Javanese turmeric (Curcuma xanthorrhiza Roxb.) is known for its diverse pharmacological activities due to its rich phytoconstituents, including curcuminoids and xanthorrhizol. Typically, these compounds are extracted using organic solvents, which pose health and environmental risks. Therefore, safer and more environmentally friendly green extraction methods are being developed. This study investigated the effect of ultrasound-assisted extraction (UAE) combined with natural deep eutectic solvents (NADES) based on choline chloride and organic acids (lactic, malic, and citric acid) to find the best combination for extracting curcuminoids and xanthorrhizol from Javanese turmeric. Results showed that UAE using choline chloride and malic acid (1:1) (ChCl-MA) yielded the best results. The Box-Behnken Design optimized water addition, solvent-to-powder ratio, and extraction time, with optimal conditions being 25 % water addition, a 20 mL/g ratio, and a 15-minute extraction time. This method yielded 4.58 mg/g of curcuminoids and 12.93 mg/g of xanthorrhizol. Furthermore, the ChCl-MA NADES with UAE extraction showed more cytoselective activity towards the HeLa cancer cell line compared to the non-cancer HaCaT cell line. In contrast, traditional ethanol extraction was non-selective, as indicated by similar cell viability reductions in both HeLa and HaCaT cells at 6.25 ppm. Collectively, this study is the first to report the optimal NADES combination with UAE, based on salts and organic acids, for the extraction of Javanese turmeric rhizomes with selective cytotoxic effects against cancer cells. These findings may contribute to the development of novel, naturally derived anticancer agents using green extraction techniques.
Orthosiphon aristatus has been known for its medicinal uses. One of the compounds responsible for the pharmacological activities of O. aristatus is a flavonoid called Eupatorin (EUP). EUP has been studied for its pharmacological activities, including anti-inflammatory, vasodilating, antiproliferative, hepatoprotective, analgesic, and antidiabetic properties. Despite its importance and abundance, currently, there is no published paper that reviews the characteristics, pharmacological activities and isolation methods of EUP. This review summarizes the botanical origin, phytochemical characteristics, pharmacological activities, isolation, as well as identification and characterization methods of EUP from O. aristatus. This paper also compares different isolation methods based on the parameters and the resulting yields. Various isolation methods had been used to obtain EUP. Reverse-phase high-performance liquid chromatography (HPLC) is the most commonly used method to isolate EUP, followed by preparative thin layer chromatography (TLC) and crystallization for the purification. Various spectroscopic methods, including UV-Vis, FT-IR, Mass, and NMR spectroscopy have been commonly used to identify and characterize EUP. This paper provides a comprehensive insight into EUP from O. aristatus which might be beneficial for future research using this compound.
7 September 2023 in International Journal of Applied Pharmaceutics
Objective: This study was aimed to study the effect of degree of esterification (DE) on the thiolation of pectin, the potential to be used as materials for buccal delivery of diclofenac as well as the effect of DE on the physicochemical and mucoadhesive properties of the buccal films. Methods: Low-methoxyl pectin (LMP) and high-methoxyl pectin (HMP) were synthesized into low-methoxyl thiolated pectin (LMTP) and high-methoxyl thiolated pectin (HMTP) by esterification reaction using thioglycolic acid (TGA). The degree of thiolation was evaluated using Ellman’s reaction and FT-IR. Pectins were fabricated into buccal films with diclofenac as a drug model and glycerin as the plasticizer. The obtained films were then studied for swelling and erosion percentage, mucoadhesion time, and in vitro drug release. Results: HMTP and LMTP showed no significant difference in the degree of thiolation regardless of DE (p>0.05). The fabricated LMTP and HMTP films showed significantly higher mucoadhesion time and swelling than HMP and LMP (p<0.05). Moreover, HMTP and LMTP also exhibited sustained release of diclofenac compared to LMP (p<0.05). HMTP showed the highest mucoadhesion time, swelling capacity, and retention of drug release among all groups (p<0.05). Conclusion: Thiolated pectin showed prospective potential to be utilized as a biopolymer for buccal delivery of diclofenac with improved mucoadhesion and controlled drug delivery, regardless of their DE.
