Insights on the Nutritional Profiling of Cantaloupe (Cucumis melo L.) via 1-Naphthalene Acetic Acid.

The nutritional components of cantaloupe, including vitamins, minerals, antioxidants, and dietary fiber, contribute to overall health, improved immunity, hydration, and protection against chronic diseases. This study was conducted to investigate the influence of different concentrations (0 (control), 100, 150, and 200 ppm) of 1-naphthalene acetic acid (1-NAA) on the nutritional components of the cantaloupe (Cucumis melo L. Var. Super White Honey). All the studied treatments were applied twice at the 2nd and 4th leaf stages. The applied concentrations of 1-NAA significantly improved the sex expression and fruit yield attributes. Different nutritional components like proximate contents, minerals, vitamins, selected fatty acids, and amino acids were analyzed. The results showed that the maximum moisture content, proteins, carbohydrates, ash, and energy were recorded with 100 ppm. The higher lipids were recorded during the supplementation of 150 ppm. Significantly greater fibers were recorded using 200 ppm. Regarding minerals, 100 ppm was found to be the best as it increased calcium (Ca), magnesium (Mg), potassium (K), sodium (Na), phosphorous (P), manganese (Mn), copper (Cu), iron (Fe), and zinc (Zn). Vitamins were also found to be the maximum with 100 ppm, including vitamin A, vitamin B, vitamin C, vitamin D, vitamin E, and vitamin K. Total selected fatty acids and amino acids were also found significantly greater in the fruits administered 100 ppm.

Three new constituents from the Tujia ethnomedicine Swertia punicea Hemsl.

Three new constituents: 1,5R-dihydroxy-3,8S-dimethoxy-5,6,7,8-tetrahydroxanthone (1), (3S,4R,16S,17R)-3,16,23-trihydroxyoleana-11,13(18)-dien-28-aldehyde-3-O-ß-D-glucopyranoside (2), and new natural product (S)-gentiandiol (3), along with 41 known compounds were isolated from Tujia ethnomedicine Shuihuanglian, namely, the whole plant of Swertia punicea. Structures of all these compounds were established through extensive spectroscopic techniques, namely 1D, 2D-NMR spectroscopy, HRESIMS analysis, and the absolute configuration of the new compounds was discerned by circular dichroism (CD) spectroscopy. Antioxidative effects of these compounds were evaluated by using the DPPH radical scavenging method, compounds 7, 9 and 14 showed antioxidant activities with IC50 values of 68.9, 50.8 and 48.2 µM, respectively.

In-vitro and in-vivo anticandidal activity of Trachyspermum ammi (L.) sprague seeds ethanolic extract and thymol-containing hexanes fraction.

Candida albicans is the causative agent of candidiasis in immunocompromised and diseased individuals. The current study was designed to evaluate the antifungal activity of Trachyspermum ammi (L.) Sprague seeds ethanolic extract and hexanes fraction against Candida albicans, both in-vitro and in-vivo. The minimal inhibitory concentration of hexanes fraction was found to be 225 µg/mL, as compared to the standard drug amphotericin B (200 µg/mL). For the treatment of cutaneous candidiasis in BALB/c mice model, the extract and fraction containing ointment was topically applied on flank of mice at various concentrations, and 90-100% recovery in mice was observed which was better than the standard drug, clotrimazole. The GC/MS analysis of hexanes extract indicated the presence of three major components, including (43.91%), O-cymene (25.53%), and γ-terpinene (22.64%). The results showed that T. ammi possess potential antifungal effect, and can be used for the development of novel antifungal agents after further pre-clinical and clinical trials.

Medicinal plants used in the treatment of tuberculosis - Ethnobotanical and ethnopharmacological approaches.

