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   2021| January-March  | Volume 12 | Issue 1  
    Online since January 9, 2021

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Infrared spectroscopy technique for quantification of compounds in plant-based medicine and supplement
Effan Cahyati Junaedi, Keri Lestari, Muchtaridi Muchtaridi
January-March 2021, 12(1):1-7
Quality control of plant-based medicine and supplements must be carried out to ensure uniformity in quality and safety in their use, resulting in the need for effective and accurate analytical methods. Infrared spectroscopy is a method of qualitative and quantitative analysis that is fast, time-saving, cost-effective, accurate, and nondestructive. This method has been applied for quantitative analysis of compounds in complex matrices such as plant-based medicine and supplements supported by chemometrics techniques. The success of infrared spectroscopy applications for quantitative analysis of phytochemicals and adulterants content in plant-based medicine and supplement can happen by several factors. This article highlights the effect of spectral preprocessing and variable selection on quantitative analysis of phytochemical and adulterant in plant-based medicine and supplements using infrared spectroscopy. Literature search was conducted with PubMed, Google Scholar, and Science Direct by selecting quantitative analysis research on plant-based medicines and supplements that utilize spectral preprocessing techniques and variable selection in processing data analysis. The preprocessing spectra and variables selection can affect the accuracy and precision of infrared spectroscopy methods. The variable selection can be done using the wavenumber point technique, the wavenumber interval, or a combination thereof. Variable selection is more commonly used for near-infrared data than for IR data. The optimization of the preprocessing spectra and variables selection technique will be useful in increasing the ability of infrared spectroscopy in predicting compound levels.
  5,454 1,085 3
The antiaging property of aqueous extract of Millingtonia hortensis flowers in aging neuron
Pichaya Jumnongprakhon, Decha Pinkaew, Pravaree Phuneerub
January-March 2021, 12(1):14-21
Cellular senescence is the key mediator of cellular dysfunction before undergoing degenerative disease such as Alzheimer's disease. The aging process was mainly by the overactivation of senescence associated β-galactosidase (SA-β-gal) enzyme before mediated several negative responses, including intracellular reactive oxygen species (ROS) production, cellular senescence regulation, and death prior encourage synaptic loss. Thus, in the recent work, we evaluated the in vitro effects of aqueous extract of Millingtonia hortensis L. (MH) from flower in hydrogen peroxide (H2O2)-induced senescence in SK-N-SH cells. Herein, we demonstrated that MH significantly increased cell viability and decreased both of apoptotic cells and ROS production in a dose-dependent manner comparing to aging group (P < 0.01) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, flow cytometry, and ROS assay. Furthermore, the number of SA-β-gal-positive cells was also reduced in MH treatment (P < 0.01) together with the promotion of Sirt-1 protein. Importantly, MH also promoted the synaptic plasticity by decreased acetylcholinesterase activity and increased synaptophysin expression in aging neurons comparing to aging group (P < 0.01). Hispidulin (the active ingredient in MH) was also revealed the similarly effects to MH. Therefore, we suggested that MH might be beneficially for neurodegenerative disease that caused by aging.
  5,233 414 -
In vitro cytotoxic, genotoxic, and antityrosinase activities of Clitoria macrophylla root
Yamon Pitakpawasutthi, Maneewan Suwatronnakorn, Somchai Issaravanich, Chanida Palanuvej, Nijsiri Ruangrungsi
January-March 2021, 12(1):8-13
Clitoria macrophylla Wall. (Leguminosae), locally known as Non-tai-yak or An-chan-pa, commonly distributed in tropical nations and Southeast Asia. Regarding traditional Thai medical system, C. macrophylla roots carry out a potential in dermatology. Its roots are also used as insecticide in agriculture and animal farming. Moreover, clitoriacetal is the major component that can be detected in C. macrophylla root. This research aimed to assess the efficacy of C. macrophylla root extract and clitoriacetal for its anticancer and antityrosinase activities as well as to assess in vitro safety potential for its cytotoxic and genotoxic effects. C. macrophylla root and clitoriacetal were tested by brine shrimp lethality, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, comet assay, and antityrosinase activity. C. macrophylla root, clitoriacetal, and rotenone demonstrated the toxicity against brine shrimp nauplii with LC50 of 332.15, 136.54, and 0.15 μg/mL, respectively. C. macrophylla root and clitoriacetal showed cytotoxic potential against breast ductal carcinoma (BT-474), liver hepatoblastoma (Hep-G2), and colon adenocarcinoma (SW-620). At 100 μg/mL, the percent DNA damage of C. macrophylla root and clitoriacetal was 37.84% and 36.01%, respectively. C. macrophylla root and clitoriacetal were able to inhibit the tyrosinase enzyme with IC50 of 12.27 and 7.30 mg/mL, respectively, which less effective than glutathione (positive control). The present study revealed the in vitro biological activities of C. macrophylla root and its clitoriacetal constituent which proposed the scientific evidences in efficacy and safety evaluation including in vitro cytotoxicity, DNA damage as well as antityrosinase activities.
