Moch Futuchul Arifin, Elza Shafira, Yuslia Noviani, Yesi Desmiaty, Fauzia Noprima Okta

Our previous research investigated nanosuspension using the ionic gelation method with a 2:1 ratio of chitosan to sodium tripolyphosphate (TPP) and 0.44% Curcuma xanthorriza rhizome extract. The results indicated an unstable nanosuspension with a particle size of 399.3 nm, a polydispersity index of 0.60, and an entrapment efficiency of 73.37%. This study aims to develop a nanosuspension using Tween 80-PEG 400 to improve the characteristics and dissolution at pH 6.8. Curcuma rhizome was macerated with 96% ethanol and dried using a spray dryer. The nanosuspension formulation was designed using a 22 factorial design with Tween 80 (0.1%-0.4%) and PEG 400 (0.1%-0.4%) as factors, and the formulation was analyzed using Minitab 18. The dissolution of the optimum formulation was tested. The best formulation, comprising 0.1% Tween 80 and 0.4% PEG 400, provided a spherical shape, a particle size of 111.26 nm, a polydispersity index of 0.27, a zeta potential of 30.77 mV, an entrapment efficiency of 84.30%, and a desirability value of 0.9058. The release of curcumin at pH 6.8 after 180 minutes was 37.85% ± 0.1375 with a DE180 of 83.60% ± 0.1457. The 22 factorial design proved effective for enhancing formulation attributes. Based on the result obtained, it can be concluded that the best formulation contains 0.1% Tween 80 and 0.4% PEG 400, with zero-order release kinetics and a diffusion mechanism.

Sciences of Pharmacy

Rezky Yanuarty, Muthmainnah Tuldjanah, Ayu Wulandari

Erectile dysfunction (ED) and premature ejaculation are prevalent male sexual dysfunctions affecting various age groups. This study explores the potential aphrodisiac effects of Clove leaves (Syzygium aromaticum L.), a plant rich in secondary metabolites, including alkaloids, flavonoids, saponins, and steroids. Fractionation of the ethanol extract yielded n-hexane, ethyl acetate, and water fractions. Phytochemical screening revealed the presence of alkaloids, flavonoids, and saponins in the water fraction, while steroids were detected in the ethanol extract, ethyl acetate, and n-hexane fractions. In vivo tests on male rats demonstrated that the ethanol extract, n-hexane, and ethyl acetate fractions significantly reduced mounting latency (ML), increased mounting frequency (MF), and accelerated intromission latency (IL), indicating heightened sexual arousal and endurance. Moreover, these fractions delayed ejaculatory latency (EL) and increased ejaculation frequency (EF), akin to the positive control, X-Gra. Notably, the n-hexane fraction showed the closest efficacy to X-Gra. The presence of steroids in the active fractions suggests their role in eliciting aphrodisiac effects. Further isolation and purification of the active compound(s) may optimize therapeutic outcomes. This study underscores the potential of Clove leaf fractions as natural aphrodisiacs, warranting further investigation for clinical applications.

Sciences of Phytochemistry

Emmanuel Uronnachi, Onyinyechi Okpalaku, Chidalu Ikeotuonye

Rheumatoid Arthritis (RA) is a major challenge, especially in the elderly. Many orthodox drugs have been helpful in managing the disease; however, deleterious side effects have been reported. Essential oils have been shown to exhibit anti-arthritic properties. This study highlights and compares the chemical composition and anti-arthritic activities of essential oils from Citrus limon, Zingiber officinale, and Curcuma longa. Twenty-seven Wister rats of both sexes were divided into 9 groups of three animals each. Acute non-immunological arthritis was induced by a sub-plantar injection of 0.1 mL formaldehyde (2% v/v). The animals were treated topically with essential oils extracted by hydro-distillation and analyzed by gas chromatography. Measurement of paw volumes was done daily for 10 days using the volume displacement method. Ginger oil and turmeric oil achieved a 100% reduction in paw volume from the 8th day (p<0.05). The coconut oil as carrier for the essential oils exhibited sub-optimal reductions when administered alone as a control. Combinations of the oils showed an antagonistic effect in the ginger/turmeric oil blend, while the essential blends of turmeric/lemon and ginger/lemon oil performed better than the individual oils. The findings from this study showed that the woody essential oils (ginger and turmeric) exhibited the greatest anti-arthritic activity of all the oil treatment groups. Terpenes like ar-turmerone, turmerone, zingiberene, and D-limonene may have been responsible for the activities observed with the turmeric, ginger, and lemon essential oils, respectively. Lemon, ginger, and turmeric essential oils are effective for the management of rheumatoid arthritis.

