifteine and warifteine) in particular showed a promising antiviral effect against DENV-2 with an IC50 of 2.00 µg/mL and a selectivity index (SI) of 10.74. Warifteine was the second most active sample and had an IC50 of 8.13 µg/mL and SI = 10.94. The antiviral activity of the samples compared favorably with that of 6-methylmercaptopurine riboside (IC50 = 7.31 µg/mL and SI = 11.8). These results suggest that bisbenzylisoquinoline alkaloids may prove interesting leading antiviral compounds.

Alkaloid berberine is chemically represented as quaternary nitrogen structure, first isolated from Xanthoxylon cava Wall. long ago in the eighteenth century. Currently, this alkaloid is regarded as the most bioactive compound used by pharma industries for research and development of drugs and herbal formulations, and it is extensively employed for hundreds of years in curing numerous infectious diseases and in traditional Ayurvedic and Chinese medicine for curing diarrhoea as a detoxifying agent. Since long time, this compound is detected, isolated, and quantified from different families of plants such as Annonaceae (e.g. Xylopia L.), Berberidaceae (e.g. Berberis L.), Menispermaceae (e.g. Tinospora Miers), Papaveraceae (e.g. Argemone L.), Ranunculaceae (e.g. Coptis Salisb.) and Rutaceae (e.g. Zanthoxylum L.); most of these plants are growing in high-altitude regions of the Himalaya. Reported studies indicate that berberine possesses several pharmacological activities and cure inflammation, diabetes, cancer etc., thereby multiple of mechanisms, as the case may be halting cycle of the cell progression or triggers apoptosis. This chemical constituent shows significant activities such as antimicrobial (bacterial, fungal, protozoans, viral, helminthes), antidiarrhoeal, antitumor and apoptosis, anticarcinogenic, immunomodulatory, antihyperglycaemic, antioxidant, hepatoprotective, cardiovascular and several miscellaneous biological functions associated with human healthcare. This communication reviews and provided various undated information on the botanical sources, berberine extraction techniques and quantification methods, chemistry and several biological functions coupled with different clinical studies undertaken associated with berberine and allied research. This one place data will serve as future baseline data for researchers interested to work more on berberine and pharma industry for drug discovery and medicine development.

Menisdaurin (1), a cyano glucoside, was first isolated in 1978 from Menispermum dauricum (Menispermaceae) and named after the plant. It has been also isolated from several plant sources. The stereochemistry of the aglycone part was first reported as (Z,4R,6S)-enantiomer of (4,6-dihydroxy-2-cyclohexen-1-ylidene)acetonitrile based on the CD spectrum of menisdaurilide (2), the α,β-unsaturated γ-lactone obtained by an acid hydrolysis of menisdaurin. Later, the absolute stereochemistry was revised as (Z,4S,6R) by X-ray crystal analysis of 1 isolated from Saniculiphyllum guangxiens. The aglycone part of menisdaurin (1) has not been obtained from 1, because an acid hydrolysis of 1 gave menisdaurilide (2), and enzymatic hydrolysis with emulsin did not give the aglycone. On the other hand, a compound named coculauril (3) was isolated from Cocculus lauriforius. This compound has the same planner structure corresponding to the aglycone of 1, but the stereochemistry was reported to be (E,4R,6S). Here, we confirmed the absolute stereochemistry of 1 by Mosher's method to be (Z,4S,6R), and prepared the aglycone of 1, i.e., menisdaurigenin (4) by an enzymatic hydrolysis of 1. We also revealed that 4 is a different compound from 3 and unstable in water and MeOH.

Ethnopharmacological relevance The leaves and roots of Cissampelos sympodialis (Menispermaceae) are used by indian tribes and in folk medicine to treat genitourinary infections, inflammation, asthma and gastrointestinal disorders. Material and methods The standardized ethanolic extract (Cs-EtOHE) and alkaloids total fraction (Cs-TAF) obtained from aerial parts of C. sympodialis were evaluated in several models of acute gastric ulcers. The antisecretory and/or neutralizing mechanisms of the gastric acid secretion, cytoprotective, antioxidant and immunoregulatory mechanisms were also evaluated. Results Cs-EtOHE and Cs-TAF presented a reduction in gastric mucosa lesions against ethanol, NSAIDs, hypothermic restraint-stress and gastric juice containment induced ulcer models. This activity is related to alkaloids present in the extract, and involves the participation of sulfhydryl compounds, nitric oxide, KATP channels, prostaglandins, decreased levels of IL-1β and TNF-α and increased levels of GSH and IL-10. Conclusion The data indicate gastroprotective activity, due to the participation of the cytoprotective, antioxidant and immunoregulatory mechanisms.