  3,164 436 1
Characteristics of fatty acid composition and minor constituents of red palm olein and palm kernel oil combination
Marline Nainggolan, Ahmad Gazali Sofwan Sinaga
January-March 2021, 12(1):22-26
Red palm olein (RPOl) is one of the derivatives of palm oil. It contains a high composition of unsaturated fatty acids such as oleic and linoleic, whereas palm kernel oil (PKO) contains more saturated fatty acids of lauric acid. RPOl provides high nutrient contents such as squalene, Vitamin E, and carotene, whereas PKO that is rich in lauric acid can fight Gram-positive microorganisms. This research aims to study the chemical characteristics of RPOl, PKO, and the combination. A combination of RPOl with four different concentrations of PKO (20%, 50%, 80%, and 100%) was analyzed to obtain the composition of fatty acids, squalene content, Vitamin E levels, total carotene, and saponification numbers. RPOL contains high levels of squalene, Vitamin E, and total carotene, followed by RPOl and PKO combination of oil, with a higher percentage of RPOl in its composition. The increase of the PKO level added to the combination will decrease the saponification number and increasing the acid number. Therefore, it can be concluded that RPOl could be the source of squalene, Vitamin E, carotenoids, and oleic acid, whereas PKO is the largest source of lauric acid.
  2,882 556 2
Modification of Anti-acne Bawang Dayak (Eleutherine bulbosa (Mill.)Urb.) Cream to Propionibacterium acnes
Syahrida Dian Ardhany, Candra Dwi Putra, Susi Novaryatiin
January-March 2021, 12(1):94-98
Bawang dayak is one of the traditional medicines in Central Kalimantan, used to treat acne vulgaris. Previous research reported that a cream made with bawang dayak extract's active ingredient could inhibit Propionibacterium acnes' growth. However, bawang dayak has a pungent odor that causes discomfort, where the cream separates after 3 days of storage, which decreases its potency. This study aims to improve the quality of the anti-acne cream formulation of bawang dayak extract from previous studies with the addition of cinnamon, honey, and peppermint. The modified formula of bawang dayak extract cream was evaluated and tested for its antibacterial activity in vitro. The results showed an increase in the organoleptic test, especially the smell, which gave a more comfortable fragrance than the previous formula. The pH measurement of the cream shows the results suitable for topical applications. However, the homogeneity observations show that all the formulas are homogeneous, seen from uniform colors but contain coarse grains. The antibacterial activity test of all cream formulations against P. acnes showed inhibition zone diameter between 14.85 and 17.10 mm, all of which were moderate and larger than previous studies. It can be concluded that the modification of the cream formula with the active ingredient of bawang dayak extract showed an increase in the inhibition zone against P. acnes and improved organoleptic properties.