Sciences of Phytochemistry

Neksumi Musa, Mubarak Muhammad Dahiru, Enoch Buba Badgal

In our study, we identified the phytoconstituents and carried out antimalarial, anti-inflammatory, antioxidant, and ADMET assessments of Neonauclea excelsa. The phytochemicals were detected and quantified followed by identification via GC-MS. The antimalaria, anti-inflammatory, and antioxidant assessments were done by molecular docking (MD) and molecular dynamics simulation (MDS) while ADMET by ADMET predictions. Saponins (27.33% ±1.20) and terpenes (8.33% ±0.73) were detected while alkaloids, steroids, glycosides, and flavonoids were absent. Exactly 29 compounds were identified with squalene being the most abundant (32.41%). Compound II exhibited the lowest BA (-6.4 kcal/mol) and Ki (20.12 µM), interacting with dihydrofolate reductase-thymidylate synthase. IV exhibited the lowest respective BA and Ki interacting with Plasmodium falciparum hexose transporter protein 1 (-6.2 kcal/mol and 28.20 µM), cyclo-oxygenase-2 (-7.2 kcal/mol and 5.21 µM), and myeloperoxidase (-7.4 kcal/mol and 3.71 µM). Compound VII had the lowest respective BA and Ki interacting with inducible nitric oxide synthase (-8.0 kcal/mol and 1.35 µM), xanthine oxidase (-7.2 kcal/mol and 5.21 µM), and cytochrome p450 21A2 (-7.0 kcal/mol and 7.30 µM). The MDS showed various cluster mobilities and residue fluctuations up to 5.26, 2.96, 5.10, 3.51, 5.02, 4.65, and 6.18 Å for dihydrofolate reductase-thymidylate synthase, Plasmodium falciparum hexose transporter protein 1, inducible nitric oxide synthase (INOS), cyclo-oxygenase-2 (COX2), xanthine oxidase (XO), cytochrome p450 21A2, and myeloperoxidase, respectively. Additionally, these compounds demonstrated good pharmacological properties with minimal toxicity. Conclusively, the identified compounds might be significant contributors to the antimalarial, anti-inflammatory, and antioxidant activity of N. excelsa and are good sources of novel antimalarial, anti-inflammatory, and antioxidant drugs.

Sciences of Pharmacy

İlayda Sezin YALÇINKAYA, Onur AKTAN, Leyla AÇIK, Gülnihal KULAKSIZ ERKMEN, NILUFER VURAL, Sibel KAYMAK, Yiğit Can ATEŞ

The ethnopharmacological significance of Rosa canina, or dog rose, transcends diverse cultures, with traditional applications in treating various diseases. This study investigates the potential pharmacological application of Rosa canina for diabetes treatment, aiming to assess its antidiabetic properties through in vitro, in vivo, and in silico analyses targeting pro-cytokines. Biochemical profiling utilizing HPLC, and phenolic content analyses were conducted to reveal the antioxidant properties of Rosa canina. In diabetic rats, root extracts influenced the expression of TNF-α and IL-1β, with an exploration of DNA-binding and protective activities. DPPH scavenging and iron chelating activities were measured, identifying significant IC50 values. The chromatographic analysis identified various compounds, with Kaempferol 3-O-glucoside and Rutin exhibiting high inhibitory activity against TNF-alpha. In silico analyses highlighted inhibitory activities by molecular docking against TNF-α and IL-1β (PDB IDs 2AZ5 and 9ILB, respectively) and their drug potential based on ADMET properties. The obtained results have demonstrated a significant decrease in blood glucose levels in mice through the reduction of TNF-α and IL-1β mediated diabetic processes, facilitated by the Rosa canina extract. In conclusion, this study exploring the effects of Rosa canina extracts on diabetic rats have provided valuable insights into its potential therapeutic benefits. The observed reductions in blood glucose levels, improvements in lipid profiles, and modulation of antioxidant activity highlight its promising role in managing diabetes-related complications. Further research is warranted to elucidate the underlying mechanisms and optimize the dosage regimens for harnessing the full therapeutic potential of Rosa canina extracts in diabetes management.

Sciences of Pharmacy

Hauwau Abubakar, Albashir Tahir, Aminu Kura Umar

Medicinal plants are gaining popularity as safer and more natural alternatives to orthodox medicines for managing health challenges and diseases. One such plant is Boswellia dalzielii, a renowned tree in northern Nigeria extensively used due to its ethnomedicinal importance. To determine the analgesic properties of Boswellia dalzielii methanol extract (BDME), the extract was screened in mice using thermal and acetic acid-induced pain models. The extract's acute toxicity and phytochemical constituents were determined using standard protocols. The results showed that the acute toxicity of the methanol stem bark extract was greater than 2000 mg/kg. Phytochemical screening of BDME revealed the presence of flavonoids, tannins, saponins, and glycosides. The extract, at the dose of 50 mg/kg significantly (p < 0.05) prolonged the pain reaction time at 15 and 30 minutes in the hot plate test, and reduced acetic acid-induced writhing at the 12.5, 25, and 50 mg/kg doses. The analgesic activity of the extract may be attributed to the phytochemical contents. The findings suggest that BDME have analgesic properties and could be beneficial in alleviating painful conditions.

