PTP1B Inhibitory and Anti-inflammatory Properties of Constituents from Eclipta prostrata L.

The white-flowered leaves of Eclipta prostrata L. together with leaves of Scoparia dulcis and Cynodon dactylon are mixedly boiled in water and given to diabetic patients resulting in the significant improvement in the management of diabetes. However, the active constituents from this plant for antidiabetic and anti-obesity properties are remaining unclear. Thus, this study was to discover anti-diabetes and anti-obesity activities through protein tyrosine phosphatases (PTP)1B inhibitory effects. We found that the fatty acids (23, 24) showed potent PTP1B inhibition with IC50 values of 2.14 and 3.21 µM, respectively. Triterpenoid-glycosides (12-15) also exhibited strong to moderate PTP1B inhibitory effects, with IC50 values ranging from 10.88 to 53.35 µM. Additionally, active compounds were investigated for their PTP1B inhibitory mechanism and docking analysis. On the other hand, the anti-inflammatory activity from our study revealed that compounds (1-4, 7, 8, 10) displayed the significant inhibition nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Especially, compound 9 showed the potent inhibitory effects in LPS-induced NO production on RAW264.7 cell. Therefore, further Western blot analysis was performed to identify the inhibitory expression including heme oxygenase-1 (HO-1) and inhibitor of kappaB (IκB) phosphorylation.

Synthesis and biological evaluation of chalcone derivatives as neuroprotective agents against glutamate-induced HT22 mouse hippocampal neuronal cell death.

Seventeen chalcone analogues were synthesized from 7-methoxy-3,4-dihydronaphthalen1(2H)-one and various aromatic aldehydes under basic conditions and their therapeutic properties were studied in mouse hippocampal cell line HT-22 against neuronal cell death induced by glutamate. From this study, we selected an analogue C01 as a active compound which showed significantly high neuroprotection. This compound inhibited Ca2+ influx and reactive oxygen species (ROS) accumulation inside cells. The glutamate-induced cell death was analyzed by flow cytometry and it showed that C01 significantly reduced apoptotic or dead cell induced by 5 mM glutamate. Western blot analysis indicates that glutamate-mediated activation of MAPKs were inhibited by compound C01 treatment. In addition, the C01enhanced Bcl-2 and decreased Bax, the anti and pro apoptotic proteins respectively. Further analysis showed that, C01 prevented the nuclear translocation of AIF (apoptosis inducing factor) and inhibited neuronal cell death. Taken together, compound C01 treatment resulted in decreased neurotoxicity induced by 5 mM of glutamate. Our finding confirmed that compound C01 has neuro-therapeutic potential against glutamate-mediated neurotoxicity.

Experimental and Computational Study to Reveal the Potential of Non-Polar Constituents from Hizikia fusiformis as Dual Protein Tyrosine Phosphatase 1B and α-Glucosidase Inhibitors.

Hizikia fusiformis (Harvey) Okamura is an edible marine alga that has been widely used in Korea, China, and Japan as a rich source of dietary fiber and essential minerals. In our previous study, we observed that the methanol extract of H. fusiformis and its non-polar fractions showed potent protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase inhibition. Therefore, the aim of the present study was to identify the active ingredient in the methanol extract of H. fusiformis. We isolated a new glycerol fatty acid (13) and 20 known compounds including 9 fatty acids (1-3, 7-12), mixture of 24R and 24S-saringosterol (4), fucosterol (5), mixture of 24R,28R and 24S,28R-epoxy-24-ethylcholesterol (6), cedrusin (14), 1-(4-hydroxy-3-methoxyphenyl)-2-[2-hydroxy -4-(3-hydroxypropyl)phenoxy]-1,3-propanediol (15), benzyl alcohol alloside (16), madhusic acid A (17), glycyrrhizin (18), glycyrrhizin-6'-methyl ester (19), apo-9'-fucoxanthinone (20) and tyramine (21) from the non-polar fraction of H. fusiformis. New glycerol fatty acid 13 was identified as 2-(7'- (2″-hydroxy-3″-((5Z,8Z,11Z)-icosatrienoyloxy)propoxy)-7'-oxoheptanoyl)oxymethylpropenoic acid by spectroscopic analysis using NMR, IR, and HR-ESI-MS. We investigated the effect of the 21 isolated compounds and metabolites (22 and 23) of 18 against the inhibition of PTP1B and α-glucosidase enzymes. All fatty acids showed potent PTP1B inhibition at low concentrations. In particular, new compound 13 and fucosterol epoxide (6) showed noncompetitive inhibitory activity against PTP1B. Metabolites of glycyrrhizin, 22 and 23, exhibited competitive inhibition against PTP1B. These findings suggest that H. fusiformis, a widely consumed seafood, may be effective as a dietary supplement for the management of diabetes through the inhibition of PTP1B.