Objectives:Coscinium fenestratum (Gaertn.) Colebr. (CF, Family: Menispermaceae) is an important endangered woody climber in India. CF contains various major secondary metabolites for the treatment of various disease conditions. The present study aimed to establish the antioxidant and anthelmintic activity of Coscinium fenestratum fruit pulp.Materials and Methods:The dried fruit pulp was subjected to aqueous, methanol, and mixed aqueous and methanol (1:1) solvent extraction followed by phytochemical investigations, estimations of alkaloids, phenolics, flavonoids, antioxidant potentiality (DPPH and hydrogen peroxide scavenging methods), and anthelmintic activity tests were carried out.Results:Preliminary phytochemical screening of CF fruit extracts revealed the presence of alkaloids phenols, flavonoids, tannins, steroids, and resins, which are responsible for biologic properties. The combined aqueous and methanol extract resulted in significant anthelmintic and antioxidant properties in a dose-dependent manner. The DPPH free radical scavenging assay and H2O2 assay exhibited IC50 values of 42.38±0.012 µg/mL and 46.80±0.011 µg/mL, respectively. Thereafter, the anthelmintic activity test was carried out against Pheretima posthuma and Taenia solium with the extract at varying concentrations of 25, 50, 100 and 150 mg/mL and compared with standard albendazole (25 and 50 mg/mL) and saline (0.9%) as a control. All the extracts exhibited concentration-dependent paralytic effect, followed by death on the test organism, but significant activity was observed with the combined methanol and aqueous extract.Conclusion:The study was conducted in order to find possible isolated compounds as a biosources for future novel antioxidants in food and pharmaceutical formulations. Our findings indicate for the first time that the CF fruit pulp has therapeutic values with prominent antioxidant and anthelmintic properties.

Proteins, which behave as random coils in high denaturant concentrations undergo collapse transition similar to polymers on denaturant dilution. We study collapse in the denatured ensemble of single-chain monellin (MNEI) using a coarse-grained protein model and molecular dynamics simulations. The model is validated by quantitatively comparing the computed guanidinium chloride and pH-dependent thermodynamic properties of MNEI folding with the experiments. The computed properties such as the fraction of the protein in the folded state and radius of gyration (Rg) as function of [GuHCl] are in good agreement with the experiments. The folded state of MNEI is destabilized with an increase in pH due to the deprotonation of the residues Glu24 and Cys42. On decreasing [GuHCl], the protein in the unfolded ensemble showed specific compaction. The Rg of the protein decreased steadily with [GuHCl] dilution due to increase in the number of native contacts in all the secondary structural elements present in the protein. MNEI folding kinetics is complex with multiple folding pathways and transiently stable intermediates are populated in these pathways. In strong stabilizing conditions, the protein in the unfolded ensemble showed transition to a more compact unfolded state where Rg decreased by ≈17% due to the formation of specific native contacts in the protein. The intermediate populated in the dominant MNEI folding pathway satisfies the structural features of the dry molten globule inferred from experiments.

During an attempt to discover insulin mimetics, thirteen new triterpenoid saponins (1–13), including three phytolaccagenic acids (1, 2, and 12) and ten serjanic acids (3–11 and 13), as aglycones were isolated from a 70% ethanol extract of leaves and stems from Pericampylus glaucus. The chemical structures of compounds 1–13 were determined through spectroscopic data analysis, including NMR, IR, and HRESIMS. All isolated compounds (1–13) were evaluated using 2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)amino]- d -glucose (2-NBDG) as a fluorescent-tagged glucose probe to determine their stimulatory effects on glucose uptake in differentiated 3 T3-L1 adipocyte cells. Consequently, four compounds (4, 7, 11, and 12) exhibited stimulatory effects on glucose uptake.

