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Determination of betulinic acid from Orthosiphon stamineus leaf extract in rat plasma

Akowuah GA, Zhari I

Pharmazie, 2008 Nov;63(11):788-90.
PMID: 19069237

A simple high-performance liquid chromatography (HPLC) method to determine the content of betulinic acid (BA) in rat plasma collected at different times (0-8 h) after oral administration of Orthosiphon stamineus leaf extract was developed. The features of the assay include protein precipitation using acetonitrile and isocratic elution using reverse phase C-18 column with ultraviolet (UV) detection. The recovery of BA from plasma varied from 98.4 to 102.5%. The R.S.D of intra- and inter-day precision from rat plasma ranged from 4.2 to 9.8%. The maximum concentration of BA in the plasma was 1.2 +/- 0.3 microg/ml at 1 h after oral administration of the extract.
Analysis of urinary andrographolides and antioxidant status after oral administration of Andrographis paniculata leaf extract in rats

Akowuah GA, Zhari I, Mariam A

Food Chem Toxicol, 2008 Dec;46(12):3616-20.
PMID: 18824206 DOI: 10.1016/j.fct.2008.09.008

A simple high-performance liquid chromatography (HPLC) method was developed to determine the content of andrographolide (AP) and 14-deoxy-11,12-dideoxyandrographolide (DIAP) in a pooled urine of rat obtained within 24h after an oral dose of Andrographis paniculata leaf extract at 1g/kg body weight. Cumulative urinary excretion of AP and DIAP in 24h after oral administration of the extract was 0.88% and 1.61% of oral dose administered, respectively. The extract showed significant reduction (p<0.05) of MDA levels and elevation of total antioxidant status in rat urine samples collected in 24 after oral administration.
Absorption of andrographolides from Andrographis paniculata and its effect on CCl(4)-induced oxidative stress in rats

Akowuah GA, Zhari I, Mariam A, Yam MF

Food Chem Toxicol, 2009 Sep;47(9):2321-6.
PMID: 19540299 DOI: 10.1016/j.fct.2009.06.022

A simple and validated high-performance liquid chromatography (HPLC) method with UV detection has been used to determine the content of andrographolide (AP) and 14-deoxy-11,12-didehydroandrographolide (DIAP) in rat plasma after oral dose of methanol extract (1 g/kg body weight) of Andrographis paniculata leaf. An increase in plasma concentration of AP and DIAP was observed from 30 min to 3 h after oral administration of the extract. The maximum plasma concentrations of AP and DIAP were 1.42+/-0.09 microg/ml and 1.31+/-0.04 microg/ml, respectively. Fourteen days oral treatment of rats with the methanol extract (1 g/kg body weight) followed by CCl(4) administration preserved catalase (CAT), and superoxide dismutase (SOD) activities in erythrocytes, whereas plasma lipid peroxidation, alanine transaminase (ALT) and aspartate transaminase (AST) activities were restored to values comparable with control values. Treatment of rats with CCl(4) did not showed significant alteration (p>0.05) in plasma total antioxidant status (TAS) as compare to values of control group.
Docking Studies of Curcumin and Analogues with Various Phosphodiesterase 4 Subtypes

Yi YX, Gaurav A, Akowuah GA

Curr Drug Discov Technol, 2020;17(2):248-260.
PMID: 30332967 DOI: 10.2174/1570163815666181017091655

INTRODUCTION: The primary aim of this study is to understand the binding of curcumin and its analogues to different PDE4 subtypes and identify the role of PDE4 subtype inhibition in the anti-inflammatory property of curcumin. Docking analysis has been used to acquire the above mentioned structural information and this has been further used for designing of curcumin derivatives with better anti-inflammatory activity.
MATERIALS AND METHODS: Curcumin and its analogues were subjected to docking using PDE4A, PDE4B, PDE4C and PDE4D as the targets. A data set comprising 18 analogues of curcumin, was used as ligands for docking of PDE4 subtypes. Curcumin was used as the standard for comparison. Docking was performed using AutoDock Vina 1.1.2 software integrated in LigandScout 4.1. During this process water molecules were removed from proteins, charges were added and receptor structures were minimised by applying suitable force fields. The docking scores were compared, and the selectivity of compounds for PDE4B over PDE4D was calculated as well.
RESULTS: All curcumin analogues used in the study showed good binding affinity with all PDE4 subtypes, with evident selectivity towards PDE4B subtype. Analogue A11 provides the highest binding affinity among all ligands.
CONCLUSION: Curcumin and analogues have moderate to strong affinity towards all PDE4 subtypes and have evident selectivity towards PDE4B. The Oxygen atom of the methoxy group plays a key role in PDE4B binding and any alterations could interfere with the binding. Tetrahydropyran side chain and heterocyclic rings are also suggested to be helpful in PDE4B binding.
Inhibitory effects of Cinnamomum burmannii Blume stem bark extract and trans-cinnamaldehyde on nasopharyngeal carcinoma cells; synergism with cisplatin

