Background and Objectives: While Theobroma cacao L has long been utilized in the food, cosmetic, and pharmaceutical industries, it was also found to possess antibacterial activity. The beans comprise 10% of the fruit, while the remaining 90%, consisting of pods, is considered waste. It was reported that the pods possess antibacterial activity, and if utilized for this purpose, T. cacao pods will no longer be considered as waste. The aim of this study was to evaluate the antibacterial activity of the cream formulated from the aqueous extract of T. cacao L pods. Methods: The milled T. cacao pods were extracted using distilled water at 4°C for 24 hours. The crude extract was subjected to liquid-liquid partitioning using hexane, ethyl acetate, and n-butanol. Phytochemical screening was performed to identify the constituents present in the extract and its fractions. The extract and its fractions were tested against Staphylococcus aureus, Staphylococcus epidermidis, and Pseudomonas aeruginosa. Determination of IC50 using 3,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) Reduction Assay was used to evaluate the antibacterial activity. The extract with the highest yield and the highest antibacterial activity were formulated into a cream. T. cacao cream was evaluated with quality control tests for creams and emulsions. Acute skin irritation test was performed on the T. cacao cream to assess skin irritability upon application on adult male albino rabbits. Results: T. cacao crude extract and its fractions possessed antibacterial activity. Among the fractions tested, n-butanol fraction had the highest activity against S. aureus, S. epidermidis, and P. aeruginosa. There was a significant difference between the fractions tested on the three bacterial strains (p<0.05). Although n-butanol fraction had the highest activity, the actual yield obtained after extraction was 0.95%. Since T. cacao aqueous extract also exhibited good antibacterial activity, it was chosen for the formulation study. There was no significant difference between the IC50 of the T. cacao crude extract and the IC50 of T. cacao cream, hence formulating it into a cream did not affect the antibacterial activity of the extract. Conclusion T. cacao pod extract, as well as its fractions, possessed antibacterial activity against three bacterial strains. The T. cacao cream produced was a water-in-oil, non-irritant cream with antibacterial activity, and with acceptable physical attributes.
Inhibitory Concentration 50

In our search for natural soluble epoxide hydrolase (sEH) inhibitors from plants, an extract of the dried whole plants of Euphorbia supina Rafin was found to significantly inhibit sEH activity in vitro. Phytochemical investigation of E. supina resulted in isolation of 17 compounds (1 - 17), including triterpenes (1 - 4), phenolic compounds (5 - 8), and flavonoid derivatives (9 - 17). The structures of the isolated compounds were established mainly by extensive analysis of the 1D and 2D NMR, and MS data. All of the isolated compounds were evaluated for their sEH inhibitory activity. Among the isolated phenolic compounds, 8 was identified as a significant inhibitor of sEH, with an IC50 value of 15.4 +/- 1.3 microM. Additionally, a kinetic analysis of isolated compounds (2, 5, 8 - 11, 13, and 17) indicated that the inhibitory effects of flavonoid derivatives 10 and 11 were of mixed-type, with inhibitory constants (Ki) ranging from 3.6 +/- 0.8 to 21.8 +/- 1.0 microM, whereas compounds 2, 5, 8, 9, 13, and 17 were non-competitive inhibitors with inhibition Ki values ranging from 3.3 +/- 0.2 to 39.5 +/- 0.0 microM.
Euphorbia* ; Euphorbiaceae ; Inhibitory Concentration 50 ; Phenol ; Triterpenes

A new L-isoascorbic acid derivative epi-leptosphaerin (1) and two known compounds leptosphaerin (2), and verongamine (3) were isolated from sponges of the orders Verongida and Thorectidae. Compounds 1 and 2 are most likely of sponge-associated fungal origin. In the present study, isolated compounds were investigated for their inhibition of soluble epoxide hydrolase (sEH), which is considered a promising target for the management of pain, inflammation, and comorbidities associated with diabetes. Compound 3, verongamine, displayed weak inhibitory activity against sEH with an IC50 value 51.5 +/- 1.0 microM.
Comorbidity ; Inflammation ; Inhibitory Concentration 50 ; Porifera*

