Isolation, anticancer potency, and camptothecin-producing ability of endophytic fungi isolated from .

Camptothecin (CPT) is an important alkaloid used for anticancer treatment. It is mainly produced by two endangered and overharvested and plants. Endophytic fungi are promising alternative sources for CPT production.

PQF9 Isolated from Growing in Vietnam as a New Producer of Paclitaxel.

Unlabelled: Endophytic fungi are known as an alternative promising source of anticancer drug, paclitaxel, however fungi inhabiting in medicinal plant and their paclitaxel production have not been reported to date. In the present study, a total of 15 culturable fungi classified into 5 genera, were successfully recovered from collected in Vietnam. Screening fungal dichloromethane extracts for anticancer activity revealed that only PQF9 extract displayed potent inhibitory effects on A549 and MCF7 cancer cell lines with IC values of 33.

Cinchonain Ia Shows Promising Antitumor Effects in Combination with L-Asparaginase-Loaded Nanoliposomes.

Cancer is among the leading causes of death worldwide, with no effective and safe treatment to date. This study is the first to co-conjugate the natural compound cinchonain Ia, which has promising anti-inflammatory activity, and L-asparaginase (ASNase), which has anticancer potential, to manufacture nanoliposomal particles (CALs). The CAL nanoliposomal complex had a mean size of approximately 118.

Stigmastane-type steroid saponins from the leaves of and their -glucosidase and xanthine oxidase inhibitory activities.

Two new vernonioside K () and vernonioside L () and four known Δ stigmastane-type steroidal saponins-vernonioside B2 (), vernoniacum B (), vernonioside B1 (), and vernoamyoside A ()-were isolated from the leaves of . Their structures were determined by comprehensive spectroscopic analysis with one-dimensional nuclear magnetic resonance, two-dimensional nuclear magnetic resonance, and high-resolution mass spectrometry. All isolated compounds (-) were evaluated to determine their inhibitory effects on -glucosidase and xanthine oxidase.

Study on the Anticancer Activity of Prodigiosin from Variants of QBN VTCC 910026.

Prodigiosin (Pg), a secondary metabolism produced by numerous bacterial species, is known as anticancer, antibacterial, antifungal, immunosuppressant, antioxidant, antimalarial properties. Pg has been tested for antitumor activity in many different cancer cell lines but studies in LU-1, KB cell lines, and tumor-bearing mice are still limited. In this study, QBN VTCC 910026 strain (GenBank: KX674054.

Cembranoids from the Vietnamese soft coral .

Using various chromatographic separations, two new cembranoids, ehrenbergols F and G ( and ), along with three known analogs ehrenbergol D (), (+)-isosarcophine () and sinulariol Z () were isolated from the soft coral . The structural elucidation was done by extensive analysis of the 1 D and 2 D NMR, HR-ESI-QTOF-MS as well as CD experiments. In addition, compounds (IC of 38.

Upconversion NaYF:Yb/Er@silica-TPGS Bio-Nano Complexes: Synthesis, Characterization, and Tests for Labeling Cancer Cells.

Fluorescence imaging is an important technique used for early diagnosis and effective treatment of some incurable diseases including cancer. Herein, we report novel NaYF:Yb/Er@silica-TPGS bio-nano complexes for labeling cancer cells. The NaYF:Yb/Er nanoparticles have been successfully synthesized a hydrothermal route, further coated with a silica shell, and functionalized with d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS).

Chemical Constituents of and Anti-Inflammatory, Cytotoxic, and Apoptotic Activities of Eupatoriopicrin on Cancer Stem Cells.

Thunb. of the plant family Asteraceae is a popular traditional herb in Vietnam. However, its chemical constituents as well as bioactive principles have not been investigated yet.

Bioactive compounds from and their anti-inflammatory and cytotoxic activities.

A new compound, physalucoside A (), together with seven withanolides (-) and three flavonoids (-), were isolated from L. (Solanaceae), a medicinal plant native to Vietnam. The chemical structures of these compounds were elucidated by one- and two-dimensional NMR spectra, high-resolution electrospray ionization mass spectrometry analyses, and chemical reactivity.

Antiproliferative and antiinflammatory coxib-combretastatin hybrids suppress cell cycle progression and induce apoptosis of MCF7 breast cancer cells.

In our study, some newly synthesized aryl-substituted pyrazole derivatives mimicking cis-diphenylethylene scaffold of two apoptotic inducing agents celecoxib and combretastatin A-4 were found to have strong antiproliferative as well as antiinflammatory activities. Among these coxib-combretastatin hybrids, two lead compounds 8 and 6c simultaneously inhibited prostaglandin E2 (PGE2) production in LPS-activated murine macrophage RAW 264.7 cells and suppressed cell cycle progression of MCF7 cells at G2/M or G0/G1 phases, but only compound 8 induced apoptosis via caspase-3 activation.

Chemical constituents of Oldenlandia pinifolia and their antiproliferative activities.

This study describes the chemical constituents of Oldenlandia pinifolia (Wall. Ex G. Don) Kuntze (synonym Hedyotis pinifolia Wall.

A new lignan glycoside from the aerial parts and cytotoxic investigation of Uvaria rufa.

