Phytochemical and Biological Investigation of an Indigenous Plant of Bangladesh, Gynura procumbens (Lour.) Merr.: Drug Discovery from Nature.

Gynura procumbens (Lour.) Merr. (Family: Asteraceae) is a tropical Asian medicinal plant found in Thailand, China, Malaysia, Indonesia, and Vietnam. It has long been utilized to treat a variety of health concerns in numerous countries around the world, such as renal discomfort, constipation, diabetes mellitus, rheumatism, and hypertension. The chemical investigation resulted in the isolation and characterization of six compounds from the methanol (MeOH) extract of the leaves of Gynura procumbens, which were identified as phytol (1), lupeol (2), stigmasterol (3), friedelanol acetate (4), ß-amyrin (5), and a mixture of stigmasterol and ß-sitosterol (6). In-depth investigations of the high-resolution 1H NMR and 13C NMR spectroscopic data from the isolated compounds, along with comparisons to previously published data, were used to clarify their structures. Among these, the occurrence of Compounds 1 and 4 in this plant are reported for the first time. The crude methanolic extract (CME) and its different partitionates, i.e., petroleum ether (PESF), chloroform (CSF), ethyl acetate (EASF), and aqueous (AQSF) soluble fractions, were subjected to antioxidant, cytotoxic, thrombolytic, and anti-diabetic activities. In a DPPH free radical scavenging assay, EASF showed the maximum activity, with an IC50 value of 10.78 µg/mL. On the other hand, CSF displayed the highest cytotoxic effect with an LC50 value of 1.94 µg/mL compared to 0.464 µg/mL for vincristine sulphate. In a thrombolytic assay, the crude methanolic extract exhibited the highest activity (63.77%) compared to standard streptokinase (70.78%). During the assay for anti-diabetic activity, the PESF showed 70.37% of glucose-lowering activity, where standard glibenclamide showed 63.24% of glucose-reducing activity.

Isolation and Characterization of One New Natural Compound with Other Potential Bioactive Secondary Metabolites from Glycosmis cyanocarpa (Blume) Spreng. (Family: Rutaceae).

Glycosmis cyanocarpa (Blume) Spreng is a plant in the Rutaceae family and a species in the Glycosmis genus that has received little attention. Therefore, this research aimed to report the chemical and biological analysis of Glycosmis cyanocarpa (Blume) Spreng. The chemical analysis involved the isolation and characterization of secondary metabolites through an extensive chromatographic study, and the structures of these metabolites were elucidated on the basis of a detailed analysis of NMR and HRESIMS spectroscopic data and by comparison with those of related compounds reported in the literature. Different partitions of the crude ethyl acetate (EtOAc) extract were evaluated for antioxidant, cytotoxic, and thrombolytic potentials. In chemical analysis, one new phenyl acetate derivative, namely 3,7,11,15-tetramethylhexadec-2-en-1-yl 2-phenylacetate (1), along with four known compounds N-methyl-3-(methylthio)-N-(2-phenylacetyl) acrylamide (2), penangin (3), ß-Caryophyllene oxide (4), and acyclic diterpene-phytol (5) were isolated for the first time from the stem and leaf of the plant. The ethyl acetate fraction showed significant free radical scavenging activity with an IC50 value of 11.536 µg/mL compared to standard ascorbic acid (4.816 µg/mL). In the thrombolytic assay, the dichloromethane fraction showed the maximum thrombolytic activity of 16.42% but was still insignificant compared to the standard streptokinase (65.98%). Finally, in a brine shrimp lethality bioassay, the LC50 values of dichloromethane, ethyl acetate, and aqueous fractions were found to be 0.687 µg/mL, 0.805 µg/mL, and 0.982 µg/mL which are significant compared to the standard vincristine sulfate of 0.272 µg/mL.

Isolation, Characterization and Pharmacological Investigations of a New Phenolic Compound along with Four Others Firstly Reported Phytochemicals from Glycosmis cyanocarpa (Blume) Spreng.