Green tea, the leaves of Camellia sinsneis (Theaceae), is generally acknowledged as the most consumed beverage with multiple pharmacological functions including antioxidant activity. This study was performed to analyze the effect of extraction conditions of green tea on its antioxidant effects using DPPH assay. Three extraction factors such as extraction solvent (EtOH, 0 – 100%), extraction time (3 – 15 min) and extraction temperature (10 – 70℃) were analyzed and optimized extraction condition for antioxidant activity of green tea extract (GTE) was determined using response surface methodology with three-level-three-factor Box-Behnken design (BBD). Regression analysis showed a good fit of data and the optimal conditions of extraction were found to be 57.7% EtOH, 15 min and 70℃. Under this condition, antioxidant activity of experimental data was 88.4% which was almost fit to the ideal value of 88.6%. As epigallocatechin gallate (EGCG) is known for the major ingredient for antioxidant activity of green tea, we investigated the effect of EGCG on antioxidant activity of GTE. EGCG showed antioxidant activity with the IC50 value of 4.2 µg/ml and a positive correlation was observed between EGCG content and the antioxidant activity of GTE with R2 = 0.7134. Interestingly, however, GTE with 50 – 70% antioxidant activity contain less than 1.0 µg/ml of EGCG, which is much lower than IC50 value of EGCG. Therefore, we suppose that EGCG together with other constituents contribute to antioxidant activity of GTE. Taken together, these results suggest that green tea is more beneficial than EGCG alone for antioxidant ability and optimal extraction condition of green tea will be useful for the development of food and pharmaceutical applications.
Antioxidants ; Beverages ; Camellia ; Inhibitory Concentration 50 ; Tea*

Phytochemical investigation from the stem bark of Beilschmiedia pulverulenta resulted in the isolation of five lignans, (+)-yangambin (1), (+)-sesartemin (2), (+)-excelsin (3), (+)-sesamin (4), and (+)-syringaresinol (5), together with lupeol (6), lupenone (7), β-sitosterol (8), and β-sitostenone (9). Their structures were established by the analysis of their spectroscopic (1D and 2D NMR) and spectrometric (MS) data, as well as by comparison with those reported in the literature. The isolated lignans were tested for their anticholinesterase (AChE: acetylcholine esterase and BChE: butyryl cholineesterase) and anti-inflammatory (COX-2: cyclooxygenase-2 and LOX: lipoxygenase) activities. All the isolated lignans (1 – 5) exhibited significant inhibition activities in AChE/BChE and COX-2/LOX assays with IC50 values ranging from 168.8 – 504.2 µM and 21.0 – 59.4 µM, respectively.
Acetylcholine ; Cyclooxygenase 2 ; Inhibitory Concentration 50 ; Lignans

The roots of Phlomis umbrosa (Turcz.) (Phlomidis Radix) have been traditionally used to treat cold, reduce swelling and staunch bleeding. Four iridoids (1 – 3 and 5) and six phenylethanoid derivatives (4, and 6 – 10) were isolated from the roots of P. umbrosa. A simple, sensitive, and reliable analytical HPLC/PDA method was developed, validated, and applied to determine 10 marker compounds in Phlomidis Radix. Furthermore, the isolates were evaluated for cytotoxic and anti-oxidant activities as well as DPPH-HPLC method. Among them, compounds 4 and 6 – 9 displayed potent anti-oxidant capacities using DPPH assay with IC50 values of 27.7 ± 2.4, 10.2 ± 1.1, 18.0 ± 0.8, 19.1 ± 0.3, and 19.9 ± 0.6 µM, and compounds 6, 8, and 9 displayed significant cytotoxic activity against HL-60 with IC50 values of 35.4 ± 3.1, 18.6 ± 2.0, and 42.9 ± 3.0 µM, respectively.
Hemorrhage ; Inhibitory Concentration 50 ; Iridoids ; Methods ; Phlomis