Tuberculosis is a highly infectious disease declared a global health emergency by the World Health Organization, with approximately one third of the world's population being latently infected with Mycobacterium tuberculosis. Tuberculosis treatment consists in an intensive phase and a continuation phase. Unfortunately, the appearance of multi drug-resistant tuberculosis, mainly due to low adherence to prescribed therapies or inefficient healthcare structures, requires at least 20 months of treatment with second-line, more toxic and less efficient drugs, i.e., capreomycin, kanamycin, amikacin and fluoroquinolones. Therefore, there exists an urgent need for discovery and development of new drugs to reduce the global burden of this disease, including the multi-drug-resistant tuberculosis. To this end, many plant species, as well as marine organisms and fungi have been and continue to be used in various traditional healing systems around the world to treat tuberculosis, thus representing a nearly unlimited source of active ingredients. Besides their antimycobacterial activity, natural products can be useful in adjuvant therapy to improve the efficacy of conventional antimycobacterial therapies, to decrease their adverse effects and to reverse mycobacterial multi-drug resistance due to the genetic plasticity and environmental adaptability of Mycobacterium. However, even if some natural products have still been investigated in preclinical and clinical studies, the validation of their efficacy and safety as antituberculosis agents is far from being reached, and, therefore, according to an evidence-based approach, more high-level randomized clinical trials are urgently needed.

Triterpenoids from stems of Kadsura heteroclita.

In the present work, we reported the triterpenoids isolated from n-butanol fraction of Kadsura heteroclita which is a Tujia ethnomedicine with trivial name "Xuetong". This effort resulted in the isolation of six unpresented triterpenoids xuetongsu A-F (1-6), along with five known triterpenoids (7-11). The structures of the reported compounds were established on the 1D, and 2D NMR and HRESIMS spectra, along with CD spectroscopic analysis. Moreover, the absolute stereochemistry of compound 7 was determined by X-ray diffraction analysis. Antioxidant and cytotoxic activities were evaluated for all isolated compounds, compound 7 shown weak cytotoxic activity against HL-60 with IC50 value of 50.0 µM.

Kadsura coccinea: A rich source of structurally diverse and biologically important compounds.

Kadsura coccinea belongs to medicinally important genus Kadsura from the Schisandraceae family. It has been used in traditional Chinese medicine (TCM) for the treatment of rheumatoid arthritis and gastroenteric disorders. The initial phytochemical work focused on the identification of some structurally novel and diverse natural products, which turned the attention of many researchers towards this plant. Thus far, 202 compounds have been reported in this plant. Lignans and terpenoids were found as the main chemical constituents of this plant. Some of the triterpenoids and sesquiterpenoids with novel structures are of particular interest for natural product researchers. The isolated compounds of this plant have shown different bioactivities including anti-tumor, anti-HIV, anti-inflammatory, nitric oxide (NO) production inhibitory and other pharmacological effects. This review systematically summarizes all the phytochemical and pharmacological work done so far on K. coccinea, and can be used as a reference for future research on this plant.

Two new alkaloids isolated from traditional Chinese medicine Binglang the fruit of Areca catechu.

Binglang, the fruit of Areca catechu L, has a long history as an important Chinese herbal medicine. Two new alkaloids (1 and 2), along with forty-one known compounds (3-43) were isolated from the dried fruit of Areca catechu L. The structures were elucidated on basis of the IR, UV, MS and 1D, 2D NMR spectroscopic data. Compounds 26 and 33 showed weak cytotoxicity against human gastric cancer cell line (BGC-823) with IC50 of 15.91 µM and 20.13 µM, respectively.

RETRACTED: Medicinal plants used in the treatment of tuberculosis - Ethnobotanical and ethnopharmacological approaches.