  1,978 336 1
Assessment of potential drug interactions among psychiatric inpatients receiving antipsychotic therapy of a secondary care hospital, United Arab Emirates
Haneen A. R. Aburamadan, Sathvik Belagodu Sridhar, Talaat Matar Tadross
January-March 2021, 12(1):45-51
The majority of the antipsychotic drugs are also known to interact with other co-administered drugs. Drug–drug interaction (DDI) reports among patients receiving antipsychotic medications are common. The study aims to identify the potential drug–drug, drug–tobacco, and drug–ethanol interactions associated with antipsychotics and significant predictors of potential DDIs (pDDIs). A prospective observational study was conducted among psychiatric inpatients receiving antipsychotic therapy and met the inclusion criteria that were reviewed for the presence of pDDIs using DRUGDEX-Micromedex database 2.0. The identified pDDIs were graded according to the severity and type of documentation. A total of 110 patients had a minimum of a single interaction, and the overall frequency of pDDIs reported was 64.7%. Of 158 pDDIs, 92 interactions (58.2%) were of major severity, while 66 interactions were of moderate severity (41.8%). Olanzapine with valproate (40 [25.3%]) was the most commonly documented pDDIs, followed by risperidone with valproate (20 [12.6%]). Olanzapine with tobacco (20 [69%]) was the most common drug–tobacco interaction. Simultaneously, olanzapine with ethanol was the most common potential drug and ethanol interaction (9 [50%]). Variables such as the number of drugs and polypharmacy statistically significantly predicted pDDIs (F[7, 162] = 8.155, P < 0.05, R2 = 0.26). Knowing the severity of different pDDIs will help clinicians and prescribers monitor patient safety through regular monitoring for interactions and adverse drug effects in future. The number of medications and polypharmacy was found to be the most significant predictor of pDDIs.
  1,936 336 3
Cytotoxicity and proliferation evaluation on fibroblast after combining calcium hydroxide and ellagic acid
Intan Nirwana, Elly Munadziroh, R Mohammad Yogiartono, Candrika Thiyagu, Chong Sin Ying, Aristika Dinaryanti
January-March 2021, 12(1):27-31
Calcium hydroxide induces chronic inflammation and pulp tissue necrosis due to its high pH value. Ellagic acid is an anti-inflammatory and antioxidant flavonoid. Therefore, the effect of combining calcium hydroxide and ellagic acid must be researched to reduce cell damage due to the application of calcium hydroxide. The objective of the study was to determine the cytotoxicity and proliferation of fibroblasts after combining calcium hydroxide and ellagic acid with ratios of 99:1, 98:2, 97:3, 96:4, and 95:5. Calcium hydroxide and ellagic acid with different ratios were mixed with water and stirred. Rat gingival fibroblasts were prepared and incubated in two 96-well microplates. The control group and treatment groups (16 samples) were placed in the microplate and incubated for 1 and 3 days. An MTT assay test was performed, and the absorbance was observed using the ELISA reader with a wavelength of 540 nm. Following that, the cell viability was calculated. The results were tabulated and analyzed using a one-way ANOVA. For all treatment groups, the fibroblast cells showed a viability of higher than 50%. There was a significant increase (P < 0.05) in the fibroblast cell proliferation after combining calcium hydroxide and ellagic acid with ratios of 99:1 and 97:3. The combination of calcium hydroxide and ellagic acid is nontoxic. The treatment groups with ratios of 99:1 and 97:3 showed increased fibroblast cell proliferation.
  1,832 383 5
Antidiabetic and anticancer activity of Chinese water chestnut (Eleocharis dulcis) extract with multistage extraction
Ace Baehaki, Indah Widiastuti, Susi Lestari, Masruro Masruro, Hemi Adi Putra
January-March 2021, 12(1):40-44
The aims of this research were to observe yield extract, phytochemical content, the antidiabetic and anticancer activity of Chinese water chestnut. This research method used an experimental laboratory, and data analysis was carried out descriptively. The stages carried of this research are sample extraction, extract yield, phytochemical analysis (flavonoid and phenolic content), antidiabetic, and anticancer activity. The results showed that the yield of extract using ethanol on Chinese water chestnut was higher than that extracts using n-hexane and ethyl acetate solvents. Phenolic and flavonoids compounds are polar so that the results of extracts with ethanol solvents show higher values than that extracts using n-hexane and ethyl acetate solvents. The result of antidiabetic activity has the highest value at a concentration of 2000 ppm using ethanol value of 65.74%. The results of the anticancer activity were expressed by (IC50), the IC50 value of the n-hexane extract was 1.231.74 ppm, ethyl acetate 941.04 ppm, and ethanol 2.261.90 ppm.
