A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, ¹H-NMR, ¹³C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT (LC₅₀ value 29.80–1704.23 µM); most of the compound exhibited cytotoxic activity against HeLa cell lines, which is comparable to the activity of cisplatin (IC₅₀ value 40.65–95.55 µM), and most of the compound tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC₅₀ value 7.86–35.88 µM). However, the selectivity index (SI) of the compounds was low (<1–1.96). Among the synthesized compounds, compound 1b was the most cytotoxic and selective against MCF7 cell lines. It could be considered for further development to obtain the more active and selective chemotherapeutic agents against breast cancer.

Introduction: Ageratum conyzoides Linn is one of the Indonesian herbs are used as folk medicine. There are many studies to the therapeutic activity. However, the study of the influence in extraction parameters and how to standardize different batches of plant is still limited. Objective: The present study was designed to investigate the influence of extraction parameters on the variables matter, yield, phytochemical profile, and total quercetin from A. conyzoides L. leaves extract. The study also evaluates Liquid Chromatography-Mass Spectroscopy (LC-MS) and TLC fingerprint profiles of the extract to determine the proper quality of plant material of A. conyzoides L. leaves. Methods: Different temperatures (from 0°C to 60°C), solvent types (water and 70% ethanol (%v/v), and extraction time (192 h VS 2 h) were used to investigate the influence of extraction parameters. The profiles of extract were performed by TLC and LC-MS method. Results: The extract yield was influenced by temperature, solvent types, and time extraction. Our results suggest that the digestion technique at 60°C with 70% ethanol for 2h was recommended for the extraction method to obtained high yield and quercetin content as bioactive compound in A. conyzoides L. leaves extract. The range of quercetin content (40-52 ppm) combined with TLC and LC-MS profile can be used to determine the proper quality of plant material. Conclusion: All parameter of extraction have an affect on the yield extract and total quercetin on the final extract. Thus, there is a need an optimized method to obtain the suitable method.

Prior study has shown that Ageratum conyzoides L. extract that containing quercetin has been proved to prevent inflammation and proteoglycan degradation by inhibiting tumor necrosis factor-alpha and matrix metalloproteinase (MMP-9) expression. Target of osteoarthritis (OA) treatment was in the synovial joint that requiring a drug delivery system. The aim of this study was to prove the efficacy of quercetin-loaded lecithin-chitosan nanoparticles on the OA model rats by observed its effect on interleukin (IL-1) β, MMP-9, MMP-13, and a disintegrin and metalloproteinase with thrombospondin motifs (ADAMTS-5) expressions. In this study, 70 white male Sprague Dawley rats were divided into 14 groups, 7 groups each for destabilization of medial meniscus (DMM) and monoiodoacetate (MIA)-induced OA. After 28 days from induction, SHAM and negative group received gel base topically; positive group received sodium diclofenac gel; three-dose group received each 0.84, 1.68, 3.36 mg/g quercetin-loaded nanoparticles gel; and A. conyzoides L. group received A. conyzoides L. extract gel. Each group gets treatment until day 70, and then, blood sample was collected for serum analysis; knee joint was isolated and subjected to histology samples treatment. Quercetin-loaded nanoparticle gel dose 1 (0.84 mg/g gel), dose 2 (1.68 mg/g gel), dose 3 (3.36 mg/g), and A. conyzoides L. extract gel could decreased the level of IL-1 β, MMP-9, MMP-13, ADAMTS-5, and increasing color intensity significantly on histopathological observations on DMM and MIA-induced OA.