A new lignan and a new alkaloid, and α-glucosidase inhibitory compounds from the grains of Echinochloa utilis Ohwi & Yabuno.

A new lignan, utilisin (1), and a new alkaloid, echinoutilin (2), together with eleven known compounds 3-13 were isolated from the grains of Echinochloa utilis Ohwi & Yabuno. Their structures were identified through the analysis of spectroscopic data. The absolute configuration of 2 was determined by Mosher's method. These compounds were evaluated for α-glucosidase inhibitory activity. Among them, compounds 2, 3 and 6 exhibited considerable α-glucosidase inhibitory activity with IC50 values of 42.1±1.3, 58.9±3.7, and 40.9±1.1µM, respectively. The results indicate that the grains of E. utilis will be useful in the treatment of diabetes control agents.

PTP1B inhibitors from Selaginella tamariscina (Beauv.) Spring and their kinetic properties and molecular docking simulation.

Diabetes is one of the most popular worldwide diseases, regulated by the defects in insulin secretion, insulin action, or both. The overexpression of protein tyrosine phosphatase 1B (PTP1B) was found to down-regulate the insulin-receptor activation. PTP1B has been known as a strategy for the treatment of diabetes via the regulation of insulin signal transduction pathway. Herein, we investigated the PTP1B inhibitors isolated from natural sources. The chemical investigation of Selaginella tamariscina (Beauv.) Spring revealed seven unsaturated alkynyl phenols 1-7, four new selaginellins T-W 1-4 together with three known compounds 5-7 isolated from the aerial parts. The structures of the isolates were determined by spectroscopic techniques (1D/2D-NMR, MS, and CD). The inhibitory effects of these isolates on the PTP1B enzyme activity were investigated. Among them, compounds 2-7 significantly exhibited the inhibitory effects with the IC50 values ranging from 4.8 to 15.9µM. Compound 1 moderately displayed the inhibitory activity with an IC50 of 57.9µM. Furthermore, active compounds were discovered from their kinetic and molecular docking analysis. The results revealed that compounds 2 and 4-7 were mixed-competitive inhibitors, whereas compound 3 was a non-competitive inhibitor. This data confirm that these compounds exhibited potential inhibitory effect on the PTP1B enzyme activity.

Ellagitannin and flavonoid constituents from Agrimonia pilosa Ledeb. with their protein tyrosine phosphatase and acetylcholinesterase inhibitory activities.

A new ellagitannin, agritannin (1), a new flavone glycoside, agriflavone (2), and another flavone glycoside with spectroscopic data reported for the first time, kaempferol-3-O-[(S)-3-hydroxy-3-methylglutaryl (1→6)]-ß-d-glucoside (3), along with 16 known compounds were isolated from the aerial parts of Agrimonia pilosa Ledeb. These compounds were evaluated for PTP1B inhibitory activity. Among them, compounds 9 and 18 displayed potential inhibitory activity against PTP1B with IC50 values of 7.14±1.75 and 7.73±0.24µM, respectively. In addition, compound 1 showed significant inhibitory effect with an IC50 value of 17.03±0.09µM. Furthermore, these compounds were tested in AChE inhibitory assays. Most of them were found to have moderate inhibitory effects, with IC50 values ranging from 60.20±1.09 to 92.85±1.12µM. Except compounds 3, 8, and 18 were inactive.

Acute Kidney Injury After Percutaneous Coronary Intervention Guided by Intravascular Ultrasound.

