Bioassay-Guided Isolation and Identification of Cytotoxic Compounds from Fruits.

The fruit extract of yielded a total of 19 compounds, including two novel spiro-biflavonoid enantiomers ( and ) and a chalcone derivative (). Their structures were determined through spectroscopic analysis. The enantiomers of the racemic mixture of compound were successfully resolved into (+)- and (-)- using chiral-phase HPLC.

Oral sub-chronic toxicity of fingerroot () rhizome extract formulation in Wistar rats.

Background: (fingerroot) rhizome extract contains two major bioactive components, panduratin A and pinostrobin. In our previous study, we found the anti-inflammatory effects of the fingerroot extract against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in golden Syrian hamsters. In the present study, we evaluated the sub-chronic toxicity of a fingerroot extract formulation over 90 consecutive days of oral administration.

Anti-inflammatory Quinoline Alkaloids from the Roots of .

Sixteen new quinoline alkaloids (-, , , , -, , and ) and 10 known analogs (, , , , -, and -), along with three known cyclopeptide alkaloids (-), were isolated from the roots of . The structures of the new compounds were elucidated by detailed NMR and circular dichroism with computational support and mass spectrometry data interpretation. Anti-inflammatory potential of isolates was evaluated based on inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production and tumor necrosis factor-alpha (TNF-α)-induced nuclear factor kappa B (NF-κB) activity with cell culture models.

Coumarinolignans with Reactive Oxygen Species (ROS) and NF-κB Inhibitory Activities from the Roots of .

Seven new coumarinolignans, walthindicins A-F (, , -, ), along with five known analogs (, -), were isolated from the roots of . The structures of the new compounds are determined by detailed nuclear magnetic resonance (NMR), circular dichroism (CD) with extensive computational support, and mass spectroscopic data interpretation. Compounds were tested for their antioxidant activity in Human Cervical Cancer cells (HeLa cells).

Mechanism of Action of Flavonoids of on the Alleviation of Myocardial Ischemia-Reperfusion Injury.

Bunge is a plant used in traditional Tibetan medicine, with reported anti-inflammatory and antioxidants effects and alleviation of myocardial ischemia reperfusion injury (MIRI). However, the underlying mechanism against MIRI and the phytochemical composition of are vague. One fraction named OFF1 with anti-MIRI activity was obtained from , and the chemical constituents were identified by ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS).

Inhibition of mouse embryonic stem cell proliferation and induction of differentiation by natural products isolated from Rhazya stricta Decne.

Embryonic stem cells provide an ideal system to study various therapies for serious human diseases such as juvenile diabetes, neurodegenerative diseases, heart diseases and cancer. Synthetic or natural compounds that affect cell proliferation and/or differentiation of embryonic stem cells are of great value. Focus of the current project was upon the isolation and evaluation of natural components from a medicinal plant; Rhazya stricta on proliferation/ differentiation potential of embryonic stem cells.

Bioactive Sesquiterpene Lactones Isolated from the Whole Plants of .

Twelve sesquiterpene lactones were isolated from the whole plants of . These included eight new compounds, vercinolides A-H (-), along with four known substances (-). The structures of the new compounds were determined by 1D and 2D NMR experiments and mass spectrometric methods.

Butterfly cluster like lamellar BiOBr/TiO nanocomposite for enhanced sunlight photocatalytic mineralization of aqueous ciprofloxacin.

The present study for the first time reports facile in-situ room temperature synthesis of butterfly cluster like lamellar BiOBr deposited over TiO nanoparticles for photocatalytic breakdown of ciprofloxacin (CIP). The butterfly cluster arrangement of BiOBr resulted in an increase in surface area from 124.6 to 160.

Physalactone and 4β-Hydroxywithanolide E Isolated from Physalis peruviana Inhibit LPS-Induced Expression of COX-2 and iNOS Accompanied by Abatement of Akt and STAT1.

In previous studies, withanolides isolated from Physalis peruviana were found to exhibit anti-inflammatory potential by suppressing nitrite production induced by lipopolysaccharide (LPS) treatment. Currently, we selected two of the most potent compounds, 4β-hydroxywithanolide E (1) and physalactone (2), to examine the underlying mechanism of action. With LPS-stimulated RAW 264.