Plants are serving the mankind with important bioactive phytochemicals from the very ancient ages to develop novel therapeutics against different disease states. Glycosmis cyanocarpa (Blume) Spreng is a plant from the Rutaceae family and a very less explored species from the Glycosmis genus. Thus, this present study was intended to present the chemical and biological investigation of Glycosmis cyanocarpa (Blume) Spreng. The chemical investigation resulted in the isolation of one new phenolic compound to the best of our knowledge which is (4-(3-hydroxy-2-methylpropyl)-2-methoxyphenol) (1) along with four known compounds that are isolated for the first time from this species- 3-methyl-1H-indole (2), Tri-transpoly-cis prenol-12 (3), Stigmasterol (4) and ß-sitosterol (5). Their chemical structures were elucidated based on extensive spectroscopic methods, including 1D and 2D NMR, and comparison with the available literature data. Isolated phytochemicals were further investigated to unveil their antioxidant properties with IC50 values (ranged from 9.97-75.48 µg/mL), cytotoxicity with LC50 values (ranged from 1.02-1.92 µg/mL), and antibacterial properties against some selected Gram (+) ve and Gram (-) ve bacteria. Among the compounds, 3-methyl-1H-indole (2) was found to be the most active against Staphylococcus aureus. Moreover, the phenolic compound (1) and the alkaloid (2) revealed the highest antioxidant (9.97 µg/mL) and cytotoxic activities (1.02 µg/mL), respectively. Thus, the isolation of these bioactive phytochemicals from the plant revealed a new perception in the study arena of drug discovery and the findings may ease the development and discovery of novel therapeutics. Further investigations are still recommended to understand their exact molecular mechanism and toxicological impact.

Chemico-Biological Profiling of Blumea lacera (Burm.f.) DC. (Family: Asteraceae) Provides New Insights as a Potential Source of Antioxidant, Cytotoxic, Antimicrobial, and Antidiarrheal Agents.

Blumea lacera (Burm.f.) DC., popular for its traditional use in different diseases, was employed in phytochemical and biological investigations. The chemical studies led to the isolation of acyclic diterpene-phytol (1) along with two fatty acids-linolenic acid (2) and oleic acid (3). All the structures were determined by 1H NMR spectroscopic analysis and first time reported from this plant. Different fractions of crude methanol extract were subjected to antioxidant, cytotoxicity, antimicrobial, and antidiarrheal assays. The molecular docking studies have been implemented using PyRx, UCSF Chimera, Discovery Studio, and online tools. In addition, The ADME/T analysis and PASS prediction were implemented by using PASS online tools. In the molecular docking study of antioxidant, cytotoxicity, antimicrobial, and antidiarrheal activity, the compounds showed strong binding affinity ranging from -4.5 to -6.2 kcal/mol. Again, all three isolated compounds met the preconditions of Lipinski's five rules for drug discovery. In DPPH free radical scavenging assay, the pet-ether and chloroform soluble fraction showed noteworthy antioxidant activity sowing promising IC50 values (10.76 µg/ml and 11.77 µg/ml, respectively), compared to the standard (6.05 µg/ml) with a total phenolic content range of 7.33-40.33 mg of GAE/gm. The pet-ether soluble fraction revealed substantial cytotoxicity showing an LC50 value of 1.03 µg/ml, compared to the standard (0.93 µg/ml). Besides, ethyl acetate soluble fraction showed moderate activity against both Gram-positive and Gram-negative bacteria, while both ethyl acetate and pet-ether soluble fraction showed excellent dose-dependent antidiarrheal activity.

Profiling of minerals, water soluble vitamins and carotenoid in selected unconventional leafy and non-leafy vegetables of Bangladesh.

