Indonesian Journal of Pharmacy
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    The Effect Formulation on The Activity of Catechins as A Sunscreen and Skin Lightening

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    Catechins are found in many plants, one of which comes from gambier. The stability of catechins which is affected by pH and temperature also affects the activity test after being made in dosage form. This study aims to see the effect of catechin formulations in the form of gel and nanoemulsion on the activity of sunscreen and skin lightening. Tests carried out in vitro included antioxidant activity tests using the DPPH method and B16F0 cell viability against catechins, determination of Sun Protecting Factor (SPF), Protection grade UVA (PA), tyrosinase and melanogenesis inhibition using the spectrophotometric method of catechin formulas in the form of gel and nanoemulsion dosage forms. The results showed that catechins have very strong antioxidant activity with an IC50 of 16.421 µg/mL, not toxic to B16F0 cells up to a concentration of 200 µg/mL. Catechins gel and nanoemulsion dosage forms have good stability during storage. The formulation had a significant effect (p<0.05) on the value of SPF, PA, percentage of tyrosinase, and melanogenesis inhibition. Catechins in the form of nanoemulsion formulation provide better sunscreen and skin lightening activity than those in gel dosage forms

    One-Pot Synthesis and Biological Evaluation of Piperidinium-3,3'-(arylmethylene) bis-lawsone derivatives by targeting caspase-7

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    Caspase-7, an effector enzyme activated by the initiator caspase-1, plays a crucial role in triggering apoptosis. It is also a significant factor in neurodegenerative conditions like Alzheimer's and Huntington's diseases. While both peptide and nonpeptide caspase inhibitors have shown promise in preclinical research, peptide inhibitors face challenges such as poor cell permeability, brief half-life, limited efficacy, and complex structures that are difficult to optimize. Additionally, they encounter bioavailability issues. Consequently, the development of nonpeptide-based caspase inhibitors remains an area of interest for researchers. Using a multicomponent reaction, eight lawsone derivatives, specifically piperidinium-3,3'-(arylmethylene) bis-lawsone, were successfully synthesized. This group included five novel compounds (2, 3, 4, 7, 8) and three previously known ones (1, 5, 6). The products were analyzed using Nuclear Magnetic Resonance (NMR) 1-2D spectroscopy and High Resolution Mass Spectrometry (HRMS), followed by an evaluation of their inhibitory activity against caspase-7. Notably, this study marks the first instance of piperidinium-3,3'-(arylmethylene) bis-lawsone being investigated for its potential to target the caspase-7 enzyme. Among the eight compounds, compound 8 demonstrated the most promising results, exhibiting an inhibitory activity of approximately 29.80% against caspase-7. This finding suggests that compound 8 could serve as a valuable fragment molecule for future development of caspase-7 inhibitors

    Methyleugenol enhances the anticancer effect of chemotherapeutic drug and boosts chemotherapy drug tolerance

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    Chemotherapy plays an important role in treating lung cancer. Chemotherapy drugs usually have good therapeutic effect, but due to the side effects, the dose needs to be considered. The use of non-toxic adjuvant natural product combined with chemotherapy drugs will be an important treatment mode in the future. The purpose of this study is to use non-toxic natural product (methyleugenol) to increase the therapeutic effect of chemotherapeutic agent (doxorubicin) on lung cancer and investigate the toxic effect of methyleugenol combined with chemotherapeutic agents on drug-resistant lung cancer cells. Methyleugenol combined with doxorubicin treated lung adenocarcinoma A549 cell line and established drug-resistant lung adenocarcinoma cell line (A549DoxR) were used in the study.    The methods including proliferation assay, cell wound healing assay, colony formation assay, DNA fragmentation assay, gelatin zymography assay, comet assay, reverse transcriptional polymerase chain reaction (RT-PCR), and western blot were adopted. The results showed methyleugenol significantly enhanced doxorubicin inhibited the cell growth, the cell colony formation, the cell migration, and the metastasis of A549 cells and A549DoxR cells. Methyleugenol strengthened doxorubicin to induce apoptosis and autophagy of A549 cells and A549DoxR cells. Methyleugenol can significantly enhance the treatment effect of chemotherapy drugs in lung cancer and strengthened the toxic effect of chemotherapy drugs on drug-resistant lung cancer cells. Methyleugenol can be developed to be used as an adjuvant to assist Chemotherapy drugs s and is targeted to clinically treat patients with multidrug resistance.   &nbsp

    Formulating of moringa oil microemulsion used Surfactant Poly Ethylene Glycol 40 Hydrogenated Castrol Oil and Co-Surfactant of Glycerin