Tuberculosis is a highly infectious disease declared a global health emergency by the World Health Organization, with approximately one third of the world's population being latently infected with Mycobacterium tuberculosis. Tuberculosis treatment consists in an intensive phase and a continuation phase. Unfortunately, the appearance of multi drug-resistant tuberculosis, mainly due to low adherence to prescribed therapies or inefficient healthcare structures, requires at least 20months of treatment with second-line, more toxic and less efficient drugs, i.e., capreomycin, kanamycin, amikacin and fluoroquinolones. Therefore, there exists an urgent need for discovery and development of new drugs to reduce the global burden of this disease, including the multi-drug-resistant tuberculosis. To this end, many plant species, as well as marine organisms and fungi have been and continue to be used in various traditional healing systems around the world to treat tuberculosis, thus representing a nearly unlimited source of active ingredients. Besides their antimycobacterial activity, natural products can be useful in adjuvant therapy to improve the efficacy of conventional antimycobacterial therapies, to decrease their adverse effects and to reverse mycobacterial multi-drug resistance due to the genetic plasticity and environmental adaptability of Mycobacterium. However, even if some natural products have still been investigated in preclinical and clinical studies, the validation of their efficacy and safety as antituberculosis agents is far from being reached, and, therefore, according to an evidence-based approach, more high-level randomized clinical trials are urgently needed.

Bioactive constituents from Croton sparsiflorus Morong.

Whole plant extracts of Croton sparsiflorus in methanol have shown significant enzyme inhibition and antioxidant activities. Bioassay-guided isolation of chloroform fraction at pH 3 resulted in the identification of crotsparinine (1) and crotsparine (2), while sparsiflorine (3) was purified from the chloroform fraction at pH 9. The structures of the compounds were confirmed through spectral analyses (EI-MS, (1)H and (13)C NMR). The isolated compounds 1-3 exhibited remarkable enzyme inhibition activity with IC50 values 27.01 ± 1.1, 22.26 ± 1.0 and 18.02 ± 1.3 µM in xanthine oxidase and 48.42 ± 1.5, 48.05 ± 1.4 and 7.42 ± 1.0 µM in acetylcholine esterase assays, respectively. These compounds also showed potent radical scavenging and reducing properties in DPPH and FRAP assays, respectively. The present results suggest the validity of the traditional uses of C. sparsiflorus in rheumatism and gout. Furthermore, the isolated noraporphine alkaloids can be useful in the treatment of neurodegenerative diseases.

Analysis and development of structure-fragmentation relationships in withanolides using an electrospray ionization quadropole time-of-flight tandem mass spectrometry hybrid instrument.

Structural elucidation and gas-phase fragmentation of ten withanolides (steroidal lactones) were studied using a positive ion electrospray ionization quadropole time-of-flight mass spectrometry (ESI-QqTOF-MS/MS) hybrid instrument. Withanolides form an important class of plant secondary metabolites, known to possess a variety of biological activities. Withanolides which possess hydroxyl groups at C-4, C-5, C-17, C-20, and C-27, and an epoxy group at C-5/C-6, were evaluated to determine the characteristic fragments and their possible pathways. ESI-QqTOF-MS (positive ion mode) showed the presence of the protonated molecules [M + H](+) . Low-energy collision-induced dissociation tandem mass spectrometric (CID-MS/MS) analysis of the protonated molecule [M + H](+) indicated multiple losses of water and the removal of the C-17-substituted lactone moiety affording the [M + H-Lac](+) product ion as the predominant pathways. However, withanolides containing a hydroxyl group at C-24 of the lactone moiety showed a different fragmentation pathway, which include the loss of steroidal part as a neutral molecule, with highly diagnostic ions at m/z 95 and 67 being generated from the cleavage of lactone moiety. Our results also determined the influence of the presence and positions of hydroxyl and epoxy groups on product ion formation and stability. Moreover, the knowledge of the fragmentation pattern was utilized in rapid identification of withanolides by the LC/MS/MS analysis of a Withania somnifera extract.

Separation of phenylpropanoids and evaluation of their antioxidant activity.

Phenylpropanoids are a group of natural products with a wide range of biological and pharmacological importance. They have been isolated from a large number of plants by utilizing a diverse range of chromatographic techniques. We describe here the utilization of normal, reverse phase, and high pressure liquid column chromatographic techniques for the purification of phenylpropanoids from the crude plant extracts. Most important of them is the recycling reverse phase HPLC effectively utilized to purify the highly oxygenated phenylpropanoids glycosides from the butanolic and water extracts. The antioxidant activity of the different phenylpropanoids is also reported on the basis of DPPH, superoxide anion scavenging and Fe(2+)-chelating assays, along with electron spin resonance (ESR) method.