  1,905 300 3
The effect of coating chitosan on Porphyromonas gingivalis biofilm formation in the surface of orthodontic mini-implant
Haru Setyo Anggani, Renaldo Guruh Perdana, Erwin Siregar, Endang Winiati Bachtiar
January-March 2021, 12(1):84-88
Infection is the main problem for the failure of orthodontic mini-implant. Modern prevention of infection is now focused on local antibacterial coatings on implant devices. Chitosan is biocompatible and has antibacterial properties. Azithromycin is a synthetic antibiotic with immunomodulatory properties in which it has an advantage over the rest of antibiotics. This study aimed to evaluate the effect coating chitosan on the orthodontic mini-implant in Porphyromonas gingivalis biofilm formation. This is an experimental study using 25 orthodontic mini-implants. Five samples were coated with chitosan, 5 samples were coated with chitosan–azithromycin, 5 samples were coated with azithromycin, 5 samples were uncoated, and 5 samples were uncoated and were not exposed to P. gingivalis. P. gingivalis biofilms on the surface of the orthodontic mini-implant were observed after 24 h of incubation. P. gingivalis biofilm mass inhibition was highest in the azithromycin-treated group, followed by chitosan + azithromycin and chitosan only. The one-way ANOVA statistic test and post hoc Bonferroni statistic test of P. gingivalis biofilm mass show a significant difference between and within groups of experiments (P < 0.05). The Pearson correlation test with a value of R = +0.88, indicated that the bacterial viability count and the biofilm mass have a strong positive correlation. In conclusion, orthodontic mini-implant coated with chitosan, chitosan with azithromycin, or azithromycin only effectively suppressed P. gingivalis biofilm formation.
  1,766 291 2
Evaluation of the stability and antibacterial activity of crude extracts of hydro-endophytic fungi
Surachai Techaoei, Khemjira Jarmkom, Thisakorn Dumrongphuttidecha, Warachate Khobjai
January-March 2021, 12(1):61-66
The production and screening of secondary metabolites of four hydro-endophytes isolated from lotus, and the stability of bioactive compounds was evaluated. Surface-sterilized technique was used to isolate the endophytic fungi (EF) on potato dextrose agar and identified by using morphological and molecular techniques. The extracts were tested for anti-microbial activity against methicillin-resistant Staphylococcus aureus (MRSA) DMST20651, Streptococcus mutans (SM) DMST18777, Staphylococcus epidermidis (SE) ATCC12228, Pseudomonas aeruginosa (PA) TISTR1467, and Propionibacterium acnes (PN) DMST14916. The bacteriostatic and bactericidal activities were determined. Finally, thermal and ultraviolet (UV) stability was evaluated. Four endophyte isolates (EF 14, EF36, EF53, EF58, and EF60) produced secondary metabolites and showed activity against MRSA, SM, SE, PA, and PN, respectively. The crude ethyl acetate (EtOAc) and methanol (MeOH) extract of EF14 showed activity against MRSA with the inhibition zone of 9.00 ± 0.00 and 7.50 ± 0.50 mm, and minimum inhibitory concentration was 4.80 and 4.90 mg/mL, respectively. The minimum bactericidal concentration was 9.60 mg/mL. Whereas, the crude EtOAc and MeOH extract EF60, which were extracted by EtOAc and MeOH, showed inhibition zone of SE as 12.33 ± 0.57 and 12.33 ± 0.57 mm, respectively. Crude EtOAC extracts of EF14 showed highest thermal stability at 55°C–121°C, and UV stability with MRSA and SE, respectively. The results showed that the EtOAc extracts of EF could be potential antibacterial pathogens and displayed UV-thermal stability. This information is beneficial for future investigations, since some bioactive compounds have potential as anti-resistant strains of some bacterial pathogens.
  1,671 276 2
Antibiofilm effect of C-10 massoia lactone toward polymicrobial oral biofilms
Diyah Tri Utami, Sylvia Utami Tunjung Pratiwi, Herman P Spaink, Tetiana Haniastuti, Triana Hertiani
January-March 2021, 12(1):89-93
This study is aimed to test the efficacy of C-10 Massoia lactone in oral polymicrobial degradation. Polymicrobial of Streptococcus sanguinis, Streptococcus mutans, Lactobacillus acidophilus, and Actinomyces viscosus were studied. C-10 Massoia lactone against biofilm degradation was investigated using modified crystal violet for biofilm staining. The effectiveness of C-10 Massoia lactone against biofilms was calculated by the minimum biofilm inhibitory concentration (MBIC50) and the minimum value of biofilm eradication concentration (MBEC50). Scanning electron microscope was used to study biofilm cell viability and morphological changes. The results showed a degradation effect of C-10 Massoia lactone against mature oral polymicrobial at 0.25% v/v. C-10 Massoia lactone can degrade polymicrobial biofilms of S. mutans, S. sanguinis, L. acidophilus and A. viscosus. This compound can destroy the extracellular polymeric substances (EPS) of polymicrobial biofilms. The potential application of C-10 Massoia lactone for anti-polymicrobial medication should be applied in such a way that any negative effects are minimized. Further research is needed to confirm the findings of this study.