Background: The exploration of bryophytes biodiversity in Indonesia due to its abundance and the bioactivity of its phytochemical content, such as alkaloids and polyphenols, has received increased interest. Despite some species proven to possess pharmacological properties, the antiproliferative study of Indonesian native moss, such as the Pogonatum genus, is limited. Hence, this study aims to evaluate the anticancer effects of Pogonatum neesii Dozy antiproliferative activity on colon and cervical cancer through in silico and in vitro methods. Methods: Molecular docking analysis using Autodock VINA in PyRx softwre was conducted between natural compounds found on P. neesii and several target proteins, DNA (cytosine-5)- methyltransferase 1 (DMT-1) (Protein Data Bank (PDB) id: 4WXX) in colon cancer and B-cell lymphoma 2 (Bcl-2) (PDB id: 4LXD) in cervical cancer. Afterwards, total phenolic and alkaloid contents were measured. Subsequently, P. neesii was tested on HaCaT (keratinocytes), HEK293 (human embryonic kidney), HT-29 (colorectal cancer models) and HeLa (cervical cancer model) to observe its cytotoxicity. Results: Out of eight compounds, chlorogenate was found to exert the best binding energy with target proteins, although it had lower binding affinity than the protein’s natural ligand. However, the biological, drug-likeness, and toxicity analysis suggested the drug potency of the compound, thus we did the in vitro analysis. P. neesii showed significant cytotoxic effects on HT-29 and HeLa cells, while it did not exert any cytotoxic effects on HaCaT and HEK-293 cells, at the same concentrations. Conclusion: P. neesii has been shown to have the potential as an anticancer agent through in silico and in vitro analysis, where the extract showed selective cytotoxicity towards cancer cell lines and cytocompatibility towards normal cell lines. Chlorogenate was pinpointed as the compound with the most activity and interaction with the target proteins in both cancers.
Skin aging is driven by oxidative stress, extracellular matrix degradation, and ultraviolet-B (UVB)-induced cellular injury. Plant-derived bioactives with multi-targeted protective actions offer promising avenues for cosmeceutical development. This study assessed ethanolic leaf extracts of Vitex trifolia, an Indonesian medicinal plant traditionally used for skin disorders. Phytochemical analysis showed a total phenolic content of 78.52 ± 0.01 mg GAE/g and total flavonoid content of 1.99 ± 0.02 mg QE/g. LC–HRMS profiling identified major flavonoid and phenolic acid derivatives. Antioxidant assays demonstrated strong radical-scavenging and reducing activities, with IC50 values of 63.47 ± 0.24 (DPPH) and 70.13 ± 1.28 μg/mL (ABTS) and a Ferric Reducing Antioxidant Power (FRAP) value of 36.3 ± 0.18 FeSO4 eq/100 g. Enzymatic studies confirmed potent collagenase inhibition (IC50 = 27.94 ± 3.20 μg/mL) and moderate elastase inhibition, supported by molecular docking analysis. In HaCaT keratinocytes, the extract remained non-cytotoxic up to 100 μg/mL and exerted cytoprotective activity against UVB-induced damage at 12.5–50 μg/mL. The extract also downregulated UVB-induced matrix metalloproteinase-1 (MMP-1) and matrix metalloproteinase-9 (MMP-9) expression up to 42% and 69%, respectively, outperforming ascorbic acid. These findings highlight V. trifolia as a multifunctional natural candidate for anti-photoaging cosmeceutical applications over single-compound antioxidants, as demonstrated by its combined antioxidant, enzyme-inhibitory, cytoprotective, and MMP-modulating activities, as well as a wider cell safety profile.
Skin aging is driven by oxidative stress, extracellular matrix degradation, and UVB-induced cellular injury. Plant-derived bioactives with multi-targeted protective actions offer promising avenues for cosmeceutical development. This study assessed ethanolic leaf extracts of Vitex trifolia, an Indonesian medicinal plant traditionally used for skin disorders. Phytochemical analysis showed a total phenolic content of 78.52 ± 0.01 mg GAE/g and total flavonoid content of 1.99 ± 0.02 mg QE/g. LC–HRMS profiling identified major metabolites including casticin and several flavonoid and phenolic acid derivatives. Antioxidant assays demonstrated strong radical-scavenging and reducing activities, with IC₅₀ value of 63.47 ± 0.24 (DPPH) and 70.13 ± 1.28 μg/mL (ABTS), and a FRAP value of 36.3 ± 0.18 FeSO₄ eq/100 g. Enzymatic studies confirmed potent collagenase inhibition (IC₅₀=27.94 ± 3.20 μg/mL) and moderate elastase inhibition. In HaCaT keratinocytes, V. trifolia extract remained non-toxic up to 100 μg/mL and exerted cytoprotective activity against UVB-induced damage at 12.5–50 μg/mL. The extract also downregulated UVB-induced MMP-1 and MMP-9 expression up to 42% and 69%, respectively, outperforming ascorbic acid. These findings highlight V. trifolia as a promising natural anti-aging agent with strong antioxidant, protease-inhibitory and photoprotective properties, supporting its potential as safe and effective cosmeceutical ingredient.