Free radical scavenging phenylethanoid glycosides from Leucas indica Linn.

A new phenylethanoid glycoside, 2-(3,4-dihydroxyphenyl)-ethyl-O-alpha-L-rhamnopyranosyl-(1 --> 3)-O-alpha-L-rhamnopyranosyl-(1 --> 6)-4-O-E-feruloyl-beta-D-glucopyranoside (3-O-methyl poliu-moside, 1) along with five known phenylethanoid glycosides (2-6) were isolated from the aerial parts of Leucas indica Linn. The structure of compound 1 has been elucidated on the basis of spectral data. Compounds 1-6 exhibited significant antioxidant activity in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical assay method. These compounds were also found to be moderate inhibitors of xanthine oxidase (XO) enzyme.

Leucosceptrine--a novel sesterterpene with prolylendopeptidase inhibitory activity from Leucosceptrum canum.

A novel sesterterpene, leucosceptrine, was isolated from the medicinal plant Leucosceptrum canum from Nepal. The structure was determined by single-crystal X-ray diffraction and spectroscopic techniques. The biosynthesis of leucosceptrine (1) is proposed here. Leucosceptrine (1) exhibited prolylendopeptidase inhibitory activity.

Inhibition of sustained repetitive firing in cultured hippocampal neurons by an aqueous fraction isolated from Delphinium denudatum.

In this report we investigated the effects of the aqueous fraction (AF) isolated from Delphinium denudatum on sustained repetitive firing in cultured neonatal rat hippocampal pyramidal neurons. Blockade of SRF is one of the basic mechanisms of antiepileptic drugs (AED) at the cellular level. The effects of aqueous fraction (0.2-0.6 mg/ml) were compared with the prototype antiepileptic drug, phenytoin (PHT). Using the whole cell current-clamp technique, sustained repetitive firing was elicited in neurons by a depolarizing pulse of 500 ms duration, 0.3 Hz and 0.1-0.6 nA current strength. Similar to phenytoin, aqueous fraction reduced the number of action potentials (AP) per pulse in a concentration-dependent manner until no action potentials were elicited for the remainder of the pulse. There was a corresponding use-dependent reduction in amplitude and Vmax (velocity of upstroke) of action potentials. The Vmax and amplitude of the first action potential was not affected by phenytoin, while aqueous fraction exhibited concentration-dependent reduction. At 0.6 mg/ml aqueous fraction reduced Vmax to 58-63% and amplitude to 16-20% of the control values. The blockade of sustained repetitive firing by aqueous fraction was reversed with hyperpolarization of membrane potential (-65 to -75 mV) while depolarization of membrane potential (-53 to -48 mV) potentiated the block. The results suggest that aqueous fraction blocks sustained repetitive firing in hippocampal neurons in a use-dependent and voltage-dependent manner similar to phenytoin. However, unlike phenytoin, which interacts preferably with the inactive state of the Na+ channel, the compounds present in aqueous fraction apparently also interact with the resting state of the Na+ channels as suggested by dose-dependent reduction of Vmax and amplitude of first AP. We conclude that aqueous fraction contains potent anticonvulsant compounds.

Anti-inflammatory isoflavonoids from the rhizomes of Iris germanica.