Background Moonseed vine (Triclisia gilletii Staner) a member of the Menispermaceae family, has been previously investigated and reported in our laboratory to exhibit antilithiatic potentials against ethane-1,2-diol induced nephrolithiasis. However, the mechanism underlying its action is not clear. Purpose Mechanism of action of aqueous methanolic leaf extact of Triclisia gilletii (TGAMLE 100 mg/kg) in comparison with compounds identified in TGAMLE (Quercetin (20 mg/kg), oleanolic acid (10 mg/kg), stigmasterol (20 mg/kg), and sitosterol (20 mg/kg)) was investigated against ethane-1,2-diol administered rats. Methods The mRNA expression of antioxidant marker genes (nuclear factor erythroid- 2 – related factor- 2 (NRF2) and Heme oxygenase-1 (HO-1)) and crystal binding genes (CD44 and osteopontin (OPN)) were assessed using RT-PCR. Results Ethane-1,2-diol administration down-regulated antioxidant marker genes (NRF2 and HO-1) and up-regulated mRNA expression of CD44 with no significant difference in OPN when compared with control. TGAMLE and its derived compounds significantly activated the NRF2/HO-1 pathway by up-regulating its expression and modify crystal binding molecules (CD44/OPN). Overall, the additive effects of the compounds present in the extract revealed a better efficacy in attenuating NRF2/HO-1 pathway as well as the expression of crystal binding molecules. Conclusion The present study concludes the nephro-protective effect and underlying mechanism of TGAMLE against ethane-1,2-diol exposed rats and suggests that TGAMLE or compounds in TGAMLE could be an alternative agent against kidney stones.

Tinospora cordifolia is commonly known as Gulancha in Bangladesh is belongs to Menispermaceae family and it is also available all over the world. It is widely used as a unique ingredient of various natural medicine and traditionally use for numerous aliment like fever, vomiting, diabetes, jaundice, anaemia, polyuria and skin diseases etc. It has hypoglycemic, antipyretic, anti-allergic, Antineoplastic, anti inflammatory, antioxidant, and immuno modulatory properties. A variety of constituents have been isolated from different parts of Tinospora cordifolia, mainly contains alkaloids like Aporphine alkaloids, clerodane diterpenes, berberine, palmatine, tembertarine, tinosporin, magniflorine, choline, Berberine, Palmatine, Tembetarine, Magnoflorine Choline, Tinosporin etc. and Glycoside like Tinocordiside, Tinocordifolioside, steroids, essential oils, mixture of fatty acids and polysaccharides are found in Gulancha plant. This review presents a detailed survey of the literature on traditional and modern knowledge of Tinospora cordifolia for health benefit.Asian J. Med. Biol. Res. December 2016, 2(4): 508-512

The present study deals with the phytochemical examination of Pachygone ovata (Poer.) Hook.f.& Thoms., an important medicinal plant from menispermaceae family. Leaf and Stem extracts were prepared by using different solvents systems and phytochemical screening was performed using the standard methods given by Harborne. Leaf and stem extracts were prepared from aqueous and organic solvents like petroleum ether, acetone, ethyl acetate and ethanol. Qualitative phytochemical analysis of the petroleum ether, acetone,ethyl acetate, ethanol and aqueous extracts prepared from P. ovata leaf and stem part. Leaf part revealed the presence of alkaloids, flavonoids, glycosides, cardiac glycosides, phenols and tannins. Stem part revealed the presence of alkaloids, flavonoids, glycosides, Resin, Steroids, phenols and tannins. The ethanolic extract showed higher amount of secondary metabolites than the other solvent extracts. This observation becomes important in the context of the therapeutically and drug applications of P. ovata.

Triclisinone (2), a new ochnaflavone derivative, was isolated from the aerial parts of Triclisia gilletii, along with known drypemolundein B (1) and eight other known compounds. The chemical shifts of drypemolundein B (1) have been partially revised based on reinterpretation of NMR spectroscopic data. The eight other secondary metabolites are composed of: (+)-nonacosan-10-ol (3); stigmasterol (4), 3-O-β-D-glucopyranosylsitosterol (5), 3-O-β-D-glucopyranosylstigmasterol (6); oleanic acid (7); myricetin (8), quercetin (9) and 3-methoxyquercetin (10). Their structures were elucidated using IR, MS, NMR 1D and 2D, 1H and 13C and comparison with literature data. Furthermore, compounds 1, 2, 5, 6, 8, 9 and the crude extract were tested against Mycobacterium tuberculosis. Compounds 1, 2, 8 and 9 displayed moderate to very good activity against resistant strain (codified AC 45) of M. tuberculosis with minimum inhibitory concentrations MICs ranging from 3.90 to 62.5 μg/mL.