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    Moringa seed oil contains oleic acid that benefits the skin. It has anti-inflammatory and skin moisturizing properties. Increasing effectiveness: Moringa oil is made into a microemulsion. The microemulsion system consists of Moringa oil, S-mix (Polyethylene Glycol 40 Hydrogenated Castor Oil as a surfactant and glycerine as a co-surfactant), and water. The microemulsions are formulated by a titration method and create a pseudo ternary phase diagram with S-mix (Surfactant: Co-surfactant) at 3:2, 1:1, and 2:3. The most optimized moringa oil microemulsion formulation was subjected to characterized such as organoleptic properties, %Transmittance, pH, viscosity, stability, particle globule size, zeta potential, and polydispersity index (PdI). The construction of a pseudo-ternary phase diagram and the titration methods constituted a suitable technique for preparing microemulsions, as most formulations were transparent. It was found that S-Mix (1:1) has a broad area with the oil phase in the range of 4.0% - 8.3%, S-Mix in the range of 48.0%-66.7%, and water in the field of 25.0-48%. The pH is in the range of 5.91-7.64. Meanwhile, the viscosity is in the range of 60-992cPs. The decline in oil and S-mix concentration reduces the pH value and viscosity. They are stable after the thermodynamic test, freeze-thaw cycling test, and after being kept at room temperature for one month. According to these findings, the microemulsion of moringa oil using PEG 40 Hydrogenated Castor Oil and Glycerine formulation might serve as a suitable drug delivery system

    Physicochemical evaluation and delayed aging activity of the cream containing aloe vera and rosella extracts

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    Anti-aging cream is a cosmetic product that prevents premature aging. Aloe vera and rosella have been reported to exhibit various pharmacological activities, including anti-aging. Meanwhile,  the use of a combination of these two natural products has not been widely reported. This research aims to determine the potential antioxidant and anti-collagenase activities of the combination of aloe vera and rosella in cream products. This study analyzed the quality of cream according to physical parameters, cream chemical content, antioxidant activity, anti-collagenase, and sunscreen protection factor (SPF) test of cream products. The cream formulas had white to pink colors, were semi-solid, homogeneous, and had an O/W emulsion type. Total polysaccharide content in the cream ranged from 0.73% - 0.83%, o-acetyl polysaccharide content ranged from 1.36%-3.53%, flavonoid content ranged from 2.95×10-6-6.50×10-6 g QE/g, anthocyanin content ranged from 4.57-35.94 mg/kg, phenolic content ranged from 5.06×10-6-9.42×10-6 g GAE/g. The radical scavenging, anti-collagenase activities, and SPF value of cream formulas ranged from 22.14%-50.36%, 6.85%-54.66%, and 8.21±0.01-8.73±0.02, respectively. According to all test results, the recommended cream product is C formula (1:1). Cream containing aloe vera gel and rosella flower extracts are potentially to be developed as anti-aging cream product.&nbsp

    Formulation of Cinnamon Essential Oil (Cinnamomum burmannii) and Clove Essential Oil (Syzygium aromaticum) Nanoemulsion-Based Liquid Soap

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    Soap is a cosmetic that acts as a cleaning agent, to protect the body from various diseases, such as skin diseases caused by bacteria and fungi. One of the bacteria that causes infection is Staphylococcus aureus. The eugenol content in cloves and cinnamaldehyde in cinnamon can inhibit the growth of bacteria. This research aims to determine the liquid soap formulation based on a nanoemulsion combination of clove and cinnamon essential oils that meets the physicochemical characteristics and its activity in inhibiting the growth of S. aureus bacteria using the diffusion method. The research results showed that clove and cinnamon essential oils had antibacterial activity, with the concentration of clove essential oil used being 2% and cinnamon essential oil 3%. Then it was formulated into a nanoemulsion with a composition ratio of Tween 80 and PEG 400 as the most optimal surfactant and cosurfactant of 40:10. The nanoemulsion is formulated into liquid soap where the nanoemulsion combination of clove and cinnamon essential oils is added to the liquid soap base. The resulting liquid soap has good physicochemical properties and meets the requirements

    Liposomal Formulation of Plant Based Natural Photosensitisers for Thrombosis

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    Photothermal and photodynamic therapy (PTPDT) in medical field continue to evolve due to their relatively low adverse effect and high efficiency for therapeutic application. Photosensitisers compounds have shown excellent ability in inducing mild hyperthermia and generation of reactive oxygen species (ROS) which is beneficial for thrombolysis. Herein, we explored plant-based sources rich in pigments such as beet root (BR), butterfly pea flower (BPF), red cabbage (RC), purple sweet potato (PSP) and phycocyanin (PHY) as natural photosensitisers (NPS) candidates for the treatment of thrombosis. We were able to produce extracts with strong absorption within the 400-800 nm wavelength range, the ideal window for photosensitisation. The photosensitising ability of the NPS were confirmed after significant photothermal increase was achieved after 5 minutes low intensity exposure with 450 nm and 550 nm lasers. Extract from BPF, RC, BR and PHY were the most promising and further formulated into liposomes. Through in vitro thrombolytic activity on human blood clots, we confirmed thrombolytic capability of NPS comparable to that of nattokinase. Liposomal formulation of the best NPS (Lip-PHY and Lip-BPF) produced particles of ~168.3 and 215.9 nm respectively, with good encapsulation efficiency and stability. Ultimately with this study, we have demonstrated liposomal formulation of NPs and their strong potential as thrombolytic agent

    Effect of Methyl Jasmonic Acid and Tryptophan on Increasing Vincristine Content of Leaf Cell Suspension Culture Catharanthus roseus (L.) G. Don.