To analyze the effects of Ageratum conyzoides L. on the monosodium iodoacetate induced osteoarthritis rats. Thin layer chromatography was performed to analyze the constituents of the babandotan extract leaves. White male Sprague-Dawley rats used in this study were divided into 6 groups: normal control and negative control groups, both given 0.5% carboxymethyl cellulose; the positive control group that was given glucosamine and chondroitin suspension (486 mg/200 g B.W.); the 3 dose variation extract groups including dose 1, 2, and 3 that were given 40, 80, and 160 mg/200 g B.W. respectively on day 29 until 50. All the groups were induced with 0.05 mL monosodium iodoacetate (20 mg/mL) on day 1, except normal control induced by saline. Measurement of edema volume of rat knees was performed on day 0, 8, 15, 22, 29, 43, and 50. Hematology data was measured at day 1, 29 and 50. Serum was collected at day 50 to evaluate TNF-α and MMP-9 by ELISA. Cartilage histopathology was evaluated by staining with H&E and Safranin-O-fast green staining on day 50. The babandotan leaves extract dose 2 (80 mg/200 g B.W.) and dose 3 (160 mg/200 g B.W.) could decrease the edema volume, increase the area and thickness of articular cartilage, and increase proteoglycan level. Particularly, dose 3 (160 mg/200 g B.W.) of extract babandotan leaves were able to significantly decrease the number of leukocytes, lymphocytes and udem volume, and decrease TNF alpha and MMP-9 levels. Babandotan leaves extract can recover inflammation and cartilages degradation by inhibiting TNF-α in inflammation processes and MMP-9 in the collagenase reaction in the cartilages.

Background: Binahong is a plant that has the potential to be used as a traditional herbal medicine in Indonesia, and has several kinds of classes of compounds, one of them is a flavonoids glycosides (vitexin). Previous research reported that binahong leaves have pharmacological activities as antihyperglycemic, antihyperlipidemic, antibacterial, and others. A traditional plant that has proven efficacious needs to be standardized to ensure the quality and its safety. Objective: This study aimed to characteristics of binahong leaves simplicia obtained from Bogor, West Java. Materials and Methods: The crude extract was obtained by the maceration method using 40%, 70%, and 96% ethanol solvent. The selected extract then standardized, which includes macroscopic and microscopic observations and sets the standard parameter values binahong leaf extract. Parameters LCMS to identify active compounds semiquantitatively. Results: The yield of binahong ethanol extract from 40%, 70%, 96% showed a value of 10.9%, 11.4%, and 12.32%, respectively. From these results, 96% ethanol extract has proceeded for standardization. Macroscopic observation results showed that binahong leaves simplicia has a fine and notched form with 5-10 cm long and 3-7 cm diameter. The microscopic binahong leaves contain palisade tissue, parenchymal tissue, chlorophyll grains, rosette Caoxalate crystals, and spiral type. Phytochemical screening of binahong leaves showed the presence of alkaloids, flavonoids, saponins, tannins, steroids, and phenolic compounds.The standardization of binahong leaves ethanol extract down showed a levels of ethanol-soluble extract> 14.8%, water-soluble extract content > 13.5%, drying < 10%, water content < 8.9%, total ash content < 7.2%. LCMS profiles showed that ethanolic extract 40%, 70%, and 96% all contained vitexin at retention time 5.02 minutes, and m/z values 433.1111.

Patients with diabetes are 1.6 times more likely to use complementary alternative medicine than nondiabetic patients. Previous studies have shown that Anredera cordifolia (Tenore) Steen. (A. cordifolia) leaf extract has the capacity to lower blood glucose, but the actual mechanisms are unclear. Therefore, in this study, we explored the effect of A. cordifolia leaf extract on the metabolism of fatty acids and amino acids. Six-week-old male Wistar rats were randomly divided into six experimental groups (n=5 per group). Two groups were fed with a regular diet or a high-fat diet (HFD) for six weeks. The regular diet and HFD groups were administered with 0.5 carboxymethylcellulose as a vehicle, and HFD rats were also fed with a suspension of glibenclamide (0.51mg/kg body weight (BW)) or A. cordifolia leaf extract (25, 50, and 100mg/kg BW). During the whole treatment, BW and food intake were recorded weekly. The rats were euthanized seven weeks after treatment. Blood glucose was evaluated by spectrophotometry, while fatty acids and amino acids were evaluated using a gas chromatography/flame ionization detector (GC/FID). All doses of A. cordifolia administration reduced blood glucose significantly, and 50mg/kg BW was most effective in lowering blood glucose, similar to the effects of glibenclamide. A. cordifolia leaf extract affected the levels of medium-chain fatty acids, especially at 50mg/kg BW. In contrast, glibenclamide affected long-chain fatty acids (LCFAs) to lower blood glucose. Based on the analysis conducted, we conclude that administration of A. cordifolia leaf extract can decrease blood glucose levels by regulating fatty acid metabolism and that a dose of 50mg/kg BW in rats was the optimal dose.