  1,682 253 -
Effect of water reservoirs types on the prevalence and antibiotic resistance profiles of Pseudomonas aeruginosa isolated from bathroom water in hospitals
Sri Agung Fitri Kusuma, Tina Rostinawati, Rini Hendriani, Muhammad Faisal Budiman, Ida Parwati
January-March 2021, 12(1):52-56
This study was aimed to isolate and characterize Pseudomonas aeruginosa antibiotic resistance profiles that isolated from bathroom water of five hospitals in Bandung, Indonesia, with different types of water reservoirs. Total of 25 water samples from bathrooms of five hospitals were collected and analyzed for the existence of P. aeruginosa colonies on the surface of MacConkey agar media using a streak plate method and identified using phenotypic identification and a series of biochemical tests. All P. aeruginosa isolates were tested against ceftazidime, piperacillin/tazobactam, ciprofloxacin, meropenem, and gentamicin containing in paper disc, using the agar diffusion method. Of all samples, the total number of P. aeruginosa isolates was less than that of non-P. aeruginosa. In hospitals that use permanent bathtubs, a greater total bacterial count was obtained than those using pails. From 110 isolates, 14.54% were multidrug resistance antibiotics. The majority of the resistant isolates were from hospital B with permanent bathtubs. Of 25 isolates from that hospital, P. aeruginosa isolates were resistant to ceftazidime (20%), piperacillin/tazobactam (4%), ciprofloxacin (20%), and gentamicin (20%). The multiple antibiotic resistance index value of P. aeruginosa isolates was 0.4–0.6. Thus, it can be concluded that the bathroom wáter in the hospital with permanent bathtubs were potential reservoirs of antibiotic-resistant P. aeruginosa.
  1,705 209 4
Role of dyslipidemia in the development of early-onset preeclampsia
Thabat J Al-Maiahy, Ali I Al-Gareeb, Hayder M Al-Kuraishy
January-March 2021, 12(1):73-78
Preeclampsia (PE) is a gestational-related disease presented with hypertension, peripheral edema, and proteinuria after 20 weeks of gestation. In PE, there are various metabolic changes like dyslipidemia. In addition, both PE and dyslipidemia are associated with changes of platelet indices. Thus, objective of the current study was to illustrate the potential role of dyslipidemia and platelet changes in pregnant women with PE. This case–control study involved 37 preeclamptic pregnant women as compared to 24 healthy pregnant women as controls. Blood pressure profile, lipid profile, proteinuria, and platelet indices were measured. Blood pressure profile was higher in preeclamptic pregnant women as compared to the controls (P < 0.01). There was a significant dyslipidemic status in preeclamptic pregnant women compared with the controls (P < 0.01). Platetetcrit (PCT) and platelet count (PC) were lower in preeclamptic pregnant women compared with the controls (P = 0.001). On the other hand, platelet distribution width (PDW), mean platelet volume (MPV), and platelet-large cell ratio (P-LCR) were higher in the pregnant women with PE as compared with the controls (P = 0.001). PCT and PC were insignificantly linked, while P-LCR, MPV and PDW were significantly correlated with total cholesterol, triglyceride, low-density lipoprotein (LDL)/high-density lipoprotein (HDL) ratio, systolic blood pressure, DBP, and MAP in preeclamptic patients compared with women of normal pregnancy. Both dyslipidemia and alterations in the platelet indices are correlated with blood pressure profile in PE. High MPV and PDW in association with high LDL/HDL ratio in pregnant women herald risk of PE.