Purpose We investigated the impact of intravascular ultrasound guidance on reducing the incidence of contrast-induced acute kidney injury (CI-AKI) in patients undergoing percutaneous coronary intervention (PCI). Methods Ninety-nine patients were enrolled in this prospective cohort who were not randomly assigned to angiography-guided percutaneous coronary intervention or intravascular ultrasound-guided percutaneous coronary intervention. The patients were hospitalized at the Vietnam National Heart Institute - Bach Mai Hospital between 2019 and 2020. Acute kidney injury incidence during hospitalization was the primary endpoint. Results A total of 99 patients were divided into two groups: the intravascular ultrasound-guided group (33 participants) and the angiography-guided group (66 participants). The mean ± SD contrast volume of each group was 95.2 ± 37.1 mL and 133.0 ± 36.0 mL for the ultrasound-guided and angiography-guided groups, with P < 0.0001. Intravascular imaging-guided percutaneous coronary intervention (IVUS-guided PCI) was associated with reduced acute kidney injury incidence during hospitalization: 0.0% vs. 12.12% and P = 0.049. Conclusions Intravascular ultrasound is a safe imaging tool that guides percutaneous coronary intervention and significantly reduces the rate of acute kidney injury compared to angiography alone. Patients who have a high chance of experiencing acute kidney injury benefit from using intravascular ultrasound.

A Massive Renal Infarction Due to Atheroemboli: A Case Report.

The symptoms of acute renal infarction (ARI) caused by atheroemboli are vague, making it rare. Early diagnosis of renal infarction can be made through contrast-enhanced CT of the abdomen. However, diagnosing atheroemboli is more challenging. Kidney biopsy is the most accurate method to determine the cause, but it may not always be available in clinical settings. In cases where a thrombectomy is performed, white substances in thrombus aspiration or the patient's blood can suggest a diagnosis. Intervention is an effective technique, but there is controversy due to a lack of data, particularly in lobular artery infarction. We successfully treated one case using thrombus aspiration, and the specimens suggested atherosclerosis as the cause.

Two new steroidal saponins from the roots of Cordyline fruticosa (L.) A. Chev.

Two new steroidal saponins, 26-O-ß-D-glucopyranosyl-22α-methoxy-5α-furost-25(27)-ene-1ß,3ß,26-triol 1-O-ß-D-glucopyranoside (1), and 26-O-ß-D-glucopyranosyl-22α-methoxy-furosta-5,25(27)-diene-1ß,3ß,26-triol 1-O-α-L-rhamnopyranosyl-(1→2)-ß-D-fucopyranoside (2) were isolated and elucidated from the roots of Cordyline fruticosa (L.) A. Chev. Their structures were established by interpretation of spectroscopic data (1 D and 2 D NMR) and mass spectrometry (HR-ESI-MS).

Autologous blood injection intracoronary artery for treating slow-flow and no-reflow in acute coronary syndrome related to primary pci.

Slow-flow and no-reflow phenomenon are taken to sudden loss of coronary artery flow, typically after stenting or angioplasty in primary PCI. Otherwise conventional therapy, we report a technique, which autologous blood into intracoronary to supply oxygen and break process thrombosis results in successfully management no-reflow in primary PCI in ACS.

Steroidal glycosides from the Vietnamese cultivar Cordyline fruticosa "Fairchild red".

A phytochemical study of Cordyline fruticosa "Fairchild red" (Asparagaceae) from Vietnam, led to the isolation of fourteen steroidal glycosides, including twelve previously undescribed along with two known ones. Ten compounds were obtained by successive solid/liquid chromatographic methods from an aqueous-ethanolic extract of the roots, and four from the aerial parts. Their structures were elucidated mainly by spectroscopic analysis 2D NMR and mass spectroscopy (ESI-MS), as spirostanol glycosides, 5α-spirost-25(27)-ene-1ß,3ß,4α-triol 1-O-ß-D-fucopyranoside, 5α-spirost-(25)27-ene-1ß,3ß,4α-triol 1-O-ß-D-xylopyranoside, 5α-spirost-(25)27-ene-1ß,3ß,4α-triol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-ß-D-fucopyranoside, 5α-spirost-(25)27-ene-1ß,3ß,4α-triol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-(4-O-sulfo)-ß-D-fucopyranoside, 5α-spirost-25(27)-ene-1ß,3ß-diol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-ß-D-fucopyranoside, and 5α-spirost-25(27)-ene-1ß,3ß-diol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-α-L-arabinopyranoside. Furostanol glycosides were also isolated as 26-O-ß-D-glucopyranosyl-5α-furost-(25)27-ene-1ß,3ß,4α,22α,26-pentol 1-O-ß-D-fucopyranoside, 26-O-ß-D-glucopyranosyl-22α-methoxy-5α-furost-(25)27-ene-1ß,3ß,4α,26-tetrol 1-O-ß-D-fucopyranoside, 26-O-ß-D-glucopyranosyl-5α-furost-(25)27-ene-1ß,3ß,22α,26-tetrol 1-O-ß-D-glucopyranoside, 26-O-ß-D-glucopyranosyl-5α-furost-(25)27-ene-1ß,3ß,22α,26-tetrol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-ß-D-glucopyranoside, 26-O-ß-D-glucopyranosyl-5α-furost-(25)27-ene-1ß,3ß,22α,26-tetrol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-ß-D-fucopyranoside, and 26-O-ß-D-glucopyranosyl-22α-methoxy-5α-furost-(25)27-ene-1ß,3ß,26-triol 1-O-α-L-rhamnopyranosyl-(1 â†’ 2)-ß-D-fucopyranoside. All the isolated compounds were further evaluated for their cytotoxicity against 4T1 cell line, from a mouse mammary gland tissue, using MTS method.

