Highly Cytotoxic Xanthones from Cratoxylum cochinchinense Collected in Myanmar

Eight xanthones and one anthraquinone, together with four common triterpenoids, have been isolated from the barks of Cratoxylum cochinchinense, collected in Myanmar. The structures of the metabolites were elucidated by spectroscopic data analysis and their antiproliferative activities were measured against six human tumor cell lines, by using the MTT assay. Pruniflorone N (1) showed a significant cytotoxicity against all cancer cells with IC50 values in the range 3-9 μM, on average higher than the anticancer drug cisplatin. Instead, compounds 2 and 3 exhibited high antiproliferative activity against some specific cell lines

A Review of Common Medicinal Plants in Chin State, Myanmar:

Promising sources of novel bioactive compounds include plants growing in several third-world countries where the local flora is still largely uninvestigated. A paradigmatic example is represented by medicinal plants growing in Myanmar, especially in Chin State, in northwestern Myanmar. This is one of the least developed areas of the country where the people still use natural remedies derived from a rich biodiversity. This review mainly covers the investigations done on phytochemical constituents and biological activities of 20 medicinal plants, namely Alangium chinense, Anemone obtusiloba, Anneslea fragrans, Antidesma bunius, Croton oblongifolius, Embelia tsjeriam-cottam, Ficus heterophylla, Gaultheria fragrantissima, Hydnocarpus kurzii, Leea macrophylla, Leucas cephalotes, Millingtonia hortensis, Myrica nagi, Olax scandens, Pimpinella heyneana, Pterospermum semisagittatum, Ruellia tuberosa, Smilax zeylanica, Stemona burkillii, and Tadehagi triquetrum, that have long been used in the Chin State for curing various diseases. These plants have been selected on the basis of their medicinal uses not only in Myanmar but also in the related Ayurvedic healing system. Moreover, besides their medicinal importance, most of them grow in the Chin State more abundantly than in other regions of Myanmar. Although the efficacy of some of these plants have been verified scientifically, the chemical constituents and biological activities of most of them still need to be investigated to confirm the claimed therapeutic effects

Sesquiterpene from Myanmar Medicinal Plant (<em>Curcuma comosa</em>)

Curcuma comosa (Zingiberaceae) is widely grown in tropical and subtropical areas of Asia, like Thailand, Indonesia, Malaysia, and Myanmar. In Myanmar, the rhizome of Curcuma comosa is called Sa-nwin-ga, and local people had used it as a traditional medicine for stomach ache, diabetes mellitus, and hypertension. This species produces secondary metabolites of phenolic and nonphenolic groups. Phenolic groups like diarylheptanoids and flavonoids. While nonphenolics are terpenoids, especially sesqui- and monoterpenes. In this chapter, the group of sesquiterpene compounds from Curcuma comosa starts from the isolation technique, followed by the elucidation of the molecular structure, and their activity tests have been discussed

Cytotoxic Carbazole Alkaloid from the Root of Clausena cxcavata on Hela Cell L

In a search for bioactive constituents from Myanmar medicinal plants, a carbazole alkaloid, named 7hydroxy heptaphylline (1) was isolated from the root of Clausena excavata. The structure of isolated compound was elucidated based on spectrophotometric data such as UV-vis, FT-IR, NMR and HRMS data. The cytotoxicity of the isolated compound (1) was evaluated by MTT assay against on HeLa cancer cells. The compound (1) exhibited moderate inhibition activity with IC50 41.4 µg/ml

Phytoconstituents of Genus Micromelum and Their Bioactivity—a Review.

The genus Micromelum belongs to the Rutaceae family. As its rich bioactive constituents its stems, flowers, leaves, and roots have been used in traditional medicine, for the treatment of various diseases from ancient time. Phytochemically, many bioactive compounds, including coumarins, polyoxygenated flavonoids, phenylpropanoic acid derivatives, quinolone alkaloids, and also carbazole alkaloids, have been reported as secondary metabolites of the Micromelum spp. including many new compounds. Therefore, Micromelum spp. are considered potential for drug leads. In this article, we present an overview of secondary metabolites isolated from genus Micromelum and their bioactivities that have been reported between 1982 and 2019

Biological and Pathological Studies of Rosmarinic Acid as an Inhibitor of Hemorrhagic Trimeresurus flavoviridis (habu) Venom

In our previous report, rosmarinic acid (RA) was revealed to be an antidote active compound in Argusia argentea (family: Boraginaceae). The plant is locally used in Okinawa in Japan as an antidote for poisoning from snake venom, Trimeresurus flavoviridis (habu). This article presents mechanistic evidence of RA’s neutralization of the hemorrhagic effects of snake venom. Anti-hemorrhagic activity was assayed by using several kinds of snake venom. Inhibition against fibrinogen hydrolytic and collagen hydrolytic activities of T. flavoviridis venom were examined by SDS-PAGE. A histopathological study was done by microscopy after administration of venom in the presence or absence of RA. RA was found to markedly neutralize venom-induced hemorrhage, fibrinogenolysis, cytotoxicity and digestion of type IV collagen activity. Moreover, RA inhibited both hemorrhage and neutrophil infiltrations caused by T. flavoviridis venom in pathology sections. These results demonstrate that RA inhibited most of the hemorrhage effects of venom. These findings indicate that rosmarinic acid can be expected to provide therapeutic benefits in neutralization of snake venom accompanied by heat stability

Chemical and biochemical Studies of an Antidote Active Compound against Hemorrhagic Snake Venom from Argusia argentea