Siamese Crocodile White Blood Cell Extract Inhibits Cell Proliferation and Promotes Autophagy in Multiple Cancer Cell Lines.

Cancer represents one of the most significant threats to human health on a global scale. Hence, the development of effective cancer prevention strategies, as well as the discovery of novel therapeutic agents against cancer, is urgently required. In light of this challenge, this research aimed to evaluate the effects of several potent bioactive peptides and proteins contained in crocodile white blood cell extract (cWBC) against LU-1, LNCaP, PC-3, MCF-7, and CaCo-2 cancer cell lines.

Bioactive polyprenylated benzophenone derivatives from the fruits extracts of Garcinia xanthochymus.

Two new polycyclic prenylated xanthones (1 and 2) and a new phenylpropanoid glycoside (3), along with seven known compounds (4-10) were isolated from the fruits of Garcinia xanthochymus. The structures were elucidated by 1D- and 2D-NMR, and HRMS experiments. The isolates were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbor an aberrantly active signal transducer and exhibit activation of transcription 3 (STAT3), and compared to normal NIH3T3 mouse fibroblasts.

Differential Effect of Wortmannolone Derivatives on MDA-MB-231 Breast Cancer Cells.

Background/aim: The survival rate of women diagnosed with triple-negative breast-cancer (TNBC) remains low. Hence, this study aimed at the chemical and biological optimization of furanosteroid derivatives for the treatment of this type of malignancy using TNBC cells.

Materials And Methods: Semi-synthetic analogs of wortmannolone () that negatively affected the aberrant pathways in tumor cells were evaluated in hormone-independent breast cancer cells using western blot and cell-cycle analysis.

The Daniel K. Inouye College of Pharmacy Scripts: Poha Berry () with Potential Anti-inflammatory and Cancer Prevention Activities.

The Daniel K. Inouye College of Pharmacy, during a historic event in Spring 2016, graduated the first two students in the Pacific region to earn a PhD in pharmaceutical sciences at the University of Hawai'i at Hilo. The college offers PhD programs in these five disciplines: Cancer Biology, Medicinal Chemistry, Pharmaceutics, Pharmacognosy, and Pharmacology.

PRODUCTION OF ANTIMICROBIAL PEPTIDES BY EPICOCCUM SP. NFW1: AN ENDOPHYTE OF TAXUS FAUNA.

An endophytic fungus NFWI, possessing antimicrobial activity against bacterial and fungal pathogens, was isolated from indigenous Taxus fauna. Phylogenetic analysis coupled with cultural and morphological characteristics revealed that endophyte NFWI closely resembles Epicoccum sp. It showed optimum growth and antimicrobial activity in mineral salt medium TM, incubation temperature 250C, incubation time 15 days and pH 6.

Anti-inflammatory triterpenes from the apical bud of Gardenia sootepensis.

Bioassay-guided fractionation of the dichloromethane extract from the apical bud of Gardenia sootepenesis Hutch. (Rubiaceae) led to the isolation of four new cycloartane triterpenes, sootepins F-I (1-4), along with four known derivatives (5-8). The structures of the new compounds were determined by 1D and 2D NMR experiments and by comparison of the physicochemical data with published values.

Withanolides derived from Physalis peruviana (Poha) with potential anti-inflammatory activity.

Three new withanolides, physaperuvin G (1), with physaperuvins I (2), and J (3), along with seven known derivatives (4-10), were isolated from the aerial parts of Physalis peruviana. The structures of 1-3 were determined by NMR, X-ray diffraction, and mass spectrometry. Compounds 1-10 were evaluated in lipopolysaccharide (LPS)-activated murine macrophage RAW 264.

Anti-inflammatory and Quinone Reductase Inducing Compounds from Fermented Noni (Morinda citrifolia) Juice Exudates.