The present study was aimed at evaluating mineral contents, B-vitamins (B1, B2, B3, B6), vitamin C, total carotenoids content and carotene composition of unconventional vegetables, comprising 7 leafy and 4 non-leafy, growing in Bangladesh. Investigated unconventional vegetables were found to have varied amount of minerals (0.04 ± 0.01 to 786.41 ± 6.37 mg/100 g), B-vitamins (0.06 ± 0.01 to 1.05 ± 0.13 mg/100 g) and vitamin C (5.23 ± 0.81 to 59.01 ± 2.23 mg/100 g). The study findings also revealed that the selected plant samples exhibited diverse amount of ß-carotene ranging from 106.26 ± 5.32 µg/100 g EP in Orhor dal to 994.81 ± 21.01 µg/100 g EP in Orhor Pata whereas lutein content ranged from 7.76 ± 1.02 µg/100 g EP in Pahari Kolar Thor to 566.33 ± 20.63 µg/100 g EP in Kachuripana. It can be suggested that regular intake of these vegetables may contribute to daily minerals and vitamins requirement and can combat micronutrient deficiency.

Immunoglobulins content in colostrum, transitional and mature milk of Bangladeshi mothers: Influence of parity and sociodemographic characteristics.

BACKGROUND: The study investigated the concentration of IgA, IgM and IgG in colostrum, transitional and mature milk and the effect of parity, age, BMI and family income on secreted immunoglobulin contents of human milk. METHODS: Sequential samples of colostrum, transitional and mature milk were collected from 38 women. Enzymelinked immunosorbent assay was used to analyse the immunoglobulin concentrations. RESULTS: The study revealed that IgA was the dominant immunoglobulin and mean concentration in colostrum, transitional and mature milk was 5.92 ± 1.50 g/L, 3.85 ± 0.64 g/L and 3.72 ± 0.68 g/L, respectively. Both IgA and IgM levels of colostrum decreased significantly in both transitional (P = 0.000) and mature milk (P = 0.000), while the concentration of IgG rises significantly in them (colostrum vs. transitional milk, P = 0.000; and colostrum vs. mature milk P = 0.011). While maternal age, BMI and family income had no significant influence on the immunoglobulin levels at different stages of lactation, parity showed significant influence on IgG (P = 0.03) and IgM (P = 0.05) levels of transitional milk and IgA level of colostrum (P = 0.05). CONCLUSION: The findings suggest that immunoglobulin composition in breast milk is strongly associated with stage of lactation and is likely to be more susceptible to parity than BMI and socioeconomic characteristics.

Crispenes F and G, cis-Clerodane Furanoditerpenoids from Tinospora crispa, Inhibit STAT3 Dimerization.

Two new cis-clerodane-type furanoditerpenes, crispenes F and G (1 and 2), together with seven known compounds, were isolated from the stems of Tinospora crispa. Crispenes F and G (1 and 2) inhibited STAT3 dimerization in a cell-free fluorescent polarization assay and were found to have significant cytotoxicity against a STAT3-dependent MDA-MB 231 breast cancer cell line, while being inactive in a STAT3-null A4 cell line. These two compounds share structural similarities with a previously reported STAT3 inhibitor, crispene E, isolated from the same plant. Molecular docking studies suggested that the molecules inhibit STAT3 by interacting with its SH2 domain.

Carotenoids and ß-carotene in orange fleshed sweet potato: A possible solution to vitamin A deficiency.

The present study, in line with a plant-food-based approach to address vitamin A deficiency, reports the analysis of total carotenoids, and trans- and cis-ß-carotenes, in different varieties of raw and boiled orange-fleshed sweet potatoes (OFSP). Carotenoids were isolated using acetone-petroleum ether extraction followed by spectrophotometric determination. trans- and cis-ß-Carotenes were analyzed by reversed-phase HPLC method using a mobile phase containing acetonitrile:methanol:2-propanol in the ratio of 85:15:33 with 0.01% ammonium acetate. Intra-varietal difference in carotenoids as well as trans- and cis-ß-carotenes were noted in both the raw and boiled potatoes. Carotenoid content was found to be higher in the raw potatoes compared to the boiled samples from the same variety. Amongst the OFSP varieties, Kamalasundari (BARI SP-2) was found to contain the most carotenoids in both the raw and boiled samples. ß-Carotene was significantly higher in the Kamalsundari and BARI SP-5 varieties. trans-ß-Carotene was found to be the major carotenoid in all of the raw potatoes, but boiling was associated with an increase in cis-ß-carotene and a decrease in the trans isomer. Kamalsundari and BARI SP-5 orange-fleshed sweet potatoes have the potential to be used as food-based supplements to reduce vitamin A deficiency.