Argusia argentea (Boraginaceae) is locally used in Okinawa as an antidote for jellyfish toxin and sea snakes venom poisoning. The crude methanol extract of the twigs and leaves of Argusia argentea was fractionated with ethyl acetate, 1-butanol and water successively. An acidic compound, rosmarinic acid RA (1), was isolated and purified from the ethyl acetate fraction by silica gel column chromatography, HPLC with ODS column and Cosmosil Cholester column. Snake venom neutralization activities of the active compound were examined by pharmacological assay methods. The results revealed that rosmarinic acid effectively inhibited venom-induced fibrinogenolytic, cytotoxic, edema, lethality, digestion of type IV collagen activity. Moreover, rosmarinic acid (1) inhibited both hemorrhage and neutrophil infiltrations caused by protobothrops flavoviridis venom in pathology sections. In this study, we investigated the structural requirements necessary for inhibition of snake venom activity through the use of compounds, which are structurally related rosmarinic acid (1). By examining anti-hemorrhagic activity of cinnamic acid analogs against protobothrops flavoviridis venom, it was revealed that the presence of the E-enoic acid moiety (-CH=CH-COOH) was critical. Furthermore, we examined the effect of benzenepolycarboxylic acids and substituted benzoic acids against protobothrops flavoviridis venom-induced hemorrhage. Pyromelltic acid (1,2,4,5- benzenetetra carboxylic acid) was found to be a potent inhibitor of hemorrhage, with an IC50 value of 0.35 PM

Effects of Anacetrapib in Patients with Atherosclerotic Vascular Disease

BACKGROUND: Patients with atherosclerotic vascular disease remain at high risk for cardiovascular events despite effective statin-based treatment of low-density lipoprotein (LDL) cholesterol levels. The inhibition of cholesteryl ester transfer protein (CETP) by anacetrapib reduces LDL cholesterol levels and increases high-density lipoprotein (HDL) cholesterol levels. However, trials of other CETP inhibitors have shown neutral or adverse effects on cardiovascular outcomes. METHODS: We conducted a randomized, double-blind, placebo-controlled trial involving 30,449 adults with atherosclerotic vascular disease who were receiving intensive atorvastatin therapy and who had a mean LDL cholesterol level of 61 mg per deciliter (1.58 mmol per liter), a mean non-HDL cholesterol level of 92 mg per deciliter (2.38 mmol per liter), and a mean HDL cholesterol level of 40 mg per deciliter (1.03 mmol per liter). The patients were assigned to receive either 100 mg of anacetrapib once daily (15,225 patients) or matching placebo (15,224 patients). The primary outcome was the first major coronary event, a composite of coronary death, myocardial infarction, or coronary revascularization. RESULTS: During the median follow-up period of 4.1 years, the primary outcome occurred in significantly fewer patients in the anacetrapib group than in the placebo group (1640 of 15,225 patients [10.8%] vs. 1803 of 15,224 patients [11.8%]; rate ratio, 0.91; 95% confidence interval, 0.85 to 0.97; P=0.004). The relative difference in risk was similar across multiple prespecified subgroups. At the trial midpoint, the mean level of HDL cholesterol was higher by 43 mg per deciliter (1.12 mmol per liter) in the anacetrapib group than in the placebo group (a relative difference of 104%), and the mean level of non-HDL cholesterol was lower by 17 mg per deciliter (0.44 mmol per liter), a relative difference of -18%. There were no significant between-group differences in the risk of death, cancer, or other serious adverse events. CONCLUSIONS: Among patients with atherosclerotic vascular disease who were receiving intensive statin therapy, the use of anacetrapib resulted in a lower incidence of major coronary events than the use of placebo. (Funded by Merck and others; Current Controlled Trials number, ISRCTN48678192 ; ClinicalTrials.gov number, NCT01252953 ; and EudraCT number, 2010-023467-18 .)

Evaluation of Milk Clotting and Proteolytic Activity of Moringa oleifera L.

Extracts from fruits and plants were used as milk coagulants in many areas of the world. The aim of the present study was to investigate the milk clotting and proteolytic enzyme activity of Moringa oleifera L. seed kernels with the aim of establishing the optimal conditions (pH, temperature and concentrations of enzyme) to be used for making cheese. In addition, the effects of calcium ions and cysteine on milk clotting and proteolytic enzyme activities were also studied. Moreover, the qualitative proteolytic enzyme activity was investigated utilizing the used X-ray film. The optimal conditions (pH, temperature and concentrations of enzyme) and effects of calcium ions and cysteine on proteolytic enzyme activities were determined by spectrophotometric method using Folin-Ciocalteu's reagent. Furthermore, the cheese was made by using the best optimal conditions of the enzyme solution of Moringa oleifera L

Two New Ergosterol Derivatives from the Basidiomycete Cortinarius glaucopus

Two new sterols 1 and 2 and ␣ve known ones 3 – 7 were isolated for the ␣rst time from the fruiting bodies of Cortinarius glaucopus. Their structures were established by 1- and 2D-NMR spectra and HR-FABS-MS. The relative con␣guration of 1 was ␣rmly determined by comparison of the observed 1H–1H couplings and NOESY correlations, with those predicted for the computed geometries of the conformers. Calculations were performed by means of DFT with the B3LYP functional at 6-31 + G(d,p) level of theory, in CHCl3 as the solvent. The structures of the new ergosterol derivatives, called glaucoposterol A (1) and B (2), were thus established as (3S,5R,7R,10R,13R,17R, 20S,22R,23R,24R)-5,6-epoxy-3,7,23-trihydroxystrophast-8-en-14-one and (22E,3S,5S,9S,10R,13R,17R,20R,24R)-3,5-dihy- droxyergosta-6,8(14),22-trien-15-one, respectively. Moreover, the con␣guration of known strophasterol C (3) was determined as (3S,5R,6S,7R,10R,13R,17R,20S,22S,24R). Glaucoposterol A (1) and strophasterol C (3) represent the second ␣nding in nature of steroids with the rare strophastane skeleton