The present study was aimed to check the mosquitocidal activity of tiliamosine isolated from Tiliacora acuminata (Lam.) Hook. f. & Thom against immature stages of Culex quinquefasciatus. Eggs and larvae of Cx. quinquefasciatus were exposed to different concentrations of tiliamosine – 0.5, 1.0, 1.5 and 2.0 ppm – prepared using DMSO. The compound tiliamosine showed good larvicidal activity with LC50 and LC90 values of 1.13 and 2.85 ppm respectively, against third-instar larvae of Cx. quinquefasciatus at 24 h. In control, the larvae exhibited normal movement. Tiliamosine exhibited 91% ovicidal activity at 2.0 ppm concentration after 120 h post-treatment. Lowest concentration of tiliamosine (0.5 ppm) showed 19% egg mortality. Histopathology study of the compound-treated larvae showed serious damage on the larval midgut cells. The treated larvae showed restless movement which was different from that of the control larvae. The larvae exhibited malformation in development. The compound tiliamosine was harmless to non-target organisms P. reticulata and Dragon fly nymph at tested concentrations. The compound was highly active and inhibited AChE in a concentration-dependent manner. Computational analysis of the tiliamosine had strong interaction with AChE1 of Cx. quinquefasciatus. This report clearly suggests that the isolated compound can be used as an insecticide to control mosquito population and thus prevent the spread of vector-borne diseases.

Fourteen compounds were isolated from the roots, leaves and twigs of Penianthus longifolius Miers (Menispermaceae), including two previously unreported neo-clerodane diterpenoids, penianthin (1), its C-8 epimer (2). In addition, the previously reported O-methylmoschatoline (3), taraxerol (4), taraxerone (5), rubrosterone, (6), panuosterone (7), 22-epi-20-hydroxyecdysone (8), ergosterol peroxide (9), stigmast-5-ene-3,7-dione (10), stigmasterol (11), β-sitosterol (12), stigmasterol glucoside (13) and β-sitosterol glucoside (14) were isolated. The structures of the compounds were determined by means of NMR spectroscopic and mass spectrometric analysis. The absolute configurations of 1 and 2 were determined by circular dichroism analysis. Compounds 1 and 2 were screened against the NCI60 cancer cell panel but showed no significant activity at 10 μM.

Phytochemical investigation of the roots of Cissampelos pareira Linn. led to the isolation of one new pyrrole alkaloid, cissampeline (1), together with ten known alkaloids, (−)-curine (2), (−)-cyclanoline (3), (+)-tetrandrine (4), (+)-obaberine (5), (+)-obamegine (6), (−)-oblongine (7), (+)-homoaromoline (8), (−)-nor-N׳-chondrocurine (9), trans-N-feruloyltyramine (10) and (+)-coclaurine (11). Their structures were elucidated by extensive NMR and MS spectroscopic analyses. Interestingly, compound 1 represents the first example of pyrrole alkaloid found in the genus Cissampelos. Moreover, compounds 5-11 were isolated for the first time from this genus. Among them, compound 6 showed the highest anti-acetylcholinesterase activity with an IC50 value of 3.26 µM, whereas compound 8 displayed the most potent cytotoxicity against human colon cancer (HT29) cells with an IC50 value of 7.89 µM.