Daker M, Lin VY, Akowuah GA, Yam MF, Ahmad M

Exp Ther Med, 2013 Jun;5(6):1701-1709.
PMID: 23837058

Nasopharyngeal carcinoma (NPC) is a malignancy that occurs in the epithelium of the nasopharynx. The standard treatment of NPC patients with locoregionally advanced stages is problematic and is often associated with toxicities. Therefore, it is essential to screen for naturally occurring compounds with strong apoptosis-inducing activity and minimal toxicity. This study investigated the effects of the standardized methanol extract of Cinnamomum burmannii Blume stem bark and its main constituent, trans-cinnamaldehyde (TCA), on human NPC cell lines. The content of TCA in C. burmannii methanol extract was standardized to be 13.61% w/w by means of gas chromatography-mass spectrometry (GC-MS). NPC cell proliferation was clearly inhibited within 24 h of treatment, with TCA exhibiting greater activity than the methanol extract. TCA was more active against NPC cells compared with cisplatin. There was a pronounced downregulation of the proliferation markers, Ki67 and proliferating cell nuclear antigen (PCNA) in the TCA-treated cells; while morphological observation indicated the induction of apoptosis. Caspase activation and prominent DNA damage, which are markers of apoptosis induction were detected. TCA demonstrated the ability to scavenge nitric oxide. The simultaneous combination of TCA and cisplatin produced synergistic anti-proliferative effects. Collectively, these data indicate the potential use of TCA for the treatment of NPC.
Structure-based design of selective phosphodiesterase 4B inhibitors based on ginger phenolic compounds

Xing M, Akowuah GA, Gautam V, Gaurav A

J Biomol Struct Dyn, 2017 Oct;35(13):2910-2924.
PMID: 27608741 DOI: 10.1080/07391102.2016.1234417

Phosphodiesterase 4 (PDE4) has been established as a drug target for inflammatory diseases of respiratory tract like asthma and chronic obstructive pulmonary disease. The selective inhibitors of PDE4B, a subtype of PDE4, are devoid of adverse effects like nausea and vomiting commonly associated with non-selective PDE4B inhibitors. This makes the development of PDE4B subtype selective inhibitors a desirable research goal. Thus, in the present study, molecular docking, molecular dynamic simulations and binding free energy were performed to explore potential selective PDE4B inhibitors based on ginger phenolic compounds. The results of docking studies indicate that some of the ginger phenolic compounds demonstrate higher selective PDE4B inhibition than existing selective PDE4B inhibitors. Additionally, 6-gingerol showed the highest PDE4B inhibitory activity as well as selectivity. The comparison of binding mode of PDE4B/6-gingerol and PDE4D/6-gingerol complexes revealed that 6-gingerol formed additional hydrogen bond and hydrophobic interactions with active site and control region 3 (CR3) residues in PDE4B, which were primarily responsible for its PDE4B selectivity. The results of binding free energy demonstrated that electrostatic energy is the primary factor in elucidating the mechanism of PDE4B inhibition by 6-gingerol. Dynamic cross-correlation studies also supported the results of docking and molecular dynamics simulation. Finally, a small library of molecules were designed based on the identified structural features, majority of designed molecules showed higher PDE4B selectivity than 6-gingerol. These results provide important structural features for designing new selective PDE4B inhibitors as anti-inflammatory drugs and promising candidates for synthesis and pre-clinical pharmacological investigations.
Fulltext The Effectiveness of Rambutan (Nephelium lappaceum L.) Extract in Stabilization of Sunflower Oil under Accelerated Conditions