The anti-inflammatory activity of nine isoflavonoids 5,7-dihydroxy-3-(3'-hydroxy-4',5'dimethoxy)-8-methoxy-4H-1-benzopyran-4-one 1, 5,7-dihydroxy-3-(3'-hydroxyl-4', 5'-dimethoxy)-6-methoxy-4H-1-benzopyran-4-one 2, 5, 7-dihydroxy-3-(4'-hydroxy)-6-methoxy-4H-1-benzopyrane-4-one 3, 5-hydroxy-3-(4'-hydroxy)-6,7-methylenedioxy-4H-1-benzopyran-4-one 4, 5-hydroxy-3-(4'-methoxy)-6,7-methylenedioxy-4H-1-benzopyran-4-one 5, 5-methoxy-3-(4'-hydroxy)-6,7-methyenedioxy-4H-1-benzopyran-4-one 6, 5,7-dihydroxy-3-(3'-hydroxy-4'-methoxy)-6-methoxy-4H-1-benzopyran-4-one 7, 5,7-dihydroxy-3-(3'-methoxy-4'-hydroxy)-6-methoxy-4H-1-benzopyran-4-one 8, and isopeonol 9 determined by a spectrophotometric assay using the activated human neutrophils. These isoflavonoids were isolated from an important folkloric medicinal plant Irsa (Iris germanica L.), a member of the family Iridaceae. Structures of these compounds were identified by spectral comparison with the reported data and active members of this group adds into the growing number of non-steroidal anti-inflammatory agents.

Anticonvulsant effect of FS-1 subfraction isolated from roots of Delphinim denudatum on hippocampal pyramidal neurons.

The effects were investigated of a partially purified subfraction (FS-1) isolated from Delphinium denudatum on sustained repetitive firing (SRF) of cultured neonatal rat hippocampal pyramidal neurons. The blockade of sustained repetitive firing is one of the basic mechanisms of antiepileptic drugs at the cellular level. Using the whole cell current-clamp technique, sustained repetitive firing was elicited in pyramidal neurons under study by a depolarizing pulse of 500 ms duration, 0.3 Hz and 0.1-0.6 nA current strength. FS-1 (0.01-0.06 mg/mL) reduced the number of action potentials per pulse in a dose-dependent manner until no action potentials were elicited for the remainder of the pulse. There was a corresponding use-dependent reduction in amplitude and Vmax of action potentials. The Vmax of action potential 1 exhibited a dose-dependent reduction. At a dose of 0.06 mg/mL FS-1 reduced Vmax to 29%-38% and amplitude to 16%-20 % of the control values. The blockade of sustained repetitive firing by FS-1 was reversed by hyperpolarization of the membrane potential (-65 to -75 mV) while depolarization of the membrane potential (-53 mV to -48 mV) potentiated the block. The results suggest that FS-1 blocks sustained repetitive firing in hippocampal neurons in a use-dependent and voltage-dependent manner similar to the prototype anticonvulsant drug, phenytoin. However, unlike phenytoin, which binds preferably to the inactive state, the compounds present in FS-1 also interacted with the resting state of the Na+ channels by reducing Vmax of action potential 1. The results indicate that the partially purified FS-1 subfraction of Delphinium denudatum contains a potent anticonvulsant compound.

In vitro inhibition of pentylenetetrazole and bicuculline-induced epileptiform activity in rat hippocampal pyramidal neurons by aqueous fraction isolated from Delphinium denudatum.

Roots of Delphinium denudatum W. are used for the treatment of epilepsy by traditional healers in subcontinent. Aqueous fraction (AF) isolated from D. denudatum has previously shown significant anticonvulsant activity in in vivo and in vitro models of seizures. We investigated anticonvulsant effects of AF on pentylenetetrazole (PTZ) and bicuculline (BIC)-induced epileptiform activity in primary hippocampal neuronal cultures. Electrophysiological studies on single pyramidal neurons were carried out by using whole-cell current clamp technique. Introduction of AF (0.6 mg/ml) in perfusate blocked PTZ (10 mM) and BIC (100 micro M)-induced epileptiform activity comprising of paroxysmal depolarization shifts (PDS). The PDS were elicited again when AF was removed from perfusate. We conclude that AF contains anticonvulsant compounds that possibly interact with GABA(A) receptor to produce blockade of epileptiform activity. Further studies on isolation of compounds from AF may lead to discovery of new class of anticonvulsants.