Ethnopharmacological relevance Tinospora cordifolia (Willd. Hook. f. & Thomson; family: Menispermaceae), has a long history of use in various traditional medicinal systems including “Ayurveda”. It is reported to possess anticancer, antidiabetic, antimicrobial, antispasmodic, and antiinflammatory activities. T. cordifolia has also been well documented for production of various bioactive metabolites and their antioxidant activity, but the microorganisms associated with it have been least explored for the same properties. Aim of the study Aim of the present study was to evaluate antioxidant and in vivo genoprotective potential of phenolic compounds produced by an endophytic fungus Cladosporium velox TN-9S isolated from T. cordifolia . Materials and methods The isolate of C. velox TN-9S was cultivated in malt extract medium and extracted with ethyl acetate. Total phenol content was determined by Folin Ciocalteu reagent. The antioxidant activity was measured in terms of DPPH and FRAP assay. The in vivo genoprotective activity was assessed using fish Channa punctatus as model. Identification of phenolic compounds was carried out using RP-HPLC. The fungal extract was evaluated for biosafety using Salmonella typhimurium His - strain and CHO cell lines for mutagenicity and cytotoxicity, respectively. Results The total phenolic content in the ethyl acetate extract of the fungus was determined to be 730 μg gallic acid equivalent/mL. The extract evinced significant antioxidant activity with IC 50 value of 22.5 µg/mL in DPPH scavenging assay. The phenolic extract showed good in vivo genoprotective activity against the genetic damage induced in fish C. punctatus after treatment with a non-ionic surfactant 4-nonylphenol. RP-HPLC analysis revealed the presence of peaks corresponding to various phenolic compounds in the extract. Mutagenicity and cytotoxicity results revealed the extract to be nonmutagenic and non cytotoxic in nature. Conclusion The results indicate the potential of an endophytic C. velox isolated from T. cordifolia as a producer of phenolic compounds with antioxidant and genoprotective activities which could be exploited in pharmaceutical industry. The ability of endophytes to produce similar compounds as the host, is also revealed in the present study.

Young leaves of Stephania glabra (ROXB.) Miers. (Menispermaceae) were used to establish callus cultures with the goal of studying their ability to produce the valuable alkaloid stepharine. The establishment of callus cultures from this plant is extremely difficult because primary calli are not viable and must be transferred to a liquid culture medium for subsequent subculturing. All obtained cultures possessed high morphogenic or rhizogenic potential. The methanolic extracts of two examined cell lines were analyzed by HPLC with high-resolution mass spectrometry to determine the alkaloid composition. Eleven alkaloids were detected in both cultures, including stepharine, magnoflorine, menisperine, roemerine, palmatine, corydalmine, N-methylcorydalmine, columbamine, tetrahydropalmatine, jatrorrhizine and tetrandrine. The predominant alkaloid was stepharine, the structure of which was identified through 1H and 13C NMR, UV, HRMS and tandem MS. Quantitative HPLC-UV analysis showed that stepharine was produced at high levels (0.9 % dry cell weight) in the morphogenic callus culture S2-L cultivated in liquid media. To our knowledge, this is the highest level of stepharine production identified in plant cell cultures. The overall production parameters of the culture have remained stable over a long-term cultivation period for 3 years.

Stephania tetrandra and other related species of Menispermaceae form the major source of the bisbenzylisoquinoline alkaloid – tetrandrine. The plant is extensively referenced in the Chinese Pharmacopoeia for its use in the Chinese medicinal system as an analgesic and diuretic agent and also in the treatment of hypertension and various other ailments, including asthma, tuberculosis, dysentery, hyperglycemia, malaria, cancer and fever. Tetrandrine, well-known to act as a calcium channel blocker, has been tested in clinical trials and found effective against silicosis, hypertension, inflammation and lung cancer without any toxicity. Recently, the efficacy of tetrandrine was tested against Mycobaterium tuberculosis , Candida albicans , Plasmodium falciparum and Ebola virus. Tetrandrine’s pharmacological property has been proved to be through its action on different signalling pathways like reactive oxygen species, enhanced autophagic flux, reversal of multi drug resistance, caspase pathway, cell cycle arrest and by modification of calcium channels. The present review summarises current knowledge on the synthesis, distribution, extraction, structural elucidation, pharmacological properties and the mechanism of action of tetrandrine. Future perspectives in the clinical use of tetrandrine as a drug are also considered.

The review collects together some recent information on the identity and pharmacological properties of magnoflorine, a quaternary aporphine alkaloid, that is widely distributed within the representatives of several botanical families like Berberidaceae, Magnoliaceae, Papaveraceae, or Menispermaceae. Several findings published in the scientific publications mention its application in the treatment of a wide spectrum of diseases including inflammatory ones, allergies, hypertension, osteoporosis, bacterial, viral and fungal infections, and some civilization diseases like cancer, obesity, diabetes, dementia, or depression. The pharmacokinetics and perspectives on its introduction to therapeutic strategies will also be discussed.