Nutrient composition of strawberry genotypes cultivated in a horticulture farm.

This article decribes the nutrient composition of four strawberry genotypes cultivated at the Sher-e-Bangla Agriculture University horticulture farm in Dhaka (Bangladesh). AOAC and standard validated methods were employed to analyse the nutrient composition. Protein, fat and ash contents were found to be vary significantly (LSD<0.05), while the variation in moisture (LSD<1.33), dietary fibre (LSD<0.15) and total sugar (LSD<0.09) were found to be insignificant among the genotypes. Vitamin C content ranged from 26.46 mg to 37.77 mg per 100g edible strawberries (LSD<0.060). Amount of carotenoids were found to be very low being in a range of 0.99-3.30 µg per 100g edible fruit. Analysis of mineral revealed that strawberry genotypes contained a wide array of minerals including Ca, Mg, Na, K, P, Mn, Zn, Cu and Fe; most of which varied significantly (LSD<0.05) among the genotypes. Strawberries could be a potential dietary supplement for vitamin C along with minerals, particularly for the children who do not like local fruits, but love to eat the colourful strawberries.

Cytotoxic dimeric quinolone-terpene alkaloids from the root bark of Zanthoxylum rhetsa.

Four quinolone-terpene alkaloids, chelerybulgarine (1), 2'-episimulanoquinoline (3), 2,11-didemethoxyvepridimerine B (4), and rhetsidimerine (5) were isolated from the root bark of Zanthoxylum rhetsa DC. Chelerybulgarine (1) is a C-C linked terpene alkaloid where the C-6 of dihydrochelerythrine is linked to C-11 of the sesquiterpenoid 10ß-methoxybulgarene. 2'-Episimulanoquinoline is a dimeric alkaloid containing dihydrochelerythrine and 8-methoxy-N-methylflindersine moieties, whereas 2,11-didemethoxyvepridimerine B and rhetsidimerine are dimeric prenylated quinolone alkaloids. Seven of the isolated compounds exhibited weak cytotoxicity when tested against a panel of six human stomach-cancer cell lines.

Immunosuppressive and cytotoxic properties of Nigella sativa.

In this study the volatile oil of Nigella sativa seeds (NSVO) was investigated for its immunomodulating and cytotoxic properties. A rat model was designed to examine the effect of NSVO on selected immune components. Long-Evans rats were challenged with a specific antigen (typhoid TH) and treated with NSVO; and the changes produced in their serum antibody titre along with the splenocytes and peripheral immune cells were analysed. Antibody titre for the experimental animal was found to be 1280 as compared to the 2560 in the control rats. There was a significant (p < 0.05) decrease in splenocytes and neutrophils counts, but a rise in peripheral lymphocytes and monocytes in the experimental animals. To test the cytotoxicity of NSVO, a panel of five human cancer cell lines and a fibroblast line was used. The MTT assay was employed to estimate the cell mortality. Vinblastine sulphate and mitomycin C were used as the positive control. LC(50) values for NSVO were 155.02 +/- 10.4, 185.77 +/- 2.9, 120.40 +/- 20.5, 384.53 +/- 12.1 and 286.83 +/- 23.3 micro g/ml respectively against the SCL, SCL-6, SCL-37'6, NUGC-4 cancer lines and 3T6 fibroblast line. Results indicate that the NSVO could be considered as a potential immunosuppressive cytotoxic agent.

Cytotoxic diterpenes from Scoparia dulcis.

Four new labdane-derived diterpenes, iso-dulcinol (1), 4-epi-scopadulcic acid B (2), dulcidiol (4), and scopanolal (5), together with two known diterpenes, dulcinol/scopadulciol (3) and scopadiol (6), were isolated from the aerial parts of Scoparia dulcis. The structures were determined by extensive NMR studies. The crude extracts as well as the pure diterpenes showed cytotoxicity against a panel of six human stomach cancer cell lines.