Marine and brackish Luticola D.G.Mann (Bacillariophyta) species from the Java Sea and South China Sea coasts with the description of three new species.

In this study, samples were collected from the Java Sea coasts, from the South China Sea in Hainan Island coasts and Quang Yên region and Rú Chá mangrove near Hue in Central Vietnam. In studied samples a total of eight Luticola species have been observed. Three of the taxa studied are described herein as species new to science - Luticolaorientalis sp. nov., L.cribriareolata sp. nov. and L.halongiana sp. nov. Under light microscopy (LM) L.orientalis sp. nov. and L.cribriareolata sp. nov. are similar with rhombic-lanceolate to rhombic/ elliptic-lanceolate to elliptic valve shapes and narrowly rounded apices. Both species can be easily distinguished by stria density (higher density in L.orientalis). Under SEML.cribriareolata is characterized by cribrate areola occlusions, a character thus far observed only in three established species. The remaining species of the whole genus known thus far are characterized by hymenate areola. Similar morphology Luticola species have been observed from tropical mangrove forests from Madagascar but they all can be easily distinguished based on the lack of grooves in the central area. The third species - L.halongiana sp. nov. has rhombic-elliptic to rhombic-lanceolate valves with broadly rounded to slightly protracted apices in larger specimens. This species has a relatively broad central area. Also unique among brackish-water Luticola is the small, rounded stigma positioned almost midway between the valve center and valve margin. In the habitats from which the new species are described we also identified five established Luticola taxa including, L.belawanensis, L.celebesica, L.inserata, L.seposita and L.tropica. For those species we provide detailed SEM characteristics of valve ultrastructure, as well as the range of environmental conditions and geographic distribution within the study area.

Chemical constituents from the roots of Kadsura coccinea with their protein tyrosine phosphatase 1B and acetylcholinesterase inhibitory activities.

Kadsura coccinea (Lem.) A. C. Smith has been used as a tonic, decongestant, and digestive agent. The roots are also employed in traditional medicine to treat chronic enteritis, acute gastritis, duodenal ulcers, rheumatic pain in bone, and traumatic injuries. In the present study, we have described the biological evaluation of constituents from the roots of K. coccinea with PTP1B and AChE inhibitory activities for the first time in literature. A new compound (1), kadcoccilactone T, and 24 known ones (2‒25) were isolated and identified using spectroscopic methods. All the isolates were examined for PTP1B and AChE inhibitory activities. Compounds 4 and 8 expressed strong PTP1B inhibition with IC50 values of 1.57 ± 0.11 and 3.99 ± 1.08 µM, respectively. Apparently, these compounds were further studied for PTP1B enzyme kinetic analysis. The result indicated that compounds 4 and 8 exhibited mixed-type inhibition with the Κi values of 4.97 and 3.26 µM, respectively.

Oligosaccharide and glucose esters from the roots of Polygala arillata.

The root of plant Polygala arillata has been used in the Oriental medicine as a tonic and for the treatment of certain diseases. Our current research on phytochemical profile of the roots of P. arillata led to the isolation of a new oligosaccharide ester (1, polygaloside), a new glucose ester (7, arillatoside), along with five known sucrose esters (2-6). Their structures were elucidated on the basis of extensive chemical and spectroscopic methods as well as comparison with those reported in the literature. The occurence of various oligosaccharide esters in P. arillata including unique compounds plays taxonomical impact and suggests potential in medicinal uses of the title plant.

Cytotoxic glycosides from the roots of Weigela x "Bristol Ruby".