Natural products isolated from the plant source are considered to be a potent candidate for safe and efficient therapeutic agents since the time immemorial. Numerous bio-potent natural products like Acetylsalicyclic acid, Salicin, Morphine, Digitoxin, Quinine, and Pilocarpine proved to be consecrated in health care sector. Concern to the population exploration, there is inadequate supply of drugs. Last few decades, it is observed that a surge in the herbal drug based dietary supplement in the market. Due to severe unavoidable side effects associated with the allopathic drugs, which led to increase emphasis on isolation of natural products from plant sources. Tinospora cardifolia, belongs to family Menispermaceae has well known for immune booster potency. The preliminary phytochemical screening gives the significance result for presence of alkaloids, terpenoids, glycosides, flavonoids as major phyto-constitution of this plant. Although a lot of phytoconstituents have been isolated from this plant but, still many more phytoconstituents need to be isolated from the polar fractions like n-butanol and water. This research article enlightens the activity targeted isolation of phytoconstituents from the polar fraction of methanolic extract. Different fractions were screened for the antibacterial activity. Considering the zone of inhibition, n-butanolic fraction showed the satisfactory result as compared to other fractions against some selected dental pathogens. So, the n-butanol fraction was considered for phytochemical exploration. The n-butanol fraction festivities a polar compound cordioside and it was characterized with various sophisticated instrumental techniques such as UV-Vis, FTIR, NMR, and Mass Spectroscopy.

Fifty-seven compounds were purified from the stems of Tinospora sinensis, including three new compounds characterized as a lignan (1), a pyrrole alkaloid (11), and a benzenoid (17), respectively. Their structures were elucidated and established by various spectroscopic and spectrometric analytical methods. Among the isolates, fifteen compounds were examined for their anti-inflammatory potential in vitro. The results showed that several compounds displayed moderate inhibition of N-formyl-methionyl-leucyl-phenylalanine/cytochalasin B (fMLP/CB)-induced superoxide anion generation and elastase release.

Ethnopharmacological relevance In the Leticia-Amazonas area, Uitoto indigenous people use a preparation of Curarea toxicofera (Wedd) Barneby & Krukoff (Menispermaceae) alone or combined with prescribed medications to prevent and treat malaria. Aim of study To determine the in vitro and in vivo antiplasmodial activity of traditional preparations of Curarea toxicofera alone and in combination with classical antimalarials. Material and Methods The traditional preparation was evaluated in vitro against P. falciparum FCR3 CQ resistant strain, alone and combined. The preparation was further administered orally alone or combined with chloroquine and artesunate in mice infected with Plasmodium berghei ANKA strain on the four-day antimalarial test model. Results The herbal remedy used alone was able to significantly decrease the parasitemia both in vitro (IC50 7.3 µg/ml) and in vivo (ED50 328 mg/Kg) but it was less active than chloroquine (IC50 0.29 µg/ml in vitro and ED50 2.3 mg/Kg/day in vivo), and than artesunate (IC50 0.002 µg/ml and ED50 3.7 mg/Kg/day). Interestingly it presented synergism with chloroquine in vitro (Combination Index: 0.39) and in vivo; and was additive with artesunate in vitro (Combination Index: 0.94) and in vivo. Conclusion The traditional preparation showed potential as an antimalarial and, when used in combination, does not negatively affect the efficacy of the drugs evaluated. Pre-clinical studies should be conducted with a standardized preparation to confirm its efficacy and safety alone and in combination with chloroquine and artesunate.

Non-alcoholic steatohepatitis (NASH) is one of the aggressive forms of non-alcoholic fatty liver disease (NAFLD) and is a potential risk factor of HCC. This study reports the curative effect of tiliamosine on NASH. Tiliamosine was isolated from Tiliacora racemosa Colebr. (Menispermaceae) and its structure was confirmed by studying the physical and spectroscopic data. The effects of tiliamsoine on lipid accumulation and lipotoxicity were evaluated using palmitate-oleate induced steatosis in HepG2 cells. The in vivo efficacy of tiliamosine was evaluated using HFD fed, DEN induced non-alcoholic steatohepatitis Wistar rats. In HepG2 cells, tiliamosine did not affect the cell viability up to 100 μM concentration and showed GI25 value of 264.28 μM. The treatment with tiliamsoine significantly lowered the ORO concentration by 44.17% and triglyceride accumulation by 69.32% at 50 μM concentration (P