Chemical investigation of the aerial parts of Uvaria rufa (Dunal) Blume collected from Vietnam yielded one new lignan glycoside, ufaside (1), along with six known compounds, oxoanolobine (2), ergosta-4,6,8(14),22-tetraen-3-one (3), catechin (4), epicatechin (5), daucosterol (6) and glutin-5-en-3-one (7). Their chemical structures were determined by using NMR, HR-MS spectroscopic analyses and in comparison with the reported data. A cytotoxic analysis of U.

Synthesis and biological evaluation of oseltamivir analogues from shikimic acid.

New oseltamivir analogues were designed and synthesized, starting from shikimic acid. Biological evaluation against three human cancer cell lines (KB, MCF7 and Lu-1) showed that many of them exhibited cytotoxic activity. Azides 5 are more active than the corresponding amines 6.

Toxicity and anticancer effects of an extract from Selaginella tamariscina on a mice model.

The toxicity and antitumour effect of the ethanol extract of Selaginella tamariscina (STE), a plant widely used in folk medicine, were examined in a mice model. In the single-dose acute toxicity test, an oral administration of 10,000 mg kg(-1) STE did not cause any lethality. The sub-acute toxicity study showed that the treatment by 250, 1000 and 3000 mg kg(-1 )day(-1) for 30 continuous days did neither alter the body weights nor the haematological parameters in BALB/c mice.

Preventing release in the acidic environment of the stomach via occlusion in ordered mesoporous silica enhances the absorption of poorly soluble weakly acidic drugs.

This study aimed to assess the pharmaceutical performance of formulations consisting of either indomethacin or glibenclamide and the ordered mesoporous silica material SBA-15. Both compounds were loaded on SBA-15 via solvent impregnation. Adsorption in the SBA-15 mesopores was confirmed using nitrogen physisorption.

Enhanced absorption of the poorly soluble drug fenofibrate by tuning its release rate from ordered mesoporous silica.

The aim of the present study was to evaluate the effect of release rate from ordered mesoporous silica materials on the rate and extent of absorption of the poorly soluble drug fenofibrate. Three ordered mesoporous silica materials with different pore diameter (7.3 nm, 4.

Comparison of the complexation between methylprednisolone and different cyclodextrins in solution by 1H-NMR and molecular modeling studies.

Complexation in solution between methylprednisolone and three different cyclodextrins [2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD), gamma-cyclodextrin (gamma-CD), and 2-hydroxypropyl-gamma-cyclodextrin (HP-gamma-CD)] was studied using phase solubility analysis, one and two-dimensional (1)H-NMR and molecular modeling. Estimates of the complex formation constant (K(1:1)) show that the tendency of methylprednisolone to complex with CDs follows the order: gamma-CD > HP-gamma-CD > HP-beta-CD. The large variation of chemical shifts from protons located around the interior of the hydrophobic cavity (H-3', H-5', and H-6') coupled with minimal variation of shifts from protons located on the outer sphere of gamma-CD (H-1', H-2', and H-4') provided clear evidence of inclusion complexation.

Combined use of ordered mesoporous silica and precipitation inhibitors for improved oral absorption of the poorly soluble weak base itraconazole.

The release of poorly soluble drugs from mesoporous silicates is often associated with the generation of supersaturation, which implies the risk of drug precipitation and reduced availability for absorption. The aim of this study was to enhance the in vivo performance of an ordered mesoporous silicate (SBA-15) by combining it with the precipitation inhibitors hydroxypropylmethylcellulose (HPMC) and hydroxypropylmethylcellulose acetate succinate (HPMCAS). The poorly soluble weak base itraconazole was used as a model compound.

Formulate-ability of ten compounds with different physicochemical profiles in SMEDDS.

In order to gain a better understanding of the reasons of successful self-microemulsifying drug delivery systems (SMEDDS) formulation, ten poorly water-soluble drugs, exhibiting different physicochemical properties, were selected. The solubility of the compounds was determined in various oils (long and medium chain) and surfactants (HLB>12 and HLB<10). The best performing excipients were selected for SMEDDS formulation.

Ordered mesoporous silica material SBA-15: a broad-spectrum formulation platform for poorly soluble drugs.

Encapsulating poorly soluble drugs in mesoporous silicates is an emerging strategy to improve drug dissolution. This study evaluates the applicability of the ordered mesoporous silicate SBA-15 as an excipient to enhance dissolution, for a test series of 10 poorly soluble compounds with a high degree of physicochemical diversity (carbamazepine, cinnarizine, danazol, diazepam, fenofibrate, griseofulvin, indomethacin, ketoconazole, nifedipine, and phenylbutazone). A generic solvent impregnation method was used to load all model compounds.

High-throughput study of phenytoin solid dispersions: formulation using an automated solvent casting method, dissolution testing, and scaling-up.

A high-throughput experimentation method for studying the dissolution of phenytoin, a poorly water soluble drug, was developed and validated. Solid dispersions with 12 excipients (7 polymers and 5 surfactants) were prepared and tested. Each excipient was screened with three drug loadings: 10, 20, and 40% (w/w).

Precision study on capillary electrophoresis methods for metacycline.

A CE method for metacycline (MTC) determination was investigated in an inter-laboratory experiment. Many problems were encountered in this study, most of which were related to the transfer of the method to different CE equipment. The reported problems could be classified into different categories: problems related to the precision, to the parameters in the protocol, and to the MTC peak shape.