A new fatty acid ester disaccharide, 2-O-(β-d-glucopyranosyl)-1-O-(2E,4Z,7Z)-deca-2,4,7-trienoyl-β-d-glucopyranose (1), a new ascorbic acid derivative, 2-caffeoyl-3-ketohexulofuranosonic acid γ-lactone (2), and a new iridoid glycoside, 10-dimethoxyfermiloside (3), were isolated along with 13 known compounds (4-16) from fermented noni fruit juice (Morinda citrifolia). The structures of the new compounds, together with 4 and 5, were determined by 1D and 2D NMR experiments, as well as comparison with published values. Compounds 2 and 7 showed moderate inhibitory activities in a TNF-α-induced NF-κB assay, and compounds 4 and 6 exhibited considerable quinone reductase-1 (QR1) inducing effects.

Endophytic fungi associated with Taxus fuana (West Himalayan Yew) of Pakistan: potential bio-resources for cancer chemopreventive agents.

Context: Endophytic fungi, being a prolific source of bioactive secondary metabolites, are of great interest for natural product discovery.

Objective: Isolation and partial characterization of endophytic fungi inhabiting the leaves and woody parts of Taxus fuana Nan Li & R.R.

Induction of cell cycle arrest and apoptosis with downregulation of Hsp90 client proteins and histone modification by 4β-hydroxywithanolide E isolated from Physalis peruviana.

Scope: Physalis peruviana (Solanaceae) is used for culinary and medicinal purposes. We currently report withanolides, isolated from P. peruviana, inhibit the growth of colon cancer monolayer and spheroid cultures.

Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importin α-2 Expression, and Induce Antitumor Effects against Human Glioma.

We report that hirsutinolide series, 6, 7, 10, 11, 20, and 22, and the semisynthetic analogues, 30, 31, 33, and 36, inhibit constitutively active signal transducer and activator of transcription (Stat)3 and malignant glioma phenotype. A position 13 lipophilic ester group is required for activity. Molecular modeling and nuclear magnetic resonance structural analyses reveal direct hirsutinolide:Stat3 binding.

Plants Fagonia cretica L. and Hedera nepalensis K. Koch contain natural compounds with potent dipeptidyl peptidase-4 (DPP-4) inhibitory activity.

Ethnopharmacological Relevance: The two plants investigated here (Fagonia cretica L. and Hedera nepalensis K. Koch) have been previously reported as natural folk medicines for the treatment of diabetes but until now no scientific investigation of potential anti-diabetic effects has been reported.

Assay development for the discovery of semaphorin 3B inducing agents from natural product sources.

Semaphorins are a class of membrane-bound and secreted proteins. They have been found to regulate basic cell functions such as axonal growth cone guidance and recent studies have focused on their effect on tumor progression. Semaphorin 3B (Sema3B) particularly is a secreted protein that has been known to modulate proliferation and apoptosis, processes that are critical for tumor progression and development.

Herbicidin congeners, undecose nucleosides from an organic extract of Streptomyces sp. L-9-10.

Four new undecose nucleosides (herbicidin congeners), three known herbicidins, and 9-(β-d-arabinofuranosyl)hypoxanthine (Ara-H) were isolated from the organic extract of a fermentation culture of Streptomyces sp. L-9-10 using proton NMR-guided fractionation. Their structures were elucidated on the basis of comprehensive 1D and 2D NMR and mass spectrometry analyses.

Bioactive sesquiterpene lactones and other compounds isolated from Vernonia cinerea.

Four new sesquiterpene lactones, 8α-(2'Z-tigloyloxy)-hirsutinolide (1), 8α-(2'Z-tigloyloxy)-hirsutinolide-13-O-acetate (2), 8α-(4-hydroxytigloyloxy)-hirsutinolide (3), and 8α-hydroxy-13-O-tigloyl-hirsutinolide (4), along with seven known derivatives (5-11), three norisoprenoids (12-14), a flavonoid (15), and a linoleic acid derivative (16), were isolated from the chloroform partition of a methanol extract from the combined leaves and stems of Vernonia cinerea. Their structures were established by 1D and 2D NMR, UV, and MS analyses. Compounds 1-16 were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbour aberrantly-active STAT3, compared to normal NIH3T3 mouse fibroblasts that show no evidence of activated STAT3.