Thirteen undescribed alkaloids (sinotumines A-M), including five oxoisoaporphine, a benzo[h]quinoline, an aporphine, two protoberberine, two hasubanane, and two proaporphine alkaloids, and 50 known analogues were isolated from the 95% aqueous EtOH extract of the stems and rhizomes of Sinomenium acutum. The structures and absolute configurations of the isolates were elucidated on the basis of comprehensive analysis of 1D and 2D NMR, HRMS, single-crystal X-ray diffraction, and comparison of the experimental and calculated electronic circular dichroism (ECD) data. Sinotumine F, a rare benzo[h]quinoline alkaloid, was speculated as an oxidation product of the oxoisoaporphine alkaloid, and its putative biosynthetic pathway is proposed. Sinotumines L and M are the first samples of proaporphine-based heterodimers coupled with 1-heptanone and coniferol alcohol moiety, respectively. The T-cell suppression and NO inhibition effects of the isolates were evaluated.

Introduction The stem of dioecious Tinospora cordifolia (Menispermaceae) is a commonly used traditional Ayurvedic medicine in India having several therapeutic properties. Objective To develop and validate LC-MS methods for the identification and simultaneous quantitation of various secondary metabolites and to study metabolomic variations in the stem of male and female plants. Methods Ethanolic extract of stems were analysed by HPLC/ESI-QTOF-MS/MS for rapid screening of bioactive phytochemicals. High resolution MS and MS/MS in positive ESI mode were used for structural investigation of secondary metabolites. An UPLC/ESI-QqQLIT-MS/MS method in MRM mode was developed and validated for the simultaneous quantitation of five bioactive alkaloids. Results Identification and characterisation of 36 metabolites including alkaloids, sesquiterpenes and phytoecdysteroids were performed using LC-MS and MS/MS techniques. The bioactive alkaloids such as jatrorrhizine, magnoflorine, isocorydine, palmatine and tetrahydropalmatine were successfully quantified in male and female plants. The mean abundances of magnoflorine jatrorrhizine, and oblongine were significantly (P

Ethnopharmacological relevance Tinospora cordifolia (Willd.) Miers ex Hook. f. & Thomas. (Menispermaceae) is one of the most widely used plants in various traditional medicinal systems including “Ayurveda”. The plant is used for the treatment of jaundice, rheumatism, urinary disorder, skin diseases, diabetes and anemia. The phytoconstituents present in the plant belongs to different class of compounds such as alkaloids, diterpenoids lactones, glycosides, steroids, phenol, aliphatic compounds and polysaccharides. Aim of the study The aim of present study was the isolation, structure elucidation, quantification and pharmacological evaluation of secondary metabolites from T. cordifolia for anticancer and immunomodulatory activities. Materials and methods Different extracts and fractions were prepared from the stem of T. cordifolia. Pure molecules were isolated using normal phase chromatography and characterized on the basis of NMR and mass spectroscopic techniques. The anti-cancer and immunomodulatory activities of different extracts, fractions and isolated compounds were evaluated against four different human cancer cell lines, KB (human oral squamous carcinoma), CHOK-1 (hamster ovary), HT-29 (human colon cancer) and SiHa (human cervical cancer) and murine primary cells respectively. A simple, normal phase HPTLC method was also developed for the quantification of three bioactive compounds i.e N-formylannonain (1), 11-hydroxymustakone (5) and yangambin (8) in the stem of T. cordifolia hosted on fifteen different plants. Results Chromatographic purification of different fractions led to the isolation of eight pure molecules i.e N-formylannonain (1), magnoflorine (2), jatrorrhizine (3) palmatine (4), 11-hydroxymustakone (5), cordifolioside A (6), tinocordiside (7) and yangambin (8). All extracts and fractions were active against KB and CHOK-1 cells whereas among the pure molecules palmatine (4) was found to be active against KB and HT-29; tinocordiside (7) against KB and CHOK-1; yangambin (8) against KB cells however N-formylannonain (1) and 11-hydroxymustakone (5), was found active for immunomodulatory activity. HPTLC quantification of three active molecules i.e N-formylannonain (1), 11-hydroxymustakone (5), and yangambin (8) were found in highest quantity in the stem of T. cordifolia hosted on Mangifera indica, however, other two active molecules were not quantified due to their insufficient quantity. Conclusion Eight compounds have been isolated and characterized belonging to different classes. The pharmacological evaluation of extract, fractions and pure molecules revealed the ethnomedicinal value of T. cordifolia for anticancer and immunomodulatory activities.