Toxicity of the fungicide Flutolanil was in vitro tested against 20 isolates of Macrophomina phaseolina and cotton seedlings of ten commercial cotton cultivars. The isolates were recovered from roots of cotton plants obtained from different cotton-growing areas in Egypt. Most of the tested isolates were sensitive to Flutolanil; however, they varied in sensitivity. Twenty-five percent of the isolates were highly sensitive where IC50 ranged from < 1 to 5.1 microg/ml, 20% of the isolates were sensitive where IC50 ranged from 15 to 30 microg/ml, 45% of the isolates were moderately sensitive where IC50 ranged from 46 to 58.5 microg/ml, and 10% of the isolates were not much sensitive (tolerant) where IC50 was > 100 microg/ml. Flutolanil was very safe on both shoots and roots of the tested cultivars (IC50 > 100 microg/ml). Treating cotton seeds with Flutolanil resulted in highly significant (P < 0.01) reductions in pathogenicity of 18 isolates and a significant reduction (P < 0.05) in pathogenicity of isolate M29. M1 was the only isolate, which was insensitive to the application of Flutolanil. In vivo toxicity to Flutolanil was not correlated with its in vitro toxicity. However, a highly significant correlation (r = 0.60, P < 0.01) was observed between pathogenicity of isolates and the in vivo toxicity of the fungicide.
Egypt ; Gossypium ; Inhibitory Concentration 50 ; Seedlings ; Virulence

Phytochemical investigation of the aerial components of Ducrosia ismaelis Asch. led to the isolation of six known compounds, psoralen (1), isopsoralen (2), cnidioside A (3), (-)-syringaresinol-O-beta-D-glucopyranoside (4), (E)-plicatin B (5), trilinolein (6). The chemical structures of these compounds were elucidated from spectroscopic data and by comparison of these data with previously published results. The antioxidant, anti-osteoporotic and cardiovascular related activities of the isolated compounds were assessed using oxygen radical absorbance capacity (ORAC), reducing capacity, tartrate-resistant acid phosphatase (TRAP), and soluble epoxide hydrolase (sEH) inhibitory activity assays. Compounds (3-5) showed potent peroxyl radical-scavenging capacities with ORAC values of 11.06 +/- 0.39, 7.98 +/- 0.10, and 13.99 +/- 0.06 Trolox equivalent (TE) at concentrations of 10 microM, respectively. Only compounds 4 and 5 was able to significantly reduce Cu2+ ions, with a reduction value of 9.06 +/- 0.32 and 4.61 +/- 0.00 microM Trolox Equivalent (TE) at a concentration of 10 microM. Compound 5 at 10 microM exhibited a potent inhibitory effect on osteoclastic TRAP activity with a TRAP value of 86.05 +/- 6.55% of the control. Compounds 1, 3 and 5 potently inhibited sEH activity with IC50 values of 41.6 4.9, 16.0 1.1, and 49.0 5.7 microM, respectively.
Acid Phosphatase ; Apiaceae ; Ficusin ; Inhibitory Concentration 50 ; Ions ; Osteoclasts ; Oxygen

Chemical investigation of the fermentation broth of a Soft Coral-Derived fungus Pestalotiopsis sp., led to the isolation of a new phthalide derivative, pestalotiolide A (1), three known analogues (2, 3 and 4), along with 5'-O-acetyl uridine (5) first isolated as a natural product. The structure of the new compound (1) was established by comprehensive spectroscopic analysis and chemical methods. Compounds 1 - 4 possessed varying degrees of antiviral activities, which was reported for the first time. Compared to the positive control ribavirin (IC50 = 418.0 microM), pestalotiolide A (1) exhibited significant anti-EV71 activity in vitro, with an IC50 value of 27.7 microM. Furthermore, the preliminary structure-activity relationship of antiviral activities was also discussed.
Fermentation ; Fungi* ; Inhibitory Concentration 50 ; Ribavirin ; Structure-Activity Relationship ; Uridine

Three Diels-Alder type adducts, guangsangon E (1), chalcomoracin (2) and sorocein I (3) were isolated from hairy root cultures of Morus macroura. The structures of the isolated compounds (1 – 3) were determined by spectroscopic method (NMR and MS), and spectral comparison to literature. Cytotoxic activities of the isolated compounds (1 – 3) were investigated against P-388 murine leukemia cell line. Guangsangon E (1) showed the most potent cytotoxicity against P-388 murine leukemia cell line with IC₅₀ value of 2.75 ± 0.32 µg/mL. To the best of our knowledge, guangsangon E (1) and sorocein I (3) were reported for the first time from the tissue cultures of M. macroura.
Cell Line ; Inhibitory Concentration 50 ; Leukemia ; Methods ; Morus