Seven oleanane-type glycosides were extracted and isolated by various chromatographic methods from the roots of Weigela x "Bristol Ruby" (1-7), six previously undescribed (1-6) and a known one (7). Their structures were assigned by spectroscopic analysis mainly 2D NMR and mass spectrometry (ESIMS). Selected triterpenoid glycosides (1-3, 6, 7) displayed a good cytotoxic activity against a mouse colon cancer cell line CT26.

Complete mitogenome of Cerithidea obtusa, the red chut-chut snail from the Can Gio Mangrove in Vietnam.

We sequenced the complete mitogenome of the red chut-chut snail Cerithidea obtusa, from the Can Gio mangrove in Vietnam. The mitogenome is 15,708 bp long. It is colinear with the mitogenomes of other members of the superfamily Cerithioidea, and the maximum-likelihood phylogeny obtained with the cox1, cox2 and cox3 genes of several Caenogastropoda associated all Cerithioidea together inside a strongly supported clade.

Protein tyrosine phosphatase 1B inhibitors from natural sources.

Since PTP1B enzyme was discovered in 1988, it has captured the research community's attention. This landmark discovery has stimulated numerous research studies on a variety of human diseases, including cancer, inflammation, and diabetes. Tremendous progress has been made in finding PTP1B inhibitors and exploring PTP1B regulatory mechanisms. This review investigates for the natural PTP1B inhibitors, and focuses on the common characteristics of the discovered structures and structure-activity relationships. To facilitate understanding, all the natural compounds are here divided into five different classes (fatty acids, phenolics, terpenoids, steroids, and alkaloids), according to their skeletons. These PTP1B inhibitors of scaffold structures could serve as a theoretical basis for new concept drug discovery and design.

The complete mitochondrial DNA of the tropical oyster Crassostrea belcheri from the Can Giò' mangrove in Vietnam.

The complete mitochondrial genome of the oyster Crassostrea belcheri from the Can Giò' mangrove in Vietnam has been sequenced. It consists of a circular DNA molecule of 21020 base pairs (bp), coding for 12 proteins, 20 transfer RNAs, and two ribosomal RNAs. Like the mitogenomes of Crassostrea iredalei and Crassostrea sp. DB1, it contains a non-coding region and two ORFs. The C. belcheri mitogenome provides information that could improve the molecular phylogeny of Asian oysters and be useful to the development of oyster aquaculture in South East Asia.

28-Noroleanane-derived spirocyclic triterpenoids and iridoid glucosides from the roots of Phlomoides umbrosa (Turcz.) Kamelin & Makhm with their cytotoxic effects.

Four undescribed 23,24-O-isopropylidene-19(18 → 17)-abeo-28-noroleanane-derived spirocyclic triterpenoids and an undescribed 28-noroleanane-derived spirocyclic triterpenoid, together with five known 28-noroleanane-derived spirocyclic triterpenoids, were isolated and identified. In addition, three undescribed iridoid glucosides and four known ones were also identified. All the isolates were identified using spectroscopic techniques, and the absolute configurations of 28-noroleanane-derived spirocyclic triterpenoids were determined by CD method for the first time. Additionally, the alkaline hydrolysis method and HPLC analysis were applied to confirm the moieties of the iridoid glucosides. The fraction and isolates were evaluated for cytotoxic activity on cervical cancer (Hela), human promyelocytic leukemia (HL-60), and breast cancer (MCF-7) cell lines. Among them, phlomisu E possessed an aldehyde group showed the most potent cytotoxic effect with IC50 value less than 10 µM.

Flavanonol glucosides from the aerial parts of Agrimonia pilosa Ledeb. and their acetylcholinesterase inhibitory effects.

Two new flavanonol glucoside isomers, (2R,3S)-dihydrokaempferol 3-O-ß-D-glucoside (1) and (2S,3R)-dihydrokaempferol 3-O-ß-D-glucoside (2), were isolated from the aerial parts of Agrimonia pilosa Ledeb., along with eight known flavanonol glucosides (3-10). Their structures were determined on the basis of spectroscopic analysis. In addition, these compounds were evaluated to determine their acetylcholinesterase inhibitory activities. The results indicated that these compounds have moderate inhibitory effects, with IC50 values ranging from 76.59 ± 1.16 to 97.53 ± 1.64 µM, except compounds 1 and 4 were inactive.