Mei WS, Ismail A, Esa NM, Akowuah GA, Wai HC, Seng YH

Antioxidants (Basel), 2014;3(2):371-86.
PMID: 26784877 DOI: 10.3390/antiox3020371

The oxidative properties of sunflower oil supplemented with rambutan extract, (crude extract and its fractionated fraction, SF II) in comparison with synthetic antioxidant were investigated. The supplemented sunflower oils were stored under accelerated conditions for 24 days at 60 °C. For every 6-day interval, the oxidative properties of the supplemented sunflower oil were evaluated based on the following tests, namely peroxide value, p-anisidine value, Thiobarbituric Acid Reactive Substances (TBARS) assay, iodine value and free fatty acids. The total oxidation (TOTOX) values were also calculated based on the peroxide values and p-anisidine values. Rambutan extract is a potential source of antioxidant. The oxidative activities of the extracts at all concentrations were significantly (p < 0.05) higher than the control. Generally, the partially fractionated fraction was more effective than the crude extract. With a 2-year storage period at ambient temperature, the fractionated fraction of the extract, SF II at 300 ppm, was observed to work more effectively than the synthetic antioxidant, t-Tocopherol, and it possessed a protective effect comparable with butylatedhydrioxynanisole (BHA). Therefore, rambutan extract could be used as a potential alternative source of antioxidant in the oil industry or other fat-based products to delay lipid oxidation.
Safety assessment of standardised methanol extract of Cinnamomum burmannii

Ahmad M, Lim CP, Akowuah GA, Ismail NN, Hashim MA, Hor SY, et al.

Phytomedicine, 2013 Sep 15;20(12):1124-30.
PMID: 23827665 DOI: 10.1016/j.phymed.2013.05.005

The present study aims to evaluate the safety of methanol extract of Cinnamomum burmannii (MECB) by acute 14-day (single dose) and sub-chronic 28-day (repeated doses) oral administration to Sprague-Dawley rats. Our results showed that no toxicity was found in either acute or sub-chronic toxicity studies. MECB (containing 0.07% and 0.20% (w/w) of coumarin and trans-cinnamaldehyde, respectively), which was given orally at doses of 500, 1000 and 2000 mg/kg caused neither visible signs of toxicity nor mortality. No significant differences were observed in general condition, growth, organ weight, hematological parameters, biochemical values, or the gross and microscopic appearance of the organs from the treatment groups as compared to the control group. In conclusion, MECB did not cause any mortality nor did it cause any abnormalities in the necropsy and histopathology findings of treated rats. The LD50 for the MECB was found to be more than 2000 mg/kg. No adverse effects were observed in the treated rats at all the doses tested. The no-observed-adverse-effect level (NOAEL) for the 28-day study was determined to be 2000 mg/kg body weight/day.
Natural alternatives from your garden for hair care: Revisiting the benefits of tropical herbs

Sang SH, Akowuah GA, Liew KB, Lee SK, Keng JW, Lee SK, et al.

Heliyon, 2023 Nov;9(11):e21876.
PMID: 38034771 DOI: 10.1016/j.heliyon.2023.e21876

Hair shampoos containing botanical ingredients without synthetic additives, such as parabens, petrochemicals, sulfates and silicones are more skin- and environmentally friendly. In recent years, there is a growing demand for shampoo products with botanical extracts. Shampoos with botanical extracts are well-known for their perceived health benefits. They are also generally milder, non-toxic, natural, and less likely to disrupt the hair and scalp's natural pH and oil balance. Many also believe that shampoos with botanical origins have higher standards of quality. Numerous botanical extracts had been used as natural active ingredients in cosmetic formulations to meet consumer demands. In this review, we have revisited six tropical plants commonly added as natural active ingredients in shampoo formulations: Acacia concinna, Camellia oleifera, Azadirachta indica, Emblica officinalis, Sapindus mukorossi, and Garcinia mangostana. These plants have been traditionally used for hair care, and scientific research has shown that they exhibit relevant physicochemical properties and biological activities that are beneficial for hair care and scalp maintenance.