Sciences of Phytochemistry

İsmihan GÖZE, Sibel KAYMAK, Nilüfer VURAL

This study aimed to assess the biological and biotherapeutic activities of essential oils derived from the medicinal plants Tanacetum vulgare L., Myrtus communis L. subsp. communis L., and Pimpinella flabellifolia (Boiss.) Benth. Et Hook. ex Drude. Plant samples were systematically collected from the Sivas region of Türkiye. Subsequently, essential oils were extracted using a Clevenger-type apparatus, and their compositions were assessed by gas chromatography–mass spectrometry (GC-MS) analysis. Then, antioxidant activities of the essential oil samples were investigated using β-carotene-linoleic acid and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays. Furthermore, the antimicrobial activity of these species was assessed via the disc diffusion assay. Finally, the potential effects of the essential oil compositions from these plants on milk production in dairy cows were analyzed through in-silico methods.

Sciences of Phytochemistry

Dian Ratih Laksmitawati, Umi Marwati, Fauzia Noprima Okta, Citra Prastuti Partana

Porang tuber is rich in fiber and low in calories of carbohydrates. Moringa oleifera leaf has a high protein and a low content of lipids. Obesity and diabetes mellitus are the risk factors of cardiovascular disease, also known as cardiovascular disease risk factors. Combining of porang and moringa as feed can increase nutrition without causing weight gain. This study aims to determine these two materials as antidiabetic and antiobesity agents. The samples are porang tuber, a combination of porang tuber and M. oleifera leaves, a combination of M. oleifera leaves and wheat flour, wheat flour, and standard feed of mice. The parameters tested in this study are analysis of macronutrients of feed, loss of weight of mice, average consuming feed in 28 days, and reduction of blood glucose with a glucometer. The results obtained are a combination of porang tuber and moringa had a low contain carbohydrates and a high contain lipids and protein, can reduction in body weight of 21%, the lowest consumption of feed, and the lowest fasting and postprandial blood glucose levels compared to the other feeds. A combination of porang and moringa can be an antidiabetic and antiobesity agent.

Sciences of Pharmacy

Rika Sari Dewi, Kristin Grave Gracia Saragih

Ciplukan leaves contain alkaloid compounds and exhibit pharmacological activity as bronchodilators. Bronchodilators are utilized in chronic inflammatory respiratory conditions such as asthma, involving various cell types such as mast cells, eosinophils, and epithelial cells. The objective of this study was to evaluate the effectiveness of administering Ciplukan leaf infusion as a bronchodilator. A total of 24 Sprague Dawley rats were divided into 6 groups: normal control (K1), negative control (K2), positive control (K3), 200 mg/kg BW dose (K4), 400 mg/kg BW dose (K5), and 800 mg/kg BW dose (K6). On days 1 and 8, rats were sensitized with 0.35 mg OVA + 1 mg AlOH3 in 0.9% NaCl (i.p). On days 15, 17, and 19, rats were re-sensitized with inhaled OVA. From day 20 to 28, K1 and K2 received no treatment, K3 received 2 mL/day of salbutamol, and the dose groups were administered 2 mL/day of Ciplukan leaf infusion; all treatments were carried out simultaneously. On day 29, rats were dissected, and their lung organs were collected for histopathological preparation. Research findings revealed a reduction in bronchiolar epithelial thickness across groups in the following order: 495.05; 584.95; 334.69; 421.70; 482.81; 484.95 µm. The sequential lung eosinophil counts were 19; 44; 37; 23; 17; and 27, and mast cell counts were 9; 22; 13; 15; 13; and 7. Statistical analysis demonstrated significant differences at the 200 mg/kg BW dose for the parameters of bronchiolar epithelial thickness and eosinophil count, as well as significant differences in mast cell counts at the 800 mg/kg BW dose and negative control group.

Sciences of Pharmacy

Mohamed Said Rajab

In an earlier study, six limonoids namely pyroangolensolide, calodendrolide, limonin, limonin diosphenol, harrisonin and pedonin were reported to exhibit varying larvicidal activity against Aedes aegypti L. second instar larvae. The degraded limonoids exhibited a higher larvicidal activity relative to the more complex compounds. To investigate this observation at the relevant Aedes aegypti L. receptor level, the six limonoids were subjected to an in silico docking study to evaluate the binding characteristics of the selected limonoids in the ecdysone receptor (EcR) protein (PDB code 1z5x). This was compared with the binding affinity of the dipteran specific ecdysone agonist, RH 5849 (1,2-Dibenzoyl-1-tert-butylhydrazine). The EcR protein1z5x-LBP was identified from literature data. The binding energies of the ligands docked in the EcR protein 1z5x-LBP ranged from 3.0 to -9.1 kcal/mol and the dissociation constants (Kd) ranged from 2.10×10-7 M to 1.59×10+2 M. RH 5849 had a binding energy of -8.9 kcal/mol which was comparable with those displayed by pyroangolensolide (-9.1 kcal/mol) and calodendrolide (-9.0 kcal mol). Two pharmacophoric factors were important in the observed binding: (a) the hydrogen-bonding interactions by the residues Arg 271, Arg 275 Tyr 296. Thr231 and Ala 286 and (b) the hydrophobic pocket residues Met 268, Met 272, Met 269, Phe 285, and Leu 308. The binding affinities of the selected limonoids in the EcR pocket compared well with the observed larvicidal activity as reported earlier and in the literature. This study offers an opportunity to develop structurally simpler and specific receptor targeted larvicides against Aedes aegypti L.

Sciences of Phytochemistry