  1,649 231 1
Natural product of gambier (Uncaria gambier Roxb) extracts to counter against hepatotoxicity effects due to monosodium glutamate induction in male mice
Yunita Sari Pane, Yetty Machrina, Sufitni Hasan, Fitriani Lumongga, Yuki Yunanda
January-March 2021, 12(1):104-108
Monosodium glutamate (MSG) is often added in foods to enhance the flavor. It has adverse effect to body organs. Natural remedies, such as: gambier have been known for generations used to improve health. Substances contained in gambier, i.e.: catechins are believed to reduce the occurrence of hepatotoxicity. The study aims to analyze the effects of gambier in reducing the hepatotoxicity of MSG. This study with a posttest only control group design. Mice amount 25 (5 groups, n = 5/group). All interventions are given orally for 4 weeks. At the end of the study, it carried out euthanasia taken the liver of mice to made histopathology preparations then examine by light microscope, ×400, ×5 view field. Liver damage was found in each group with various levels of histological appearance:(I) 2 normal, 2 minimal, 1 moderate and none severe; (II) none normal, 1 minimal, 3 moderate and 1 severe; (III) 1 normal, 4 minimal, none moderate and severe;, (IV) 2 normal, 3 minimal, none moderate and severe; and (V) 4 normal, 1 minimal, none moderate, and severe. The data were analyzed using Kruskal–Wallis test. The level of liver damage among all groups was significantly different (p = 0.017). The same on the Dunn test also showed the level of liver damage in Group-II to compare with other groups (p < 0.05). The present study proves that Gambier (Uncaria gambier Roxb) can reduce occurrence of hepatotoxicity caused by MSG.
  1,659 210 -
Bovine sponge amnion stimulates socket healing: A histological analysis
Tabita Imaniar Faadhila, Martha Nadila Valentina, Elly Munadziroh, Intan Nirwana, Helal Soekartono, Meircurius Dwi Condro Surboyo
January-March 2021, 12(1):99-103
Bovine sponge amnion (BSA) is made from bovine amniotic membrane, which contains several growth factors with the ability to suppress inflammation and stimulate the healing process. The healing process of the socket is clinically marked by the proliferation of fibroblasts, formation of new blood vessels, and closure of the wound site. Fibroblasts and new blood vessels are the common histological indicators of tissue regeneration. Twenty-four lower anterior teeth were extracted from the rats. The socket was then applied with BSA and sutured, while a control group was only sutured. The animals were scarified 3, 7, and 14 days after application, and the mandibular was isolated. Histological analysis of socket tissue used the staining of hematoxylin and eosin to analyze the new blood vessels and fibroblasts. An independent t-test was used to analyze the fibroblasts and new blood vessels in each group, with P < 0.05 considered as significant. The number of fibroblasts is higher in the BSA group compared others groups at 3, 7, and 14 days (P < 0.05). The new blood vessel count is higher compared to the control group at only 3 and 7 days (P < 0.05). BSA aids the regeneration of the socket after tooth extraction by stimulating fibroblast proliferation and formation of new blood vessels.
  1,566 278 2
Synergistic effect of ampicillin and dihydrobenzofuran neolignans (myticaganal C) identified from the seeds of Myristica fragrans Houtt. against Escherichia coli
Kanokrat Keawchai, Parinuch Chumkaew, Patima Permpoonpattana, Theera Srisawat
January-March 2021, 12(1):79-83
The present study was designed to enhance the antibacterial activity of ampicillin against Escherichia coli by combining it with myticaganal C. Antibacterial activity of ampicillin combined with myticaganal C against E. coli was assessed by agar well diffusion. Minimum inhibitory concentrations (MICs) and synergy by checkerboard assay of ampicillin and myticaganal C were assessed by resazurin-based 96-well microdilution. Bacterial responses were assessed by flow cytometry. Ampicillin in combination with myticaganal C showed better zone of inhibition (31.67 ± 0.58 mm) than myticaganal C or ampicillin alone. MIC of ampicillin was found to be 12.5 μg/mL, but myticaganal C was ineffective against E. coli. Myticaganal C (8000 μg/mL) with ampicillin (0.0975 μg/mL) exhibited strong synergy, so the need for ampicillin was reduced 128-fold. Combination inhibited E. coli by acting on cell membrane and by granularity disruptions. These findings indicate that myticaganal C enhances the potential of ampicillin against E. coli, thus providing an effective alternative to deal with the problem of bacterial resistance.