A primary functional receptor screening assay was performed to examine the effects of methanolic extracts from ten Vietnamese medicinal plants on the human neurokinin-1 receptor expressed from Semliki Forest virus vectors in Chinese hamster ovary cells. Extracts from Piper nigrum, Stephania cambodica and Styphnolobium japonicum were found to exert inhibition on agonist-induced human neurokinin-1 receptor activity. Secondary assays and high performance liquid chromatography of the lead compounds addressed a possible association between pharmacological responses and these chemical compounds. Strong inhibition of human neurokinin-1 receptor was observed for extracts revealing the highest inhibitory potency for rotundine (tetrahydropalmatine) in S. cambodica extracts with IC 50 of 0.88 µM, followed by piperine and capsaicin in P. nigrum extracts with IC 50 values of approximately 2 µM, whereas rutin in S. japonicum extracts failed to inhibit hNK1R up to 100 µM.

A sensitive and selective liquid chromatography-tandem mass spectrometry method has been developed and validated for simultaneous quantitation of 10 alkaloids (dauricine, daurisoline, N-desmethyldauricine, dauricicoline, dauriporphinoline, bianfugecine, dauricoside, stepholidine, acutumine and acutumidine) from Rhizoma Menispermi in rat plasma. After addition of internal standard (verapamil), plasma samples were pretreated by a single-step protein precipitation with acetonitrile. Chromatographic separation was performed on a Waters BEH C18 column with gradient elution using a mobile phase composed of acetonitrile and water (containing 0.1% formic acid) at a flow rate of 0.3 mL/min. The analytes were detected without interference in the multiple reaction monitoring (MRM) mode with positive electrospray ionization. The validated method exhibited good linearity over a wide concentration range (r≥0.9914), and the lower limits of quantification were 0.01-5.0 ng/mL for all the analytes. The intra-day and inter-day precisions (RSD) at three different levels were both less than 13.4% and the accuracies (RE) ranged from -12.8% to 13.5%. The mean extraction recoveries of analytes and IS from rat plasma were all more than 77%. The validated method was successfully applied to a comparative pharmacokinetic study of 10 alkaloids in rat plasma after oral administration of Rhizoma Menispermi extract.

Background Natural supplements and herbal medicines have been attracted to use for managing elevated cholesterol levels. Tiliacora triandra (Colebr.) Diels (TT) or Yanang (in Thai) is commonly used as an ingredient in various types of Thai foods. In this study, we investigated the effect of methanolic TT leaf extract on cholesterol absorption by measuring the uptake and the efflux of cholesterol and cholesterol micellar solubility. In addition, we tested the effect of TT leaf extract on pancreatic lipase activity. Methods The uptake and efflux of cholesterol was determined by quantification of radioactivity in differentiated Caco-2 cells after treatment with radioactive cholesterol. Cholesterol mixed micelles were prepared for cholesterol uptake, efflux and solubility studies. The pancreatic lipase activity was determined using 4-methylumbelliferyl oleate as a substrate. Results Our finding showed that TT extract decreased the uptake of cholesterol by approximately 48% but did not affect the efflux of cholesterol. TT inhibited pancreatic lipase activity with the IC50 at 273.5 μg/mL and also decreased cholesterol micellar solubility. Conclusions These findings suggest that TT leaf extract seems to be a potential candidate as cholesterol-lowering agents.

Stephania venosa (Blume) Spreng., Menispermaceae, has been traditionally used as tonic drug and treatment of various diseases in South East Asian countries. In order to evaluate the quality and standardization of S. venosa roots, the HPLC method for quantification of the content of major components in S. venosa was developed and validated. The chromatographic separation was performed on a Hypersil BDS C18 column using gradient system of 100 mM ammonium acetate in water and methanol with flow rate 1 ml/min. Detection wavelength was set at 210 nm for tetrahydropalmatine, 280 nm for dicentrine and crebanine, and 270 nm for stephanine. The validated method showed good sensitivity, linearity, precision, and accuracy. The suitable solvent that yielded highest alkaloids contents from the matrix was optimized. S. venosa samples collected from various locations were analyzed. The present study provided comprehensive overview of major components in S. venosa. A remarkable variation in the accumulation of alkaloids in each population and the between individual in the same population could be observed. Our results showed the heterogeneity of S. venosa in Thailand which would need a further study for species delimitations. Keywords: Alkaloids, Standardization, Menispermaceae, HPLC, Quantitative analysis