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    Catharanthus roseus (L.) G. Don known as tapak dara is a medicinal plant that produces alkaloid compounds such as vincristine as an anticancer which has very high economic value and is produced in very small concentrations. This study aims to increase the levels of vincristine in cell suspension cultures of tapak dara leaves by administering methyl jasmonic acid and tryptophan with various concentrations. Tapak dara leaf explants were grown on solid Murashige-Skoog (MS) media supplemented with the addition of 2.4 D 1 mg/L growth regulator and 4 mg/L kinetin. The callus was subcultured and then suspension culture was carried out on liquid MS medium by administering methyl jasmonic acid and tryptophan with various concentrations. Callus growth was carried out by weighing the fresh weight and dry weight of the callus. The vincristine content and assay were analyzed using High Performance Liquid Chromatography (HPLC). Callus growth in cell suspension cultures with X50Y300 treatment resulted in the highest fresh weight of 1.094 g, while the highest dry weight was found in treatment X75Y200 of 0.166 g. The results of the HPLC analysis showed that the administration of methyl jasmonic acid and tryptophan with various concentrations on tapak dara leaf cell suspension cultures were able to produce vincristine compounds. In treatment, X50Y100, X75Y100, X100Y100, X50Y200, X75Y200, and X75Y300 were able to increase vincristine levels, but the X100Y200, X50Y300, and X100Y300 treatments decreased vincristine levels. The highest levels of vincristine were found in treatment X50Y200 (50 mg/L tryptophan and 200 μM methyl jasmonic acid ) which was 49.311 ppm . &nbsp

    Assessing Neurobiological and Behavioral Responses in Rats: Modified UCMS Protocol with Psychological Stress Device

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    The antidepressant effect of drugs can be tested using various methods, including unpredictable chronic mild stress (UCMS). Although the initial UCMS protocol involved administering stressors for 21 days, many modifications have been made, one of which is shortening the duration of the stressors to 10-15 days. This study aims to modify the UCMS model to increase the stress response in male Wistar rats. UCMS protocol in this study did not use predator odor (2,5-dihydro-2,4,5-trimethylthiazoline) as in the previous protocol, but a psychological stress device (PSD) was used instead. Forty male Wistar rats (150-200 grams) were given UCMS treatment for 10 and 15 days. Sucrose consumption, coat score, body weight, and serum corticosterone levels were measured. Immunohistochemical examination of 5-HT1A receptors, TNF-α, NOX2, and NF-ĸB were performed in the hippocampus part of the brain. All data were analyzed using the Mann-Whitney test. UCMS treatment for 10 and 15 days reduced sucrose consumption and body weight and increased the coat score. UCMS treatment increased corticosterone levels, decreased 5-HT1A receptor expression, and increased TNF-α, NOX2, and NF-ĸB expression. The primary behavioral response during PSD was head dip as a preparatory behavior for jumping. Modifying the UCMS model using a PSD can increase the stress response. Keywords: animal model, depression, unpredictable chronic mild stress, psychological stress devic

    Anti-Acne Mushrooms: A Review

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    Acne is a common chronic inflammatory skin disease in which the skin pores are clogged with oil and dead skin cells. Acne is the second most common skin disease after dermatitis. Many factors influence the appearance of acne, such as skin disease, environmental hygiene, lifestyle, androgen hormones, inflammation, and stress, including the surface microflora of the skin and the colonization of acne-causing bacteria. Mushrooms are now offered as an alternative and complementary therapy for acne. This review aimed to evaluate natural sources of fungal origin for preventing and treating acne caused by bacteria. This review presents the application of several mushrooms in the management of acne. Electronic databases such as Web of Science, PubMed, Scopus, and Google Scholar were reviewed to identify the anti-acne effects of mushrooms. Based on the literature review results, it can be concluded that mushrooms have good potential as anti-acne by providing barriers to the growth of acne-causing bacteria, namely S. aureus, S. epidermidis and P. acnes. The ethanol extract of Shitake mushroom (Lentinula edodes) showed activity on P acnes and S epidermidis bacteria with an average inhibition zone of 13.4 mm and 15.33 mm, and was the most sensitive with a MIC value of 256 πg/mL. Warm water extract and Tris buffer extract of the Black Ear fungus Auricularia polytricha) showed activity on S. aureus bacteria with an average inhibition zone of 11.66 mm and the most sensitive with a MIC value of 5 πg/mL. At the same time, the hexane extract and methanol extract of red ear mushrooms (Auricularia auricula Judei) showed activity on S. aureus bacteria with an average inhibition zone of 28.6 mm and 25.3 mm and a sensitive MIC value of 0.78 mg/mL. In conclusion, several fungi can be used to manage acne caused by bacteria. &nbsp

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