  1,646 188 1
S-deoxydihydroglyparvin from Glycosmis parva inhibits lipopolysaccharide induced murine macrophage activation through inactivating p38 mitogen activated protein kinase
Chanyanuch Laprasert, Chaisak Chansriniyom, Wacharee Limpanasithikul
January-March 2021, 12(1):32-39
Macrophages play major roles to produce several pro-inflammatory and inflammatory mediators in chronic inflammatory diseases. All current anti-inflammatory drugs target these mediators to alleviate inflammation. Searching for new anti-inflammatory agents is always needed due to problems from the clinical use of current anti-inflammatory drugs. We intended to evaluate the anti-inflammatory potential of three main compounds, arborinine, methylatalaphylline, and S-deoxydihydroglyparvin (DDGP), from Glycosmis parva leaves and branches on macrophage stimulated by lipopolysaccharide (LPS). Only DDGP demonstrated a potent inhibitor of LPS-activated macrophages. Results indicated that the mRNA level of inducible nitric oxide synthase (iNOS) was inhibited by the treatment in accompany with the decreased nitric oxide (IC50 at 3.47 ± 0.1 μM). DDGP was shown to suppress tumor necrosis factor-α, interleukin (IL)-1, and IL-6 at the mRNA expression and at the released protein levels. In addition, DDGP inhibited the several chemokines, monocyte chemoattractant protein-1 and macrophage inflammatory proteins-1α, and enzymes for prostaglandin (PG) synthesis. It also inhibited PGE2 production. On LPS signaling pathways, DDGP profoundly decreased phosphorylation of p38 mitogen-activated protein kinase (MAPK) in the LPS-treated cells. It had little or no effect on the activation of JNK, ERK and nuclear factor kappa B. In conclusion, results suggested that DDGP from G. parva inhibited expression and production of inflammatory molecules in LPS-activated macrophages through suppressing p38 MAPK activation. DDGP should be a good candidate anti-inflammatory agent in the future.
  1,521 218 -
A single dose of in situ gel formulation of antimalarial drug chloroquine phosphate as a sustained prophylactic candidate for COVID-19
Noha Talal Zelai
January-March 2021, 12(1):57-60
In the ongoing COVID-19 outbreak, a prophylactic drug is strongly needed to stop the spread of this disease. Chloroquine (CQ) has been proposed as a prophylactic for individuals who are likely to be exposed to the virus. This study aimed to study the ability of CQ to act as a prophylactic treatment for susceptible people. The pharmacokinetic profiles of in situ gel and free CQ phosphate were determined using high-performance liquid chromatography. The effects of both formulations were examined on both liver and kidney functions. CQ levels were sustained in the plasma of both free and in situ gel-treated groups. Thus, our study shows that the in situ gel of CQ provides sustained release of CQ that is given only as a single dose. However, it should be used cautiously in patients with liver or kidney dysfunction.
  1,400 203 1
Relaxation effects of Eriobotrya japonica toward tracheal smooth muscle via action mechanism on histamine-1 receptor and phosphodiesterase-5 enzyme
Marianne Marianne, Dadang Irfan Husori, Rosnani Nasution, Annisa Wismar, Aspan Ali Pranata
January-March 2021, 12(1):67-72
The Eriobotrya japonica leaves have the activity to relax the smooth muscle in the respiratory tract. However, the mechanism of action due to that activity has never been carried out. This study aims to determine the relaxation effects of E. japonica leaves extract in the isolated trachea of the guinea pigs through the inhibition of the histamine-1 (H-1) receptor and the phosphodiesterase-5 (PDE-5) enzyme. The determination of the relaxation effects was carried out by using histamine to contract smooth muscle within the tracheal tract, followed by adding cumulative concentrations of extract. Michaelis–Menten kinetics equation was used to determine the antagonist type of extract toward H-1 receptor. The understanding of mechanism of action of the extract toward PDE-5 enzyme was performed by incubating the smooth muscle using sildenafil. The percentage value of responses, originated from the relaxation effect of the extract toward the trachea was analyzed by using the t-independent test. The result showed that the extract was able to relax the smooth muscle, which was contracted by histamine, and there was a positive correlation between concentration and relaxation effect (P < 0.05; r = 0.973). The extract also antagonized the histamine as a noncompetitive antagonist. The incubation within the trachea with sildenafil demonstrated equal relaxation effect, produced by the extract. It can be concluded that E. japonica extract had relaxation effect within the isolated trachea as antagonist noncompetitive toward H-1 receptor and inhibitor of the PDE-5 enzyme.
  1,274 205 1